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Click here for the function of HRH2. Edit this page in Wiki Genes - HRH2 or see Wiki Gene. Hyper-IgE syndrome and H2-receptor blockade. Paper-6439721. Prolactin responses to histamine H2 receptor antagonists. Paper-3649278. H2R and beta-actin mRNA were amplified by RT-PCR. Paper-1854170. H4R or H2R stimulation suppressed IL-12p70 production in MoDC. Paper-10801253. Effect of histamine H2-receptor antagonists on vitamin B12 absorption. Paper-7216693. Histamine H2 receptor blockade in patients with hyperparathyroidism. Paper-4803388. Dynamin could associate with H2R both in vitro and in vivo. Paper-12956429. VIP and histamine H2 receptor activity in human fetal gastric glands. Paper-5403164. In this study, we identified a GTPase dynamin as a binding partner of H2R. Paper-12956429. Recently, H1- and H2-receptor genes have been cloned in various animal species. Paper-8077794. Epithelial cells also expressed H1R, H2R and, to some extent, H4R. Paper-11392854. Immune cells expressed mRNA and protein for H1R, H2R, and low levels of H4R. Paper-11392854. H2-receptor antagonists are indicated in GOR complicated by esophagitis. Paper-11593416. H2-receptor antagonists inhibit gastric ADH activity to a variable extent. Paper-1871338. Histamine H2 receptor ( H2R) is a member of G protein-coupled receptor family. Paper-12956429. H2R overexpression induced PDE activity stimulation and GRK2 overexpression. Paper-11771574. The effects of histamine H2-receptor antagonists on PHA induced lymphocyte proliferation. Paper-4669458. H2 receptor antagonists and an agonist ( impromidine) inhibit intestinal DAO. Paper-4499352. Neurobehavioral syndrome induced by H2-receptor blocker withdrawal: possible role of prolactin. Paper-963382. The H2 receptor message was mainly down-regulated by activation of the H1 receptor protein. Paper-8288618. RT-PCR showed that SW756 expressed mRNA for CB1, CB2, H1R, H2R, and H4R. Paper-12754476. Histamine increases the expression of LOX-1 via H2 receptor in human monocytic THP-1 cells. Paper-9098462. This rebound in GH secretion might indicate an inhibitory effect of TRH during H2-receptor stimulation. Paper-4784579. Proton pump inhibitors are more effective than H2-receptor antagonists in virtually all cases. Paper-11210226. This may reflect differences in H1 to H2 receptor density or cell responsiveness to receptor stimulation. Paper-2882143. Efficacy of H2 receptor antagonists in the treatment of gastroesophageal reflux disease and its symptoms. Paper-1227789. Finally, K44E dynamin did not affect ERK1/2 activation induced by internalization-deficient H2R. Paper-12956429. Proton pump inhibitors are more potent inhibitors of acid secretion than H2-receptor antagonists. Paper-786264. Histamine receptor immunoreactivity ( H1R, H2R, H3R, H4R) was found in situ and in vitro. Paper-12119807. Treatment of peptic ulcer in the elderly. Proton pump inhibitors and histamine H2 receptor antagonists. Paper-856192. Cimetidine, an H2 receptor antagonist, is a potent stimulant of PRL secretion in normal women. Paper-6046887. H2 receptor antagonists, cytochrome P450, and paracetamol-induced hepatotoxicity. Paper-11932930. Like other G protein-coupled receptors, exposure of H2r to agonists produces a desensitization of the response. Paper-9070038. Histamine H2 receptor desensitization: involvement of a select array of G protein-coupled receptor kinases. Paper-9070038. Effect of histamine H2-receptor stimulation on bombesin- and peptone- stimulated gastrin release in man. Paper-5254446. Cimetidine and other H2-receptor antagonists as inhibitors of human E3 aldehyde dehydrogenase. Paper-1125122. This response was reduced by the histamine H2-receptor antagonist ranitidine ( IC50 = 3 X 10(-6) mol/l). Paper-5301253. It has been reported that cimetidine, an H2-receptor antagonist, stimulates PRL secretion in postpartum. Paper-4870326. Evaluation of combined H1- and H2-receptor blocking agents in the treatment of seasonal allergic rhinitis. Paper-4250908. Selective expression of histamine receptors H1R, H2R, and H4R, but not H3R, in the human intestinal tract. Paper-11392854. H1 and H2 receptor-mediated actions are mostly excitatory; H3 receptors act as inhibitory auto- and heteroreceptors. Paper-12883156. Effect of the new H2-receptor antagonist ranitidine on plasma prolactin levels in duodenal ulcer patients. Paper-3922702. Four- to six-week therapy of H2-receptor antagonist and antacid had no influence on serum gastrin concentrations. Paper-7744707. Furthermore, ERK1/2 activation via H2R is likely dependent of the endocytotic process rather than dynamin itself. Paper-12956429. Stimulation of postprandial somatostatin release by H2-receptor agonists and prostaglandins has been reported. Paper-5407268. Metformin and vitamin B12 deficiency: the role of H2 receptor antagonists and proton pump inhibitors. Paper-12444890. The effects of histamine H2-receptor antagonists on acetylcholinesterase and pseudocholinesterase activity were studied. Paper-5440527. Proton-pump inhibitors or H2-receptor antagonists for Helicobacter pylori eradication-a meta-analysis. Paper-517359. These results suggest a predominantly H2-receptor mediated phenomenon with a minor H1-receptor mediated component. Paper-5261622. Chronic beta 1-adrenoceptor blockade sensitises the H1 and H2 receptor systems in human atrium: rôle of cyclic nucleotides. Paper-689867. H2-receptor blockade induces peptide YY and enteroglucagon-secreting gastric carcinoids in mastomys. Paper-6485901. Proton pump inhibitors, histamine H2 receptor antagonists, and other antacid medications and the risk of fracture. Paper-12197089. Long-term effects of histamine H2-receptor antagonists on serum parathyroid hormone in chronic renal failure. Paper-4853290. The recent observation of constitutive H1- and H2-receptor activity has led to a reclassification of H1- and H2-antagonists. Paper-9509055. In fura-loaded H1- and H2-receptor-expressing cells histamine induced the release of calcium from intracellular stores. Paper-1133782. H2 receptor antagonist treatment had little effect on tissue type or urokinase type plasminogen activator activity. Paper-7848823. Histamine H2 receptor trafficking: role of arrestin, dynamin, and clathrin in histamine H2 receptor internalization. Paper-12949959. H2-Receptor antagonists and omeprazole, a H-K ATPase inhibitor, inhibit acid secretion from the parietal cells. Paper-6436952. Dimaprit analogues inhibit tyrosinase via a disulphide breakdown product independently of the histamine H2 receptor. Paper-8047757. These results suggest that the agonist-induced H2R internalization and ERK1/2 activation are partially dynamin-dependent. Paper-12956429. These options include the proton pump inhibitors, misoprostil, double-dose H2-receptor blockers and the COX-2 selective NSAIDs. Paper-10683266. The results indicate an effect of H2-receptor antagonists on physiological functions in the control of PRL secretion. Paper-3943129. The Ki value of the E3 isozyme for cimetidine was the same as the in vitro dissociation constant for the H2-receptor. Paper-1125122. Histamine H2 receptor mediated dual signaling: mapping of structural requirements using beta2 adrenergic chimeric receptors. Paper-8658154. Previous reports have suggested that the H2-receptor blocker, cimetidine, can inhibit parathyroid hormone ( PTH) release. Paper-3768031. Down-regulation of the H1 receptor message seemed to be a net result of H1 and H2 receptor activation. Paper-8288618. However, H2 receptor antagonist ( ranitidine) and H3/ H4 receptor antagonist ( thioperamide) did not alter this effect. Paper-11333706. H1 and H2-receptor antagonists have been successfully used for a long time in the treatment of allergy and ulcer, respectively. Paper-8077794. Proton-pump inhibitors and H2-receptor antagonists accounted for 261 (44.5%) and 307 (52.5%) of prescriptions respectively. Paper-8459805. The decrease in TNF-alpha production by dimaprit was reversed by cimetidine, a histamine H2 receptor antagonist. Paper-1046626. Dimaprit--[S-[3-(N,N-dimethylamino)propyl]isothiourea]--a highly specific histamine H2-receptor agonist. Part 1. Pharmacology. 1977. Paper-8217943. H1 receptor agonist ( betahistine), but not H2 receptor agonist ( amthamine), induced phosphorylation of STAT4. Paper-11333706. In the present study, we demonstrate that H1R, H2R and H4R are expressed in colon carcinoma and the adjacent normal mucosa. Paper-12774371. Attenuation of the aggressive gastric juice by anticholinergics and antihistamines of the H2 receptor blocker type and secretin. Paper-2314730. We hypothesized that SAR subjects express higher nasal mucosal histamine receptor 1 ( H1R) and 2 ( H2R) levels than do NR subjects. Paper-9899807. All H2-receptor antagonists clearly antagonized histamine- induced NKCC enhancement in monocyte-containing effector cells. Paper-5736930. Furthermore, c-Myc levels decreased following forskolin treatment, while the histamine H2 receptor agonist dimaprit had no effect. Paper-1572589. RESULTS: We found that H1R, H2R, and H4R mRNA were expressed throughout the gastrointestinal tract, while H3R mRNA was absent. Paper-11392854. OBJECTIVE: To discuss the potential of histamine H2-receptor antagonists (H2RAs) to cause malabsorption of vitamin B12 (cyanocobalamin). Paper-7216693. RESULTS: Proton pump blockers were used by 275 women, H2 receptor antagonists by 255 women, and both categories of drugs by 20 women. Paper-1590666. The time dependency and extent of histamine induced down-regulation varied between the H1 and H2 receptor message. Paper-8288618. Human gastric alcohol dehydrogenase: its inhibition by H2-receptor antagonists, and its effect on the bioavailability of ethanol. Paper-6808989. Drug interactions of H2-receptor antagonists involving cytochrome P450 (CYPs) enzymes: from the laboratory to the clinic. Paper-2007239. Agonist-induced internalization of histamine H2 receptor and activation of extracellular signal- regulated kinases are dynamin-dependent. Paper-12956429. Intestinal fibroblasts exclusively expressed H1R while the muscular layers of human intestine stained positive for both H1R and H2R. Paper-11392854. In particular, histamine, acting upon the H2 receptor for a short period of time, increased IL-10 production and reduced IL-12 secretion. Paper-8864366. AIM: In this study, we evaluated the efficacy of H2-receptor antagonist ( famotidine) and 5-HT4 receptor agonist ( mosapride citrate). Paper-11283097. Misoprostol, high-dose H2-receptor antagonists, proton-pump inhibitors, and COX-2 inhibitors have been shown to reduce this risk. Paper-10514982. Fasting and secretin- stimulated serum gastrin levels were not affected by long-term treatment with histamine H2-receptor antagonists. Paper-3008061. H1R and H2R transcript levels have been found to be up-regulated in perennial - but not in seasonal - allergic rhinitis ( AR). Paper-11233462. H2-receptor antagonists differentially inhibit cytochrome P450 and this may affect the rate at which benzodiazepines are metabolised. Paper-7778489. Ranitidine, another H2-receptor antagonist, has been shown to have an extremely low level of interaction with the cytochrome P450 system. Paper-5466432. Incubation of lymphocytes with 50 U/ml IL-2 alone in 3-day culture significantly (p less than 0.005) enhanced H2 receptor expression. Paper-7265844. RESULTS: The mRNA of the H1R, H2R and H4R could be detected in murine BM-derived DC, while mRNA of the H3R was found to be low or undetectable. Paper-12992396. The prescription of sodium citrate and the H2 receptor antagonist ranitidine has superseded that of Mist. magnesium trisilicate. Paper-6794679. The percentage of relapse-free patients, 1 year after DU or GU healing, with CBS is substantially higher than is the case with H2-receptor blockers. Paper-5515815. Cimetidine, an H2 receptor antagonist, blocked chemoattractant production, whereas diphenhydramine, an H1 receptor antagonist, did not. Paper-5256867. Experimental evidence suggested that H2-receptor antagonists may inhibit not only hepatic but also adrenal cytochrome P-450 dependent monooxygenases. Paper-7443862. The inhibitory effects of histamine on CD14 expression were antagonized by H2-receptor antagonist, but not by H1 and H3/ H4 antagonist. Paper-9988439. Pretreatment H2 receptor antagonists that differ in P450 modulation activity: comparative effects on paclitaxel clearance rates and neutropenia. Paper-258826. However, the immunohistochemical localization of histamine receptor subtypes ( H1R, H2R, H3R, and H4R) in human nasal mucosa is unknown. Paper-10343272. The evidence is consistent with sensitisation of both the histamine H1 and histamine H2 receptor systems by chronic beta 1-adrenoceptor blockade. Paper-689867. Proton pump inhibitors were mostly prescribed for reflux disease (52.7%) and H2-receptor antagonists for non-specific dyspepsia (43.6%). Paper-1604933. Furthermore, activation of extracellular-signal regulated kinases ERK1/2 in response to dimaprit, an H2R agonist, was attenuated by K44E-dynamin. Paper-12956429. Immunohistochemical staining revealed expression patterns of H1R, H2R and H4R similar to those suggested by the mRNA and Western blot results. Paper-12774371. In addition, osteogenic differentiation of MSCs was inhibited by the HRH1 inhibitor mepyramine but not the HRH2 inhibitor ranitidine. Paper-13404540. Proton pump inhibitors (PPIs) and histamine H2 receptor antagonists (H2RAs) are two major acid-suppressing drugs used for the treatment of GERD. Paper-9715979. The therapeutic use of CT in gastric hypersecretory states appears to be inferior and less practicable compared to the histamine-H2-receptor antagonists. Paper-3703737. Recent investigations suggest that H1R signaling on lymphocytes may enhance whereas activation of the H2R may inhibit lymphocyte responses. Paper-8567537. These changes persisted after H2 receptor blockade with cimetidine, but were completely abolished after H1 receptor blockade with diphenhydramine. Paper-5581148. Dimaprit, (S-[3-(N,N-dimethylamino)propyl]isothiourea). A highly specific histamine H2-receptor agonist. Part 2. Structure-activity considerations. Paper-2702151. Thus, in human skin, VIP- mediated vasodilation includes a NO-dependent component that could not be explained by H1- and H2-receptor activation. Paper-10940516. CONCLUSIONS: Our results suggest that histamine stimulated neutrophil adhesion is due to H1 and H2 receptor mediated activation of PLC, NOS and GC. Paper-1557113. Proton pump inhibitors produce a greater and longer-lasting degree of suppression of acidity than conventional doses of H2-receptor antagonists. Paper-165070. Small H1R agonists and 2-phenylhistamines interacted differentially with human and guinea pig H2R in terms of potency and efficacy, respectively. Paper-9720226. The released histamine begins the H2-receptor mediated sequence of events in the parietal cell, which results in activation of the gastric H+/K+ - ATPase. Paper-8246813. The efficacy of prophylactic administration of H1 and H2 receptor blockers to prevent adverse haemodynamic responses to heparin and protamine was studied. Paper-866965. In contrast, successful treatment of GER by H2-receptor antagonists in patients resistant to the acid-suppressing effects of omeprazole is rarely reported. Paper-364425. The modulation of the forskolin response was also observed after H2 receptor expression in HEK-293 and Sf9 cells or TSH receptor expression in COS-7 cells. Paper-1281290. Cimetidine, an H2 receptor antagonist, reversed the histamine (10(-5) M)-mediated increase in IL-1 alpha- induced IL-1 beta synthesis. Paper-7718629. Very important drug interactions are caused by inhibition of the hepatic microsomal enzyme cytochrome P450 by some of the H2-receptor antagonists. Paper-5442551. The alteration of the responsiveness of LOX-1 expression to histamine was related to suppressed expression of the H2 receptor in THP-1 macrophages. Paper-9098462. The histamine inhibition was shown to be specific for H2 receptor activation by blocking experiments with selective H1 and H2 receptor antagonists. Paper-7632849. This paper reviews the main steps in the research of the interactions of H2-receptor antagonist drugs with cytochrome P450 ( CYP) enzymes. Paper-2007239. Dimaprit, [S-[3-(N,N-dimethylamino)propyl]isothiourea]. A highly specific histamine H2-receptor agonist. Part 2. Structure-activity considerations. 1977. Paper-8217944. CONCLUSIONS: These results suggest that histamine-induced stimulation of PDE4 is mediated by the H2 receptor and related to intracellular levels of cAMP. Paper-9898164. Lack of association between atopic asthma and polymorphisms of the histamine H1 receptor, histamine H2 receptor, and histamine N-methyltransferase genes. Paper-2176308. It is thought that the difference between these two H2-receptor antagonists may lie in their affinities for binding to the cytochrome P-450 enzymes. Paper-5466485. The histamine H2-receptor antagonists cimetidine, ranitidine and tiotidine suppressed NK cell cytotoxicity ( NKCC) at a high concentration (10(-3) M). Paper-5736930. CONCLUSION: Proton pump inhibitor treatment provides more consistent heartburn relief than an H2-receptor antagonist, or "step-up" or "step-down" therapy. Paper-8845941. The histamine H2-receptor antagonists have been identified as inhibitors of human liver aldehyde dehydrogenase (EC 1.2.1.3) isozymes, E1, E2, and E3. Paper-1125122. Histamine inhibits cell proliferation and modulates the expression of Bcl-2 family proteins via the H2 receptor in human pancreatic cancer cells. Paper-12391279. The H2 receptor agonist dimaprit (10 microM) or the H3 receptor agonist imetit (100 nM) were without significant effect on the membrane properties of SPNs. Paper-11368127. Histamine maintained NKp46 and NKG2D expression despite the presence of inhibitory phagocytes by targeting an H2 receptor on phagocytes. Paper-10601948. Symptomatic relief can be achieved with pro-kinetic agents, antacids, sucralfate suspension, H2-receptor antagonists and H(+)-K+ ATPase pump blockers. Paper-7212289. Effect of a new potent H2-receptor antagonist on meal- stimulated gastric acid secretion and serum gastrin concentration in duodenal ulcer patients. Paper-4697199. Comparison between dose-responses of prolactin, thyroid stimulating hormone and growth hormone to two different histamine H-2 receptor antagonists in normal men. Paper-3943129. It would appear that the stimulatory effect of cimetidine on serum prolactin concentration is not mediated through its histamine H2-receptor antagonist activity. Paper-3915384. The H2-receptor antagonists cimetidine and ranitidine were transferred from prescription only to over-the-counter ( OTC) status in Denmark on March 27, 1989. Paper-7005154. Tolerance to H2 receptor antagonist correlates well with the decline in efficacy against gastroesophageal reflux in patients with gastroesophageal reflux disease. Paper-12189908. The H2-receptor antagonist ranitidine completely reversed the inhibition of IL-4 and IFN-gamma production, whereas the agonist dimaprit mimicked this effect. Paper-1036237. Ranitidine is thought to spare phase I hepatic metabolism mediated by cytochrome P-450, unlike its counterpart H2-receptor antagonist cimetidine. Paper-5884211. Moreover, in HDC KO cells, hCG did not increase basal expression levels of HA H1 and H2 receptor genes, while the hormone showed a significant inducing effect in WT cells. Paper-12376868. Histamine and H2-receptor agonists inhibit the generation of superoxide anion from human neutrophils activated by FMLP and by substance P. Paper-6089326. The erection-promoting action of histamine is probably due to H2 receptor activation, although another histamine receptor, possibly H3, also seems to be involved. Paper-162360. Neither the histamine H2 receptor agonist dimaprit (1 mM) nor the histamine H3 receptor agonist S-(+)-alpha-methyl histamine (1 mM) altered short circuit current. Paper-368999. In seven healthy volunteers, we studied how histamine H2-receptor blockade affected the reflex response to hypovolaemia induced by lower-body negative pressure ( LBNP). Paper-6505254. BACKGROUND: Concomitant administration of an H1-receptor antagonist with an H2-receptor antagonist may enhance the wheal and flare suppression produced by the H1-antagonist. Paper-185191. In situ hybridization with a digoxigenin-labeled H2R cRNA probe was performed on surgical specimens of nasal turbinate of patients with allergic rhinitis. Paper-1854170. Inhibition of gastric alcohol dehydrogenase activity by histamine H2-receptor antagonists has no influence on the pharmacokinetics of ethanol after a moderate dose. Paper-8206660. Treatment with okadaic acid, an inhibitor of the protein phosphatase 2A ( PP2A) family of phosphatases, reduced the recovery of both H2r membrane sites and cAMP response. Paper-12949959. Functional analyses using dominant-negative form of dynamin (K44E-dynamin) revealed that cAMP production and the following H2R desensitization are independent of dynamin. Paper-12956429. The potential of famotidine, a new H2-receptor antagonist with a guanylthiazole ring structure, to interact with the cytochrome P450 system has been extensively evaluated. Paper-5466432. Successful omeprazole therapy in patients with symptomatic gastroesophageal reflux ( GER) refractory to treatment with H2-receptor antagonists has often been reported. Paper-364425. The present study shows that, unlike ranitidine, ebrotidine, a competitive H2-receptor antagonist, is also a non-competitive inhibitor of carbonic anhydrase I and II. Paper-1096509. These results indicate that in H2r-transfected COS-7 cells, exposure to an agonist caused desensitization controlled by H2r phosphorylation via GRK2 and GRK3. Paper-9070038. Intracytoplasmic domains of the human beta2 adrenergic receptor were substituted with the corresponding sequences of the human H2 receptor and stably expressed in HEK-293 cells. Paper-8658154. Histamine H2 receptor ( H2R) stimulation controls histamine release and mediates mucus secretion, suggesting that H2R might play some role in allergic rhinitis. Paper-1854170. Proton pump inhibitors are at least as effective, and may be more effective than histamine H2-receptor antagonists in achieving this pH goal and preventing bleeding. Paper-10760098. Failure of H2-receptor antagonists to affect serum calcium and immunoreactive parathyroid hormone levels in normal subjects and patients with primary hyperparathyroidism. Paper-4245468. Studies show that patients with peptic ulcer disease treated with the H2-receptor antagonist cimetidine show significant elevations in their HDL, HDL2, and HDL3 profiles. Paper-5466513. We describe two patients who demonstrated therapeutic responses to high dose H2-receptor antagonists after high dose omeprazole failed to suppress gastric acidity and GER. Paper-364425. The intravenous administration of 200 mg cimetidine, an H2-receptor antagonist, was followed by a significant and marked rise in serum prolactin levels in all control subjects. Paper-4084437. The studies using receptor subtype-selective agonists and antagonists suggested that the effect of histamine was mediated by H2 receptor but not by H1, H3 and H4 receptors. Paper-10348832. Prolonged high-dose histamine H2-receptor dosing compromises the feedback mechanism regulating gastrin release, whilst this is maintained during dosing with omeprazole. Paper-8014500. On the other hand, tolerance can now be explained by a gastrin- induced increase in ECL cell-derived histamine at the parietal cell H2-receptor competing with the antagonist. Paper-1548840. The recent progress in therapy if acid disease has relied heavily on the performance of drugs targeted against the H,K ATPase of the stomach and the H2 receptor antagonists. Paper-13293395. Histamine H2 receptor activity (cAMP generation) has been characterized in U-937 cells before and after retinoic acid-induced differentiation into monocyte-/macrophage-like cells. Paper-5084073. Zollinger-Ellison syndrome was treated with a histamine-H2-receptor blocker, and ectopic ACTH syndrome was controlled with trilostane, metyrapone and o,p'-DDD. Paper-8217270. The major classes of OTC medication to be considered in this light include antacids, histamine H2 receptor antagonists, NSAIDs, cough and cold preparations and the antiasthma products. Paper-641390. A prospective, open, multicenter clinical trial was set up to evaluate the potential interaction of ITF 282 with H2-receptor antagonists in patients affected with iron deficiency. Paper-7588162. Using specific histamine H1 and H2 receptor antagonists, evidence is presented for the existence of both H1 and H2 receptors on human articular chondrocytes in vitro. Paper-5565081. Although we do not provide direct evidence for H2r interaction with beta-arrestin, dynamin, and/or clathrin, our results support their involvement in H2r endocytosis. Paper-12949959. It is suggested that the absence of a interaction may be attributed to a lack of specificity of the H2 receptor antagonists for CYP3A, the isoenzyme responsible for CyA metabolism. Paper-496577. In further experiments, suppression of human polyclonal IgM PFC responses by Con A and interferons, substances that activate the SIRS pathway, was inhibited by H-2 receptor antagonists. Paper-5622258. Effect of systemically administered H1- and H2-receptor antagonists on nasal blood flow as measured with laser Doppler flowmetry in a provoked allergic reaction. Paper-653396. The biphasic response of the ratio of H+ and gastrin (H+/G) following each meal was suppressed by both H2-receptor antagonists, with numerically lower values obtained in R than in C. Paper-4902001. The beta-2-selective antagonist ICI118551 was a more potent inhibitor of acid production than both the beta-1 antagonist practolol and the H2-receptor antagonist cimetidine. Paper-5806476. Activation of the CCK2 receptor results in mobilization of histamine (and pancreastatin) from the ECL cells with consequent activation of the parietal cell histamine H2 receptor. Paper-1880369. Modulation of the permeability of H2 receptor antagonists cimetidine and ranitidine by P-glycoprotein in rat intestine and the human colonic cell line Caco-2. Paper-1708119. Its various actions are mediated not only by the two well known H1- and H2-receptor subclasses but also by the recently discovered H3-receptors, with distinct localization and pharmacology. Paper-5403792. After 24-h histamine treatment, known to desensitize H1 receptors, reapplication of histamine increased cell coupling in a way prevented by ranitidine, an H2 receptor blocker. Paper-10613257. In another group of six healthy subjects the postprandial plasma PP release was not affected by inhibition of the gastric H+ secretion by the H2-receptor antagonist ranitidine. Paper-4201392. Previously, omega-guanidino- and omega-aminoalkanamides, structurally derived from arpromidine-like histamine H2 receptor agonists, were reported as novel neuropeptide Y Y1 antagonists. Paper-1683745. Mast cell chemotaxis toward histamine could be blocked by the dual H3/ H4 receptor antagonist thioperamide, but not by H1 or H2 receptor antagonists. Paper-9720234. However, other known or unknown intracellular signals, could also be triggered by the stimulation in a transfected cell of a single H1 or H2 receptor through coupling to different G-proteins. Paper-8077794. The effects on airflow resistance of an inhaled H1 receptor antagonist, clemastine, and an H2 receptor antagonist, cimetidine, have been investigated in normal and asthmatic subjects. Paper-3673618. The histamine H2 receptor ( H2r) belongs to the heptahelical receptor family; upon agonist binding, members of this family activate a G protein and the downstream effector adenylyl cyclase. Paper-9070038. A cyclooxygenase inhibitor or a thromboxane A2-prostaglandin H2 receptor antagonist partially but significantly reduced the effect of the factor.(ABSTRACT TRUNCATED AT 250 WORDS) Paper-404830. H2r desensitization was not affected by protein kinases A and C (PKA and PKC) inhibitors but was remarkably reduced by Zn(2+), an inhibitor of G protein-coupled receptor kinases (GRKs). Paper-9070038. The chemoattractant activity of histamine itself is not influenced by H1 or H2 receptor antagonists, thus it is possible that an eosinophil has a third type of histamine receptor. Paper-2882143. This interference clearly implies that tiotidine biases the system to Galphas-coupled form of the H2 receptor and turns Galphas-protein less available to interact with beta2-adrenoreceptor. Paper-9779376. The effect of an i.v. bolus of the H2-receptor antagonist ranitidine 50, 100, 200 and 300 mg on serum levels of prolactin, TSH, GH, LH, FSH and cortisol was studied in 12 normal males. Paper-4199121. Thus H2 receptor antagonists probably caused abnormalities in T helper cells leading to lymphokine unresponsiveness and subsequently loss of cellular immunity to candidal antigen. Paper-6610435. The ratio of relative gene copy numbers between the SAR and NR groups were as follows: H1R, 0.85 (P = 0.52); H2R, 0.67 (P = 0.35); EGF, 1.02 (P = 0.93), and EGFR, 103.5 (P < 0.05). Paper-9899807. These effects of histamine were antagonized by cimetidine, an H2 receptor antagonist, but not by selective H1 and H3 receptor blockers, and were mimicked by an H2 receptor agonist. Paper-1538479. The effect of an H2-receptor antagonist on food-stimjlated acid secretion, serum gastrin, and gastric emptying in patients with duodenal ulcers. Comparison with an anticholinergic drug. Paper-2315922. CONCLUSION: These data suggest that H2R mRNA is localized in the epithelium and the submucosal glands and that increased H2R may be playing some role in patients with allergic rhinitis. Paper-1854170. Effect of omeprazole 10 mg on intragastric pH in three different CYP2C19 genotypes, compared with omeprazole 20 mg and lafutidine 20 mg, a new H2-receptor antagonist. Paper-10067851. The H2-receptor antagonist, ranitidine, but not the H1-receptor antagonist, diphenhydramine, prevented histamine-induced activation of PDE4 in a concentration-dependent manner. Paper-9898164. MMP-1 responses to histamine and HB-EGF were further tested by the use of H2 receptor antagonist, EGFR inhibitor and mitogen activator protein kinase ( MAPK) inhibitor. Paper-12488748. BACKGROUND: Proton pump inhibiting drugs strongly decrease gastric acid secretion and have proven more effective in the treatment of reflux oesophagitis than H2-receptor antagonists. Paper-1242133. After pretreatment with ranitidine, a specific histamine H2-receptor antagonist, the diastolic pressure rise no longer sufficed to maintain a constant systolic pressure during LBNP. Paper-6505254. We report that histamine, acting via H2-type histamine receptors ( H2R), suppresses NADPH oxidase-dependent formation of oxygen radicals induced by WKYMVM and fMLF but not that induced by PMA. Paper-9986599. This inhibition of chemotaxis could be abolished by pretreatment with metiamide, an H-2 receptor antagonist, and levamisole, but not by diphenylhydramine, an H-1 receptor antagonist. Paper-2849656. Expression of the H2R gene, histamine accumulation, and histidine decarboxylase activity were also demonstrated in normal human monocytes/ macrophages and peripheral lymphocytes. Paper-8204642. H2 receptor blockade alone was associated with significant decreases in MAP, possibly secondary to enhanced release of histamine via an antagonist effect on recently described H3 receptors. Paper-5957976. Tiotidine, a histamine H2 receptor inverse agonist that binds with high affinity to an inactive G-protein-coupled form of the receptor. Experimental support for the cubic ternary complex model. Paper-9779376. The displayed inverse agonism of H2 antagonists appears to be a mechanistic basis for the observed H2 antagonist- induced H2 receptor upregulation in transfected CHO cells. Paper-599001. The H2-receptor antagonist cimetidine inhibits the cytochrome P-450 system, does not interfere with the administration or function of NAC, and therefore affords additive protection. Paper-5539571. The biogenic amine histamine, acting via H2-type histamine receptors ( H2R) on monocytes, completely counteracted the monocyte-mediated suppression of IL-2-induced NK-cell proliferation. Paper-6923353. The H2-receptor antagonist cimetidine has been reported to decrease the hepatic clearance of numerous drugs by inhibiting cytochrome P-450 metabolism, decreasing liver blood flow or both. Paper-6359689. Effects of two histamine H2-receptor blocking drugs on basal levels of gonadotrophins, prolactin, testosterone and oestradiol-17 beta during treatment of duodenal ulcer in male patients. Paper-3893058. Proton pump inhibitors are more effective for healing and symptom relief than histamine H2-receptor antagonists; their efficacy is proportional to their ability to reduce intragastric acidity. Paper-11223301. We report our experience with a new approach in treating severe stress-induced hemorrhagic gastritis after ineffective primary treatment with H2-receptor antagonists, pirenzepine and somatostatin. Paper-7309983. As shown previously, native or recombinant (r) human platelet factor 4 ( PF4) alleviates the suppression induced by Con A or dimaprit, a histamine type 2 receptor ( H2-R) agonist, in a murine system. Paper-727235. Treatments offered have included prokinetic drugs, anticholinergics, antacids, H2-receptor antagonists, selective muscarinic M1-receptor blockers, sucralfate, bismuth, antibiotics, and even surgery. Paper-6909336. In the present study, we examined the effects of human basic fibroblast growth factor ( bFGF) mutein CS23 (TGP-580) and histamine H2-receptor antagonists (H2-RAs) on ulcer relapse in this model. Paper-1065652. H2 receptor stimulation seems to be responsible for the reduction in histamine release observed, since it can be antagonized by cimetidine, but not by alpha 1, alpha 2 and H1 blockers. Paper-6497462. A new model for the agonistic binding site on the histamine H2-receptor: the catalytic triad in serine proteases as a model for the binding site of histamine H2-receptor agonists. Paper-8210162. These results indicate that not only the H2 receptor/cAMP/cAMP-dependent protein kinase pathway but also the H3 receptor/ GABA release pathway can attenuate NMDA-induced neurotoxicity. Paper-11337563. Real-time RT-PCR results revealed significantly decreased (p<0.001) H1R and H4R mRNA levels in tumours compared to normal colonic mucosa, without any significant change in H2R mRNA expression. Paper-12774371. The efficacy of gastric acid suppressive drugs, such as histamine H2-receptor antagonists and H+K+ ATPase inhibitors, in the management of peptic ulcer diseases has been well established. Paper-7972592. Interactions with the hepatic cytochrome P-450 microsomal enzyme system, as evidenced by statistically significant changes in pharmacokinetic parameters, have been described with some H2-receptor antagonists. Paper-7024944. OBJECTIVES: To determine the impact of OTC availability of H2-receptor antagonists on medication prescribing patterns and utilization of physician services among a population of chronic users of those agents. Paper-1806650. We recommend that H2 receptor blockade be included with other drugs in the treatment of anaphylactoid reactions following protamine, and possibly after anaphylactoid reactions associated with other substances. Paper-6385943. Plasma prolactin, sex steroids and gastrin in human volunteers treated for 2 weeks with therapeutic doses of cimetidine or the new histamine H2-receptor antagonist ramixotidine (CM 57755A). Paper-5813287. Drugs under investigation for the treatment of allergic rhinitis include histamine H2-receptor antagonists, nonsteroidal anti-inflammatory agents, anticholinergic agents, and beta-adrenergic receptor agonists. Paper-6227042. OBJECTIVE: Under the Pharmaceutical Benefits Scheme, the use of H2-receptor antagonists ( H2A) in the treatment of dyspepsia and heartburn is only subsidised when there is a proven diagnosis of ulcer. Paper-6954926. Intrinsic factor (IF) secretion in healthy male subjects was studied in response to pentagastrin stimulation with and without cimetidine, and to impromidine, a histamine H2 receptor agonist. Paper-3673606. On U937 cells, using a monoclonal antibody reacting with the 80 kd chain of the human IL-6 receptor, and H2-receptor mediated inhibition of IL-6 receptor expression was found by FACS analysis. Paper-7198223. Our findings suggest that amthamine-induced H2r internalization is crucial for H2r resensitization, processes independent of H2r de novo synthesis but dependent on PP2A-mediated dephosphorylation. Paper-12949959. In anaphylaxis histamine H1-receptor stimulation can mediate vascular permeability, smooth muscle contraction, and tachycardia, whereas H2-receptor stimulation can mediate mucus secretion. Paper-6653978. Proton pump inhibitors and H2 receptor antagonists, which are commonly used to treat peptic ulcer and gastroesophageal reflux diseases, are associated with a low incidence of adverse reactions. Paper-12127528. In this second part, two particular three-dimensional models of G-protein- coupled receptors previously reported in the literature are compared in relation to agonist binding at the histamine H2 receptor. Paper-924229. Concentrations of histamine that consistently resulted in inhibition of eosinophil movement stimulated an increase in cyclic AMP that was prevented by blocking the H2-receptor but not the H1-receptor. Paper-2882143. First experiences in man indicate, that even in catecholamine-insensitive congestive cardiomyopathy a considerable improvement of myocardial function can be attained by the H2-receptor agonist impromidine. Paper-4828474. BACKGROUND: Pilot studies have shown that histamine H2 receptor antagonists augment the natural immunity against cancer in colorectal and gastric cancer by enhancing lymphocytic infiltration in the tumors. Paper-11514792. The histamine H2-receptor antagonist cimetidine, which has recently been introduced for the treatment of gastric and duodenal ulcers and haemorrhage, respectively, stimulates prolactin ( PRL) secretion. Paper-3169262. The effects of the histamine H2-receptor antagonists, ranitidine and cimetidine on prolactin ( PRL), thyroid stimulating hormone (TSH), and growth hormone ( GH) were studied in six normal males. Paper-3943129. We conclude that gastric dysmotility is commonly detected in patients with CF and that H2 receptor blockers are more effective than prokinetics in improving dyspeptic symptoms and gastric emptying and distention. Paper-531184. Exposure of human platelets to U46619, a thromboxane (Tx) A2 mimetic, desensitizes the TxA2/ prostaglandin ( PG) H2 receptor and sensitizes adenylylcyclase to stimuli, such as PGI2 or PGD2. Paper-449447. Recent advances in molecular biological techniques have seen the cloning of the H2-receptor gene from canine parietal cells, and the structural identification and cloning of the H1- and H3-receptors should soon follow. Paper-7524979. We assessed the effects of ranitidine and cimetidine ( histamine H2-receptor antagonists) on the serum concentrations of parathyroid hormone ( PTH) in 22 patients with end-stage chronic renal failure. Paper-4853290. In conclusion, it appears that the hemodynamic changes are only partially mediated through histamine action, and the normal response to protamine may be modified, but not abolished, by H1 and H2 receptor blockade. Paper-6183753. However, hH2R poorly coupled to insect Gq-proteins as assessed by the lack of enhancement of histamine- stimulated steady-state GTP hydrolysis by regulators of G protein signaling ( RGS proteins). Paper-9376151. This, together with the action of cimetidine on PRL secretion (with or without L-dopa), suggests a possible antidopaminergic effect of H2-receptor blockade at the level of the central nervous system. Paper-4662427. We have previously reported that flushing associated with a gastric carcinoid tumor can be provoked by pentagastrin and inhibited by either somatostatin or combined histamine H1- and H2-receptor blockade. Paper-4272203. The effects of histamine (HA) and of HA in combination with H1- and H2-receptor antagonists on basal and LRH-receptor antagonists on basal and LRH-stimulated LH and FSH secretion were investigated in 10 normal men. Paper-4786031. It is interesting that the activity of HMT runs in parallel with the expression of H2R over the time course of the skin changes in MRL/l mice, but the relationship between these two observations remains obscure. Paper-13774047. We used cimetidine, a specific H2-receptor antagonist, to study the possible interference of H2-receptor blockade on plasma GH release by L-dopa and on PRL inhibition by L-dopa in normal man. Paper-4662427. No significant differences were observed in allele and genotype frequencies, and haplotype frequencies of all the SNPs of FCER1B, HNMT, HRH1, and HRH2 among the three groups (p>0.05, respectively). Paper-11262317. Dibutyryl cAMP down-regulated ICAM-1 and B7.1 expression on monocytes stimulated by LPS, suggesting the mediation by the cyclic adenosine monophosphate-protein kinase A pathway of H2-receptor activation. Paper-9707588. Ulcer patients with particularly high gastrin values (whether basal or stimulated) were not more resistant to H2 receptor antagonist treatment or prone to develop ulcer recurrence after highly selective vagotomy. Paper-6505666. In accordance with these findings, the H2-receptor antagonist cimetidine ( CIM) has an inhibitory (following central administration) or stimulatory (following systemic administration) effect on PRL secretion. Paper-6578114. The fact that histamine could inhibit the IL-18- stimulated MLR implies that immunomodulation by histamine and selective H2-receptor agonists may have an important role in future immunosuppressive strategies. Paper-9558297. Functional exploration of these receptors was performed by monitoring the increase of intracellular calcium levels ( H1R), cyclic adenosine monophosphate formation ( H2R), F-actin polymerization, and IL-12p70 production. Paper-9404578. These findings provide evidence that immune thrombocytopenia can be caused by sensitivity to an H2 R antagonist and suggest that the SZ1 binding site on GPIX may be a common target for drug-induced antibodies. Paper-1580488. Although H2R with truncation of 51 amino acids at its carboxy-terminus did not internalize after agonist stimulation, it still activated ERK1/2, but the degree of this activation was less than that of the wild-type receptor. Paper-12956429. Of the four cardinal signs of asthma ( bronchospasm, edema, inflammation, and mucus secretion), histamine is capable of mediating the first two through its H1 receptor and mucus secretion through its H2 receptor. Paper-6653978. CONCLUSION: Histamine stimulation of the H2 receptor on AGS cells evoked MMP-1 secretion and gene up regulation that was dependent on transactivation of the EGFR and downstream activation of MAPK. Paper-12488748. In fact, findings are confirmed by analysis of cytokine regulation, since activation of the H2R/cAMP pathway promoted TGF-beta1- mediated IL-4 inhibition but was ineffective in suppressing IFN-gamma. Paper-9708739. A long list of other compounds may determine an increase in prolactin levels, including prokinetics, opiates, estrogens, anti-androgens, anti-hypertensive drugs, H2-receptor antagonists, anti-convulsivants and cholinomimetics. Paper-13462078. CONCLUSIONS: PPI was superior to H2-receptor antagonist for prevention of peptic ulcer, and cotreatment with AT1 receptor blocker or ACE inhibitor seemed to reduce peptic ulcer among patients taking low-dose aspirin. Paper-13614782. Taken together, our results indicate that histamine may be involved in maintaining hibernation by sustaining hippocampal activity, possibly through H1 and H2 receptor activity and decreased inhibition by H3 receptors. Paper-9972759. Cimetidine, an H2-receptor antagonist, has been shown to inhibit the oxidative metabolism of several drugs by interacting with the hepatic cytochrome P450 system, which is involved in phase-I oxidative drug metabolism. Paper-5466432. It shares structural similarities with the histamine H2-receptor blocker cimetidine, an imidazole cyanoguanidine derivative, which is a potent inhibitor of cytochrome P-450 and of theophylline metabolism. Paper-6532961. Contractile responses to compound 48/80, a mast cell degranulator, were compared in the absence or presence of a mast cell stabilizer, H 1 and H 2 receptor antagonists, cyclooxygenase, and lipoxygenase inhibitors. Paper-10901081. This study examines the functional interactions between the H2 receptor and the EGFR in the regulation of matrix metalloproteinase-1 ( MMP-1) secretion and gene expressions in cultured gastric epithelial cells. Paper-12488748. In Part II, drugs used in the management of peptic ulcer disease (antacids, H-2 receptor and proton pump antagonists), pancreatic enzymes, prokinetic agents, and drugs used with inflammatory bowel disease are described. Paper-7674366. Selective activation of H1 receptors by combined infusion of HA and the H2 receptor antagonist cimetidine stimulated PRL secretion (delta PRL, 193 +/- 40 vs. -20 +/- 17 microIU/ml; P less than 0.0005; n = 6). Paper-5160035. Mean delta PAO was significantly higher in the normal group (17.1 +/- 4.8 mEq/hr) than in the asthmatic group (7.0 +/- 5.3 mEq/hr) (p less than 0.005) indicating suppressed selective H2-receptor stimulation in the latter. Paper-5221075. Several H2-receptor antagonists, including cimetidine and to a lesser extent ranitidine, and the proton pump inhibitor, omeprazole, may reduce the hepatic degradation of drugs metabolized by the cytochrome P450 system. Paper-6633805. The role of gastric alcohol dehydrogenase in the first-pass metabolism of alcohol is reviewed in this article and the arguments for and against any potential interaction between alcohol and H2 receptor antagonists are also discussed. Paper-1171016. The effect of a single dose of 400 mg of the H2-receptor antagonist cimetidine on protein meal stimulated immunoreactive gastrin was assessed in ten patients with gastric ulcer and ten patients with duodenal ulcer. Paper-3337315. By using transfected CHO cells expressing different densities of wild-type H2 receptors or an uncoupled H2Leu124Ala receptor, the histamine H2 receptor was found to display considerable agonist-independent H2 receptor activity. Paper-599001. These include competitive antagonists that interact with stimulatory receptors (e.g. muscarinic M1-receptor antagonists and histamine H2-receptor antagonists) as well as non-competitive inhibitors of H+,K(+)-ATPase (e.g. omeprazole). Paper-7586174. The study indicates that H1-receptor stimulation induces a stimulatory effect of TRH on GH secretion in normal men and that H2-receptor stimulation possibly induces an inhibitory effect of TRH on GH secretion. Paper-4784579. 1. Roxatidine acetate, a new histamine H2-receptor antagonist, was administered in the evening (75 mg p.o.) to eight patients with renal insufficiency ( CLCR 8-17 ml min-1) for 12 days and plasma drug concentrations were measured. Paper-225734. With recent over-the-counter ( OTC) availability of the H2 receptor antagonists and the increasing use of these drugs in the general population, physicians need to be aware of this rare but potentially serious side effect of ranitidine. Paper-1458745. Moreover, MoDC responded to a H4R agonist (and also to a H2R agonist) with increased F-actin polymerization and migration in modified Boyden chamber assays, suggesting a chemotactic effect of histamine via the H2R and the H4R. Paper-10801253. These results indicate that maintenance therapy with half the dose of H2-receptor antagonist is not required by patients with PGI less than 66 ng/ml, whereas those with hyper-PGI may be good candidates for long-term maintenance therapy. Paper-6482452. The stimulatory or inhibitory effects of histamine on cytokine production were all antagonized by H2 receptor antagonists ranitidine and famotidine in a concentration-dependent manner, but not by H1 and H3 receptor antagonists. Paper-8387524. OBJECTIVE: The objective of this study was to examine whether H2R mRNA expression is increased in patients with allergic rhinitis compared with normal subjects and to determine the localization of H2R mRNA in the human nasal mucosa. Paper-1854170. RESULTS: The mean +/- SD of H2R/ beta-actin ratios were 0.12 +/- 0.16 for the scrapings of normal subjects and 0.35 +/- 0.20 for the scrapings of patients with allergic rhinitis; the difference was statistically significant (P <.01). Paper-1854170. The effects of selective H2-receptor agonists, 4-methylhistamine and dimaprit, on CD14 expression mimicked that of histamine indicating that histamine regulated CD14 expression through the stimulation of H2-receptors. Paper-9988439. In life-long oncogenicity studies of these H2-receptor antagonists, as well as with the H+,K+-ATPase inhibitor omeprazole, gastric enterochromaffin-like cell ( ECL cell) hyperplasia and carcinoids have been found. Paper-5980505. We report a high-throughput method for genotyping of single nucleotide polymorphisms ( SNPs) within the genes of histamine H2 receptor ( HRH2), serotonin receptor (HTR2A1 and HTR2A2), and beta(3) adrenergic receptor ( ADRB3). Paper-13557949. To investigate this we studied the effect of H2-receptor antagonist therapy on basal and meal- stimulated plasma gastrin concentrations in 9 patients with pentagastrin fast gastric achlorhydria associated with pernicious anaemia. Paper-7216659. Proton pump inhibitors (14.1%) were less likely to be stopped than H2-receptor antagonists (35.3%) overall, and they were less likely to be stopped because of perceived ineffectiveness (5.3%) than H2-receptor antagonists (23.8%). Paper-1604933. The increases in CRF release from the HNC induced by 10 nM of histamine were completely suppressed in the combined presence of pyrilamine (10 microM) and cimetidine (10 microM), an H1 and an H2 receptor antagonist, respectively. Paper-7086264. We studied whether the histamine H2 receptor antagonist, cimetidine, potentiates antiproliferative effects of recombinant alpha interferon ( IFN alpha) on in vitro clonal growth of certain normal and malignant hematopoietic cells. Paper-6475393. Histamine stimulated a dose-dependent increase in [Ca2+]c, which was reversed by removal of histamine and inhibited competitively by the H1-receptor antagonist pyrilamine, but not by the H2-receptor antagonist cimetidine. Paper-5485681. Many patients self-medicate with OTC medications such as antacids and low-dose histamine H2-receptor antagonists (H2RA) to relieve episodic or food-related symptoms of GERD, and may not seek medical advice unless symptoms persist or worsen. Paper-11462451. Promethazine (a histamine H1 receptor antagonist) inhibited [Ca2+]i increase during histamine stimulation, whereas cimetidine (a H2 receptor antagonist) and thioperamide (a H3 receptor antagonist) showed no inhibition. Paper-1318690. This study evaluates the event rates for all NSAID-induced GI complications in patients with rheumatoid arthritis, describes the time course of these events, and evaluates the role of prophylactic therapy with antacids and H2 receptor antagonists. Paper-597833. CONCLUSIONS: We have demonstrated that H1R, H2R and, to some extent, H4R, are expressed in the human gastrointestinal tract, while H3R is absent, and we found that HR expression was altered in patients with gastrointestinal diseases. Paper-11392854. We have compared the effects of cimetidine and SK&F 92994, a new more potent histamine H2 receptor antagonist, on serum prolactin, and also assessed the effect of the H2 receptor agonist impromidine on the response to cimetidine. Paper-3649278. A history of gastrointestinal complications attributed to cystic fibrosis and the use of histamine H2-receptor blockers, corticosteroids, or recombinant human DNase ( dornase alfa) were associated with a higher incidence of fibrosing colonopathy. Paper-969912. Stimulation of the H1 receptor by histamine (range 0.18 to 17.8 mumol/l) significantly increased prostaglandin E (PGE) production, while activation of the histamine H2 receptor increased intracellular cyclic adenosine-5'-monophosphate (AMP). Paper-5565081. Significant elevation of MS ADCC by cimetidine alone suggested that endogenous histamine production and H2 receptor binding could be mediating a suppressive effect on MS ADCC to oligodendrocytes. Paper-5776567. The effect of perioperative immunomodulation with the H2-receptor antagonist ranitidine on postoperative changes in soluble interleukin (IL) 2 receptor and soluble CD8 levels was assessed in 24 patients undergoing major elective abdominal surgery. Paper-154895. Agonist stimulation of H2R results in several cellular events including activation of adenylate cyclase and phospholipase C, desensitization of the receptor, activation of extracellular signal-regulated kinases ERK1/2, and receptor endocytosis. Paper-12956429. This effect appears to be H2 receptor- mediated as no change in receptor density was observed after H1 or H3 antagonist treatment or after incubation with the structural analogue of cimetidine, VUF 8299, which has no H2 antagonistic effects. Paper-599001. Receptor cotransfection with dominant-negative mutants for arrestin, dynamin, Eps15 (a component of the clathrin-mediated endocytosis machinery), or RNA interference against arrestin 3 abolished both H2r internalization and resensitization. Paper-12949959. Thus, a dual role of cimetidine, acting both as inhibitor and inducer of the cytochrome P-450 system, is proposed to account for the impaired oxidative metabolism of some drugs that occurs during coadministration with this H2-receptor antagonist. Paper-5439467. Failure to document a simultaneous reduction in inulin clearance is consistent with the hypothesis that H2-receptor antagonists do not exacerbate cyclosporine nephrotoxicity and lower GFR, but rather compete with creatinine for tubular secretion. Paper-6262551. These proteins activated the transcription of the reporter gene ligated downstream of the control region of the rat ATPase alpha or beta subunit gene but had no effect on the same reporter ligated downstream of the H2 receptor gene. Paper-1120764. Teprenone, but not H2-receptor blocker or sucralfate, suppresses corpus Helicobacter pylori colonization and gastritis in humans: teprenone inhibition of H. pylori-induced interleukin-8 in MKN28 gastric epithelial cell lines. Paper-10295138. In an observational cohort study, we screened 152 adult patients from a gastroenterological outpatient clinic with negative case histories for atopy or allergy, who were medicated with H2-receptor blockers or proton pump inhibitors for 3 months. Paper-10978148. In cultured human melanoma cells, histamine H1 ( mepyramine) and H2 receptor antagonists ( cimetidine, ranitidine, impromidine) increased tyrosinase activity, whereas H2 agonists ( dimaprit, nordimaprit) decreased activity. Paper-6981227. The histamine H2 receptor agonists dimaprit and 4-methylhistamine, but not the H1 receptor agonists 2-pyridylethylamine, aminoethylthiazole and 2-methylhistamine, modulated the IL-1 production in a similar manner to histamine. Paper-5814078. These results suggest that activation of the histamine H2 receptor downregulates the production of TNF-alpha, and that histamine may be an important regulator in pathological conditions in which TNF-alpha plays an important role. Paper-1046626. Potent antisecretory drugs, such as omeprazole, increase serum and antral gastrin concentrations, whereas histamine H2-receptor antagonists, such as cimetidine, ranitidine, famotidine and roxatidine, have little influence on gastrin. Paper-5868454. Because many patients will not achieve complete relief from OTC products, clinicians will be required to rethink treatment strategies for those who present with persistent reflux symptoms after a trial of low dose H2 receptor antagonists or other antisecretories. Paper-8854331. Used judiciously and in proper dosage, antihistaminic drugs are helpful in the control of allergic disorders, allergic rhinitis and urticaria in particular; newly developed H2-receptor inhibitors show therapeutic promise in the treatment of peptic ulceration. Paper-2474479. These findings suggest that the H1 receptor- mediated PRL-stimulating effect of HA occurs through an inhibition of the dopaminergic system, whereas the H2 receptor- mediated PRL-inhibiting effect of HA does not involve dopaminergic neurons. Paper-5160035. The results indicate that histamine-induced relaxation of human cranial arteries is partially mediated via an endothelial H1-receptor coupled to the production of nitric oxide and partially via a H2-receptor associated with the smooth muscle cells. Paper-1077360. The histamine-mediated decrease in TNF-alpha synthesis was not affected by indomethacin, nor by diphenhydramine, an H1 receptor antagonist, but was reversed by cimetidine or ranitidine, H2 receptor antagonists, in a dose-dependent manner. Paper-7126790. METHODS: Mastomys were orally administered an irreversible H2-receptor antagonist loxtidine for 0, 8, and 16 weeks, and ECL cell transformation was monitored by assessing gastrin levels, mucosal histamine content, and chromogranin immunoreactivity. Paper-744105. Although the H2 receptor was classically thought to couple to the adenylate cyclase pathway, recent work with the cloned receptor indicates that it can also activate the phosphoinositide signaling cascade through an independent G protein-dependent mechanism. Paper-1241195. Median 24 hour acidity decreased with all H2-receptor antagonists from 25.1 mmol/l on placebo to 10 mmol/l (-60.1%) during cimetidine, to 3.2 mmol/l (-87.25%) during ranitidine and to 2.5 mmol/l (-90.0%) during famotidine treatment (p less than 0.0005). Paper-5806414. Prostaglandin E2 release is facilitated principally by histamine H1 receptors as the H1 receptor antagonist pyrilamine attenuates prostaglandin E2 release whereas the H2 receptor antagonist cimetidine only slightly reduces release. Paper-6872072. After the combination of either phenylalanine or tryptophan with pentagastrin, the H2-receptor antagonist significantly inhibited gastric acid secretion, whereas somatostatin, atropine, and the prostaglandin E1 analogue were not effective. Paper-5789062. We compared the interaction of AH 22216 (a new histamine H2 receptor antagonist) and cimetidine on the receptor-cAMP systems sensitive to histamine and to Vasoactive Intestinal Peptide ( VIP) in the human gastric cancer cell line HGT-1. Paper-4479472. Histamine, betahistine and impromidine all induced rises in Rna in both normal individuals and those with rhinitis but histamine had the most potent effect; the H2-receptor effect on Rna was predominant over that of the H1-receptor. Paper-8088658. We therefore provoked 25 healthy human subjects with histamine after local pretreatment with the H1 receptor antagonist, chlorpheniramine maleate, the H2 receptor antagonist, ranitidine hydrochloride, and a combination of these two antihistamines. Paper-4137176. Since previous studies on the effect of histamine H2-receptor blockade on gastrin release are conflicting, we have studied the effect of histamine infusion (130 nmol/kg/hr) with simultaneous H1-receptor blockade on gastrin release in healthy male subjects. Paper-5254446. Advancing age, prior chronic disease, malnutrition, coma on admission, and use of H2-receptor antagonists or antacids may impair host defenses of the gastrointestinal tract and predispose to invasive infection, thereby aggravating the severity of existing MOSF. Paper-7589176. The results of the present study indicate that an activation of A kinase via H2 receptor stimulation may cause the phosphorylation of a 160 kD protein and that this phosphorylation is probably involved in the process leading to differentiation of HL-60 cells. Paper-7531723. BACKGROUND: Proton pump inhibitors are superior to H2-receptor antagonists in the prevention of relapse of oesophagitis, but few data directly compare the relative efficacies of lansoprazole and omeprazole in preventing oesophagitis relapse over a prolonged period. Paper-1685846. In the case of the brain the H1 receptor stimulation of adenylate cyclase can be differentiated from H2 receptor stimulation of the enzyme by the use of blocking agents and by the fact that the H1 receptor response is enhanced in the presence of adenosine. Paper-3642755. 2. The histamine-induced eosinophil shape change was completely abolished by thioperamide (10 microm), an H3/ H4 receptor antagonist, but was not inhibited by pyrilamine or cimetidine (10 microm), H1 and H2 receptor antagonists, respectively. Paper-10195114. Our in vivo studies show that the intracerebroventricular administration of the histamine-1 ( H1) receptor antagonist, mepyramine, but not the H2 receptor antagonist, ranitidine, can block the LH surge in ovariectomized estrogen-treated rats. Paper-1965384. ITF 282 resulted, also when administered together with H2-receptor antagonists, in the expected therapeutic efficacy, with the expected clinical tolerability and biological safety, without signs of possible interaction, negative or positive.(ABSTRACT TRUNCATED AT 250 WORDS) Paper-7588162. We present the case of two rheumatoid arthritis patients with a history of severe acute IR to infliximab who subsequently underwent successful infusion using a prophylactic treatment with a combination of H1 and H2 receptor blockers, hydrocortisone, and diphenhydramine. Paper-12155150. METHODS: In 131 consecutive patients treated with either omeprazole (n = 111) or histamine H2-receptor antagonists (n = 20), serum vitamin B12 and folate levels and complete blood counts were determined after acid secretion had been controlled for at least 6 months. Paper-1454883. Here we report that histamine enhances TH1-type responses by triggering the histamine receptor type 1 ( H1R), whereas both TH1- and TH2-type responses are negatively regulated by H2R through the activation of different biochemical intracellular signals. Paper-9072664. Interestingly, while MMP-2 mRNA levels increased in response to histamine H1 or H2 receptor activation, significantly larger increases were observed in cells co-treated with ICAT and histamine or the histamine receptor agonists, HTMT and dimaprit. Paper-13736143. Ebrotidine (N-[(E)-[[2-[[[2-[(diaminomethylene)amino]-4 -thiazoly]methyl]thio]ethyl]amino]methylene]-4-bromo-benzenesulfon amide, CAS 100981-43-9, FI-3542) is a new H2-receptor antagonist characterized by its high receptor affinity and gastroprotective effect. Paper-1096505. In these experimental models, specific inhibitors are required to block acid secretion; for example histamine H2-receptor antagonists will block histamine- induced secretion but will be inactive when secretion is evoked by gastrin or by cholinergic stimulation. Paper-6134941. This histamine effect on LOX-1 gene expression, via the histamine H2 receptor-mediated cAMP signal transduction pathway, was reduced after differentiation of the cells into macrophages, even though forskolin and Bt2-cAMP still enhanced the gene expression. Paper-9098462. This H2-receptor antagonist had no effect on the receptor-adenylate cyclase systems sensitive to PGE2, isoproterenol ( beta 2-receptor), VIP and on forskolin-induced activation of the Gs/catalytic units of the membrane-bound enzyme prepared from human fundic glands. Paper-6085634. Ebrotidine (N-[(E)-[[2-[[[2-[(diaminomethylene)amino]-4-thiazolyl]methyl] thio]ethyl]amino]methylene]-4-bromo-benzenesulfonamide, CAS 100981-43-9, FI-3542) is a new H2-receptor antagonist with a potent antisecretory activity and evidenced gastroprotection. Paper-1096101. Granulocyte release of the lysosomal enzyme beta-glucuronidase ( BG) occurred after incubation with complement-activated zymosan particles, and this release was inhibited by isoproterenol (ISO), histamine (HIS) acting via its H2 receptor, and prostaglandin E1 ( PGE1). Paper-3527796. Multiple linear regression selected advancing age, malnutrition, APACHE II score, shock and coma on admission, number of blood transfusions, use of H2 receptor antagonists or antacids, bacteraemia and intra-abdominal infection as independent factors related to the MOSF score. Paper-8157018. BACKGROUND: We studied the effects of a proton pump inhibitor (PPI) and an H2-receptor antagonist (H2-blocker) on angiogenesis during gastric ulcer healing, by examining stromal cell-derived factor ( SDF-1) and CXC chemokine receptor 4 ( CXCR4) expression in the gastric mucosa. Paper-11031791. The effects of histamine on both ICAM-1 expression and cytokine production were mimicked by the selective H2-receptor agonists 4-methylhistamine and dimaprit and were antagonized by the H2-receptor antagonist famotidine but not by H1- and H3-receptor antagonists. Paper-9558297. Advancing age, malnutrition, shock and coma on admission, transfusion requirement and use of H2 receptor antagonists or antacids may impair host defences of the gastrointestinal tract and enhance the vulnerability for invasive infection, thereby aggravating the severity of existing MOSF. Paper-8157018. Ebrotidine (N-[(E)-[[2-[[[2-[(diaminomethylene)amino]- 4-thiazolyl]methyl]thio]ethyl]amino]methylene]-4-bromo-benzenesulfonamid e, CAS 100981-43-9, FI-3542) is the first of a new generation of H2-receptor antagonists with both antisecretory and cytoprotective activities. Paper-1096512. The H1 receptor is involved not only in allergic inflammatory reactions but also in augmentation of helper T cell (Th)1 responses, whereas H2 receptor suppresses Th responses and participates in immune tolerance through interleukin-10 and transforming growth factor-beta. Paper-12015675. Differentiation of U937 and HPM cells with 12-O-tetradecanoylphorbol-13-acetate (TPA) enhanced the H1 receptor expression and rather suppressed the H2 receptor, resulting in up-regulation of the histamine-induced expression and secretion of TNF-alpha, modulated via TACE. Paper-8461198. In this study we investigated the inhibition profiles of CYP1A2 (substrate: caffeine) CYP2D6 (substrate: dextromethorphan), and CYP3A4/5 (substrate: dextrorphan) by cimetidine, ranitidine, and the novel H2-receptor antagonist ebrotidine in human liver microsomes. Paper-1818842. Dimaprit and 4-methyl histamine, H2 receptor agonists, simulated the effect of histamine whereas the H1 receptor agonist 2-(2-aminoethylthiazole) was ineffective, confirming that the effect of histamine on C2 production by monocytes is mediated by the H2 receptors. Paper-3649362. Examination of the H2-receptor antagonist structures for insight into the moieties accounting for E3 isozyme inhibition pointed to the side-chain polar groups as strongly influencing inhibition, with the cyanoguanidine side chain of cimetidine and tiotidine having the strongest influence. Paper-1125122. Histamine responses were sensitive to the H1 receptor antagonist triprolidine (10 microM) and the nonselective potassium channel blocker barium (1 mM) but were unaffected by the H2 receptor antagonist tiotidine (10 microM) and the H3 receptor antagonist, clobenpropit (5 microM). Paper-11368127. Histamine H2 receptor antagonists (H2-blockers), which are currently available only by prescription, are presented as a case study and were examined to determine how OTC availability of these agents would alter the patterns, effectiveness, and risks of self-treatment for acid-peptic disorders. Paper-6507129. Ebrotidine (N-[(E)-[[2-[[[2-[(diaminomethylene)amino]-4-thiazolyl] methyl]thio]ethyl]amino]methylene]-4-bromo-benzenesulfonamide, CAS 100981-43-9, FI-3542) is a new antiulcer drug which combines the properties of an H2-receptor antagonist with those of a cytoprotective agent. Paper-1096102. Pretreatment of guinea pigs with a combination of the histamine H1 receptor antagonist pyrilamine and the histamine H2 receptor antagonist cimetidine (both 10 mg/kg), partially abolished tryptase-induced microvascular leakage as well as attenuating the reaction to histamine. Paper-1255747. When used at the usual recommended dose, all four H2 receptor antagonists ( cimetidine, ranitidine, famotidine and nizatidine) are equally effective and are found to be generally very safe; interactions with other drugs metabolized through the cytochrome p450 notwithstanding. Paper-1227789. The ability of SFV to infect cells without H-2 antigens and then to effect viral antigenic expression in the cells' cytoplasm and on their surface with similar kinetics and in equivalent amounts as cells with H-2 antigens indicates that the H-2 receptor is not needed for SFV infection. Paper-3554522. Multiple linear regression selected advancing age, prior chronic conditions, malnutrition, injury severity score (ISS), coma on admission, use of H2-receptor antagonists or antacids, number of blood transfusions, and intraabdominal infection as independent factors related to the MOSF score. Paper-7589176. In this work we show that in vivo tumour proliferation in immunodeficient mice xenotransplanted with a human melanoma cell line is diminished by cimetidine, an H2 receptor antagonist, if combined with a tamoxifen derivate acting on cytochrome p450 molecules (DPPE). Paper-9334263. Because the H2-receptor antagonists elevate gastric pH, bind to and inhibit the hepatic cytochrome P-450 enzyme system, and undergo renal tubular secretion, competition with other drugs sharing these pathways has resulted in a number of drug interactions, most of which are not clinically significant. Paper-5466512. Neither its CCK-B receptor antagonistic moiety of Compound 1 ( Compound 2) nor its histamine H2 receptor antagonistic moiety of Compound 1 ( Compound 3) had any effect on [125I]PYY binding, suggesting that the entire structure of Compound 1 is essential for Y1 receptor blocking activity. Paper-1579442. H1 receptor stimulation of the coronary artery was performed with a selective intracoronary infusion of histamine (2 micrograms/min) in 21 patients with variant angina after blockade of the H2 receptor with cimetidine (25 mg/kg) and its effect on the coronary artery diameter was examined. Paper-6869741. The potential interaction of the H2-receptor antagonist famotidine ( CAS 76824-35-6) with calcium carbonate ( CAS 471-34-1) and magnesium hydroxide ( CAS 1309-42-8) during administration of the famotidine fixed dose combination (FDC) formulation was investigated. Paper-13547850. Proton pump inhibitors are considered the best choice for the management of grades II-IV oesophagitis and are more cost-effective than H2-receptor antagonists because of their fast healing of oesophagitis, early relief of symptoms, and prevention of recurrent oesophagitis and development of complications. Paper-906279. We also found that the cimetidine-mediated down-regulation of NCAM expression in HSG cells did not occur via blocking of the histamine receptor, even though H2R expression was observed on HSG cells, as two other H2R antagonists, famotidine and ranitidine, did not show similar effects. Paper-12449817. Doses of the H2-receptor antagonist ranitidine, the prostaglandin E1 analogue misoprostol, atropine, and somatostatin that produced approximately 50% inhibition of pentagastrin-stimulated acid secretion significantly inhibited phenylalanine- and tryptophan-stimulated acid secretion. Paper-5789062. The aims of the present study were to investigate the participation of GRK2 in the desensitization mechanism of the H2 receptor in U-937 cells by reducing GRK2 levels through antisense technology and to evaluate the differentiating capacity of cells expressing lower GRK2 level, stimulated by H2 agonists. Paper-9577867. The conclusion that histamine acts directly on T cells and does not require accessory cells to induce suppression is further confirmed by the demonstration that IL-2 production by the human T-cell leukemia line Jurkat was significantly suppressed by histamine in a H-2 receptor-restricted manner. Paper-5458143. The effects of the H3-agonist R-alpha-methylhistamine (R-alpha-MeHA) and the H3-antagonist thioperamide on the spontaneous and concanavalin A (ConA) induced histamine release from human mast cells were tested and compared with the effect of some H1- and H2-receptor active substances. Paper-7167447. In experiment 1, H2-receptor antagonists were discontinued for 48 hours; SMS 201-995, 1 microgram/kg, was given subcutaneously; gastrin and SMS levels in plasma were determined by radioimmunoassay; and gastric secretion was measured and titrated at 0, 1, 2, 3, 4, 5, 6, 8, 10, 12, 14, 16, and 18 hours. Paper-5241266. Histamine, selective histamine H1- and H2-receptor agonists, and chemical analogues of these compounds lacking activity at histamine receptors, were tested as inhibitors of phytohaemagglutinin-induced human lymphocyte proliferation and zymosan-induced release of lysosomal enzymes from human polymorphs. Paper-4239856. Cimetidine has no antidopaminergic activity or this hypothetic action is very slight; 2. serum PRL increase after the drug is probably ascribable to the H2-receptor blocking, 3. this effect is observable only with the bolus i.v. of cimetidine, but not during or after acute and chronic oral administration. Paper-3317476. The concept of H2-R interaction with other receptors such as muscarinic receptors (M3-R), mediating the action of acetylocholine released from local cholinergic nerves, and those mediating the action of gastrin ( CCK2-R) on parietal cells, has been confirmed both in vivo studies and in vitro isolated parietal cells. Paper-11523499. Only ranitidine was efficiently transported by hOAT2 (Km, 396 microM). rOct1 accepts all of the H2 receptor antagonists with a similar activity, whereas the transport activities of ranitidine and famotidine (Km, 61/56 microM) by r/ hOCT2 were markedly lower than that of cimetidine (Km, 69/73 microM). Paper-10971910. CONCLUSIONS: Infants with trisomy 21 and atrioventricular septal defect who undergo fundoplication are less likely to experience major complications of reflux early after cardiac surgery than those treated with a medical regimen of upright posture, thickened feedings, metoclopramide, and H2-receptor blockade. Paper-8302801. CONCLUSIONS: Intravenous administration of pantoprazole after endoscopic therapy for peptic ulcer bleeding reduces rates of ulcer rebleeding, surgical intervention and overall duration of hospital stay, but not mortality and blood transfusion requirements compared with placebo, H2 receptor antagonist or somatostatin. Paper-13720718. Itraconazole has an affinity for mammalian cytochrome P-450 enzymes as well as for fungal P-450-dependent enzyme, and thus has the potential for clinically important interactions (e.g., astemizole, terfenadine, rifampin, oral contraceptives, H2 receptor antagonists, warfarin, cyclosporine). Paper-1421242. Ebrotidine (N-[(E)-[[2-[[[2-[(diaminomethylene)amino]- 4-thiazolyl]methyl]thio]ethyl]amino]methylene]-4-bromo-benzenesulfonamid e, CAS 100981-43-9, FI-3542) is a new H2-receptor antagonist providing a new therapy for the prevention and healing of non-steroidal anti-inflammatory drugs-induced gastroduodenal lesions. Paper-1096509. To evaluate the acute effect of histamine H2-receptor blockade with cimetidine on PTH concentrations and its endogenous biological activity, we studied the effect of iv administration of cimetidine (50-mg bolus followed by 500 mg/60 min infusion) in normal subjects and patients with primary and secondary hyperparathyroidism. Paper-4804032. H2 receptor blockade with cimetidine did not affect these changes, while H1 receptor blockade with diphenhydramine significantly reduced the histamine-induced increase in coronary blood flow and the decrease in coronary vascular resistance (26 +/- 6%, p less than 0.005 and -18 +/- 5%, p less than 0.001, respectively). Paper-5581148. These include antagonists that interact with stimulatory receptors ( histamine H2-receptor antagonists, muscarinic receptor antagonists, and gastrin receptor antagonists), agonists that interact with inhibitory receptors ( somatostatin and prostaglandin E analogues), and irreversible inhibitors of the luminal enzyme, H+K(+)-ATPase. Paper-6602459. There is, however, a different mode of secretion for both substances: atropine, vagotomy, and H2 receptor antagonists inhibit both intrinsic factor and acid secretion, but secretin and the hydrogen-potassium ATPase antagonist omeprazole have no effect on intrinsic factor while substantially reducing acid secretion. Paper-7079065. Eleven single nucleotide polymorphisms ( SNPs) of the beta chain of the high-affinity IgE receptor ( FCER1B) and three histamine-related genes- histamine N-methyltransferase ( HNMT), histamine H1 receptor ( HRH1), histamine H2 receptor (HRH2)-were screened using the SNP-IT assay based on a single base extension method. Paper-11262317. The effects of short-term, 7-day, treatment with synthetic 15-leucine human gastrin I, pentagastrin or sulfated cholecystokinin-8 on the activity of histamine (HA)-stimulated adenylate cyclase in membranes isolated from guinea pig gastric mucosa and H2-receptor-mediated contractions of isolated ilea were evaluated. Paper-67107. The transport activities of the H2 receptor antagonists ( cimetidine, famotidine, and ranitidine) by rat and human basolateral organic anion and cation transporters [human organic anion transporter (hOAT) 1, hOAT2, r/ hOAT3, rat organic cation transporter (rOct) 1, and r/ hOCT2] were compared using their cDNA transfectants. Paper-10971910. The effect of histamine on NK cell responsiveness to IL-2 was mediated by H2-type histamine receptors, as judged by mimicry exerted by the specific H2 receptor agonist dimaprit, but not by an H2-receptor-inactive derivative of this compound, N-methyldimaprit, and blocking by the H2 receptor antagonist ranitidine. Paper-6842865. The effect of two different H2-receptor antagonists, nizatidine and cimetidine, on sperm counts and hypothalamic-pituitary-gonadal function as determined by responses to provocative gonadotropin releasing factor, GnRH, thyrotropin releasing factor, TRH, and clomiphene were compared to those of men receiving placebo medication. Paper-5466468. CONCLUSION: The data indicate that ML 3000 affects acid-secretory mechanisms downstream of cAMP mobilization induced by histamine H2 receptor activation, that it directly inhibits H,K-ATPase specific activity, and that baseline gastric epithelial cell IL-8 secretory inhibition may be mediated by ML 3000 inhibition of 5-lipoxygenase activity. Paper-10246973. During in vitro differentiation parallel culture incubations were performed by adding H1 receptor antagonist triprolidine, H2 receptor antagonist tiotidine, the tamoxifene derivate DPPE which blocks the intracellular binding of histamine, and an irreversible blocker of histidine decarboxylase, alpha-fluoromethyl histamine (alpha-FMH). Paper-8946848. This study shows that: (a) in hypergastrinaemia in pernicious anaemia subjects, meal stimulation leads to a marked and prolonged increase in plasma gastrin concentrations; (b) H2-receptor antagonists have no effect on plasma gastrin in the neutral stomach and this is consistent with their gastrin effect being entirely secondary to acid inhibition. Paper-7216659. Proton pump inhibitors (PPIs) are the drugs of choice for patients with peptic ulcer bleeding because the drugs are more effective than histamine H2-receptor antagonists for maintaining the target intragastric pH (6 or higher) and preventing the recurrence of peptic ulcer bleeding, although an impact on mortality has not been demonstrated. Paper-11103061. These studies suggest that: (1) human LES pressure increases in response to intravenous histamine phosphate through its action at an H2-receptor; (2) the H1-receptor has no apparent role in the human LES response to histamine; and (3) H2-antagonism with cimetidine has no effect on the human LES basal pressure or its response to gastrin stimulation. Paper-3061185. As a result, famotidine should be considered the H2-receptor antagonist of choice for critically ill patients who require gastric-acid suppression and at the same time are being treated with other drugs that depend on the cytochrome P-450 mixed-function oxidase system for their metabolism and/or on renal tubular mechanisms for their excretion. Paper-6436510. Thus, histamine-dependent inhibition of the eosinophil chemotactic response to other agents is mediated through the H2-receptor and is associated with an increase in the intracellular level of cyclic AMP whereas histamine dependent enhancement of eosinophil migration to other agents appears to be mediated through the H1-receptor. Paper-2882143. A hypothetical metabolic pathway for ebrotidine (N-[(E)-[[(2-[[[2-[(diaminomethylene]amino]-4-thiazolyl] methyl]thio]ethyl]amino]methylene-4-bromo-benzenesulfonamide, CAS 100981-43-9, FI-3542) has been proposed on the basis of previous data on the metabolism of other H2-receptor antagonists as well as on in vitro degradation assays of ebrotidine. Paper-1096104. The observed inhibition of basal PTH concentration by cimetidine induced histamine H2 receptor blockade (but not by H1 blockade) in normal human subjects suggests that endogenous histamine with H2 receptor activation stimulates even basal PTH secretion and may serve as a modulator of PTH secretion in normal man. Paper-3730720. These synonyms are used for gene HRH2 (histamine receptor H2): Histamine H2 receptor, H2R, Gastric receptor I. These accession numbers are used for gene HRH2: Q14464 (UNIPROT__AC). HRH2 is a homologue of HRH2 (histamine receptor H2) from Canis familiaris. HRH2 is a homologue of HRH2 (histamine receptor H2) from Bos taurus. HRH2 is a homologue of HRH2 (histamine receptor H2) from Gallus gallus. HRH2 is a homologue of HRH2 (histamine receptor H2) from Pan troglodytes. HRH2 is a homologue of Hrh2 (histamine receptor H2) from Mus musculus. HRH2 is a homologue of Hrh2 (histamine receptor H 2) from Rattus norvegicus. HRH2 is a homologue of hrh2 (histamine receptor H2) from Danio rerio. Important links ! iHOP - Information Hyperlinked over Proteins . Concept & Implementation by Robert Hoffmann. |