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Low levels of CB1 were also reported in osteoclasts. Paper-12697956.
Loss of cannabinoid receptor CB1 induces preterm birth. Paper-13020322.
Nucleotide sequence of a human cannabinoid receptor cDNA. Paper-6647163.
The cannabinoid CB1 receptor is expressed in pancreatic delta-cells. Paper-12850434.
Twenty point-mutation studies were used to construct a CBR functionality matrix. Paper-10028296.
Cannabinoids inhibit emesis through CB1 receptors in the brainstem of the ferret. Paper-9024638.
Modulation of paraoxon toxicity by the cannabinoid receptor agonist WIN 55,212-2. Paper-12244098.
Anti-inflammatory potential of CB1-mediated cAMP elevation in mast cells. Paper-11099800.
We have recently discovered the presence of an allosteric site on the CB1 receptor. Paper-11410111.
CB1 receptors are expressed mainly in the central and peripheral nervous system. Paper-9690673.
CB1 receptors were also present in macrophages and infiltrated T-lymphocytes. Paper-13134528.
The SAR studies to optimize the CB1 binding affinity led to the potent urea derivatives. Paper-12770085.
Estrogenic induction of cannabinoid CB1 receptor in human colon cancer cell lines. Paper-13042651.
OBJECTIVE: To test the hypothesis that the CNR1 gene is associated with nicotine dependence. Paper-12871681.
Cannabinoid receptor agonists inhibit Ca(2+) influx to synaptosomes from rat brain. Paper-11822861.
Molecular cloning of a human cannabinoid receptor which is also expressed in testis. Paper-43139.
Signal transduction of cannabinoid CB1 receptors in a smooth muscle cell line. Paper-8723867.
Anandamide, 2-AG, and the CBR agonist HU-210 potently inhibit CaCo-2 cell proliferation. Paper-9985357.
CB1 cannabinoid receptor antagonism: a new strategy for the treatment of liver fibrosis. Paper-12031935.
We have isolated two overlapping clones from a human lung cDNA library with CB1 cDNA inserts. Paper-171872.
Similarly, a rat somatostatinoma cell line, MSL-G2-Tu6, was found to express CB1 receptor. Paper-12850434.
This augmentation was blocked by the CB1 receptor antagonist SR141716A or the D2 antagonist sulpride. Paper-1067887.
We found that CB1R is associated with cholesterol- and sphyngolipid-enriched membrane domains (rafts). Paper-11459231.
An amino-terminal variant of the central cannabinoid receptor resulting from alternative splicing. Paper-171872.
Nonetheless, CB2 receptor activation may play a protective role during chronic liver diseases. Paper-13911787.
Design, synthesis and biological evaluation of piperazine analogues as CB1 cannabinoid receptor ligands. Paper-12770085.
Twenty-four hours after CLP, the CB2R-deficient mice had increased lung injury. Paper-13849164.
However, further studies are needed to elucidate the role of CNR1 and the cannabinoid system in migraine. Paper-13884022.
Germ cells including spermatozoa were positive for CB1 immunoreactivity. Paper-11763985.
OBJECTIVE: Blockade of the CB1 receptor is one of the promising strategies for the treatment of obesity. Paper-13061670.
Using the Semliki Forest virus (SFV) expression system, CB1 was expressed in baby hamster kidney (BHK) cells. Paper-12057437.
Helix 8 Leu in the CB1 cannabinoid receptor contributes to selective signal transduction mechanisms. Paper-13393917.
The cannabinoid receptor agonist, WIN 55,212-2, inhibits cool-specific lamina I medullary dorsal horn neurons. Paper-12305563.
RESULTS: 17beta-estradiol induced CB1 gene expression in all the human colon cancer cells studied. Paper-13042651.
Effect of cannabinoid receptor agonists on streptozotocin-induced hyperalgesia in diabetic neuropathy. Paper-13032402.
Here, through CB1, they inhibit sperm motility measured as the percentage of motile spermatozoa (SPZ). Paper-13365250.
Identification, characterization, and function of a novel oncogene: the peripheral cannabinoid receptor Cb2. Paper-9746087.
CB1 inverse agonists attenuated basal [(35)S]GTPgammaS binding and restored the capacity of DAMGO to stimulate. Paper-12788707.
SR 141716A failed to antagonize this activity in either cell line, confirming its specificity for CB1. Paper-592414.
RESULTS: Allele frequencies of the CNR1 G1359A polymorphism were within the range reported by previous studies. Paper-10096798.
The endocannabinoid noladin ether acts as a full agonist at human CB2 cannabinoid receptors. Paper-10738901.
Significant levels of anandamide were also found in the thalamus which expresses low levels of CB1 receptors. Paper-700750.
In mice, the polyphenols dose-dependently reverse acute hypothermia produced by a CB1 agonist. Paper-13852074.
These data do not suggest a major role of human adipose CNR1 in fat cell function or metabolic disease development. Paper-13171551.
On the other hand, acute morphine administration produced tolerance that lasted only 3 days and did not affect the CB1R. Paper-13671028.
At 1 week p.p., some spermatogonia and Leydig cells showed strong immunoreactivity of CB1. Paper-11763985.
MAIN OUTCOME MEASURES: CNR1 genotypes and anthropometric measures of body fat distribution were determined. Paper-13279338.
We report here the identification of a novel class of azetidinone CB1 antagonists by using virtual screening methods. Paper-12784016.
CONCLUSIONS: CB1 deficiency altering normal progesterone and estrogen levels induces preterm birth in mice. Paper-13020322.
E. coli membranes expressing CB2 also activated cognate G-proteins in an in vitro coupled assay. Paper-11220424.
In support of this conclusion, the CB1 antagonist SR141716A enhances capsaicin-evoked bronchospasm and cough. Paper-8586698.
Genetic variations at the endocannabinoid type 1 receptor gene ( CNR1) are associated with obesity phenotypes in men. Paper-13279338.
These data suggest an important role for CB1 receptors and BAD in the regulation of apoptosis in colorectal cancer cells. Paper-12509639.
This finding suggests that the homozygous genotype CNR1 1359A/A confers vulnerability to alcohol withdrawal delirium. Paper-9375887.
Cannabinoid receptor agonists have been demonstrated to inhibit medullary and spinal cord dorsal horn nociceptive neurons. Paper-12305563.
In this connection, interest has been focused on factors such as sex steroid hormones, which regulate CB1 receptor expression. Paper-13042651.
Our data indicate that the G1422A polymorphism in the CNR1 gene is associated with increased abdominal adiposity in obese men. Paper-12495822.
Inhibition of THC-induced effects on the central nervous system and heart rate by a novel CB1 receptor antagonist AVE1625. Paper-13538670.
Competitive binding studies indicated that DML20, DML21 and DML23 are selective ligands for cannabinoid CB1 receptors. Paper-10470057.
Question 1: CB1 receptor activation reduces emesis and gastric emptying but the latter is associated with nausea. Paper-12584935.
Lymphocytes have also a specific AEA transporter and a functional CB1 cannabinoid receptor, which were not modulated by LPS. Paper-8856240.
Distinct expression profiles of the peripheral cannabinoid receptor in lymphoid tissues depending on receptor activation status. Paper-10253861.
The arachidonamides of GABA and L-serine were inactive in both binding and functional assays at the CB1 receptor. Paper-328758.
In addition, CB1-R-lacking Chinese hamster ovary (CHO) cells underwent cell death after anandamide treatment. Paper-9764330.
BAY 38-7271: a novel highly selective and highly potent cannabinoid receptor agonist for the treatment of traumatic brain injury. Paper-10056203.
Expression of CB1 cannabinoid receptor in the anterior cingulate cortex in schizophrenia, bipolar disorder, and major depression. Paper-13349298.
CONCLUSIONS: This method allows precise measurement of the mRNA of CB2-r performed on cell numbers as low as 10(5) after sorting. Paper-1835916.
Further complexity arises from possible interactions between the anandamide-sensitive CB(1) receptor and GPR55. Paper-13911774.
Shortly after, Sanofi also reported the synthesis of the first selective CB(2) cannabinoid receptor antagonist, SR144528. Paper-11033730.
The actions of cannabimimetic agents via CB1 receptors in brain are mediated by GI/O to inhibit adenylate cyclase and Ca2+ channels. Paper-273792.
Immunocytochemical distribution of the cannabinoid CB1 receptor in the primate neocortex: a regional and laminar analysis. Paper-12375400.
Characterization of anandamide-stimulated cannabinoid receptor signaling in human ULTR myometrial smooth muscle cells. Paper-13958808.
Carbon tetrachloride-induced liver fibrosis was studied in mice invalidated for CB2 receptors. Paper-11005741.
The cannabinoid CB1 receptor antagonist, rimonabant, protects against acute myocardial infarction. Paper-14020998.
Novel 3,4-diarylpyrazolines 1 as potent CB1 receptor antagonists with lipophilicity lower than that of SLV319 are described. Paper-11086913.
In humans, the CB1 antagonist rimonabant increases the risk of depressed mood disorders and anxiety. Paper-13841889.
In contrast to 2-arachidonoylglycerol, anandamide, another endogenous cannabinoid receptor ligand, failed to induce the migration. Paper-9779907.
This study aimed to investigate the function of the cannabinoid receptor in the neuromuscular junction of the frog ( Rana pipiens). Paper-13190441.
Human sperm express cannabinoid receptor Cb1, the activation of which inhibits motility, acrosome reaction, and mitochondrial function. Paper-11139025.
2-Arachidonoylglycerol, an endogenous cannabinoid receptor ligand, induces accelerated production of chemokines in HL-60 cells. Paper-10451345.
Cannabinoid abuse has been shown to exacerbate liver fibrogenesis in patients with chronic hepatitis C infection involving CB1 receptor. Paper-13911787.
Conversely, chiral headgroup methylation in the 2-gem-dimethyl series led to chiral analogues possessing a wide range of CB1 affinities. Paper-8997733.
Cannabinoid CB2 receptor potentiates obesity-associated inflammation, insulin resistance and hepatic steatosis. Paper-13831263.
Our results emphasize the therapeutic efficacy of cannabinoid receptor agonists and their inhibitory effects on the formation of gliosis. Paper-13717925.
Treatment of human saphenous veins and atria with 2-AG stimulated basal NO release, which was antagonized by l-NAME and a CB1 antagonist. Paper-8645539.
Here, we evaluated the efficacy of cannabinoid receptor agonists, a new family of potential antitumoral compounds, at skin melanoma. Paper-12343965.
Stimulation of cannabinoid ( CB1) and prostanoid (EP2) receptors opens BKCa channels and relaxes ocular trabecular meshwork. Paper-11116221.
Long-term effect of CB1 blockade with rimonabant on cardiometabolic risk factors: two year results from the RIO-Europe Study. Paper-12883109.
In the hypothalamus, CB1 receptor and endocannabinoids are integrated components of the networks controlling appetite and food intake. Paper-10820350.
Cannabidiol inhibits human glioma cell migration through a cannabinoid receptor-independent mechanism. Paper-11211243.
Thermodynamic cycle calculations indicated that a direct interaction occurs between the C3 substituent of SR141716A and K3.28 in WT CB1. Paper-9577843.
Cannabinoid receptor CB2 localisation and agonist-mediated inhibition of capsaicin responses in human sensory neurons. Paper-12985045.
It is well known that agonists of the cannabinoid receptor are able to reduce hyperalgesia and allodynia that develop after nerve injury. Paper-11451034.
CB(2) knockout mice showed larger cerebral infarction and worse neurological function compared to wide type. Paper-13839220.
Immunofluorescence revealed that CB1 was densely located in glucagon-secreting alpha cells and less so in insulin-secreting beta cells. Paper-12720881.
In addition, loss of CB1 resulted in aberrant secretions of corticotrophin-releasing hormone and corticosterone during late gestation. Paper-13020322.
3. The same phenomenon was observed when COS-7 cells were cotransfected with CB1 cannabinoid receptors and either mu- or delta-opioid receptors. Paper-8455014.
Here we show that rats with biliary cirrhosis have low blood pressure, which is elevated by the CB1 receptor antagonist SR141716A. Paper-9008927.
THC modulates neuronal excitability by inhibiting synaptic transmission via presynaptic CB1-mediated mechanisms. Paper-11516049.
We demonstrated that the gene encoding the peripheral cannabinoid receptor (Cb2) is the potential target, suggesting that Cb2 is a proto-oncogene. Paper-9759673.
CONCLUSION: Variants and haplotypes in the CNR1 gene may alter the risk for nicotine dependence, and the associations are likely sex specific. Paper-12871681.
Cannabinoid receptor CB1 mRNA is highly expressed in the rat ciliary body: implications for the antiglaucoma properties of marihuana. Paper-1550243.
These data corroborate the possible therapeutic interest of CB(2) cannabinoid specific chemicals in the treatment of Alzheimer's disease. Paper-13788326.
Using fluorescence resonance energy transfer, we found that CB1-417 and Galpha(i1)beta(1)gamma(2) proteins were colocalized in the cells. Paper-12615869.
We conclude that airway epithelial cells are sensitive to both CB2R-dependent and independent effects mediated by THC. Paper-12931140.
Characterisation of the cannabinoid receptor system in synovial tissue and fluid in patients with osteoarthritis and rheumatoid arthritis. Paper-12855966.
This down-regulation of survivin by CB1 is mediated by a cyclic AMP-dependent protein kinase A signaling pathway. Paper-12887987.
These results suggest that the CB1 receptor could be a novel target of FTY720 and that sphingosine could be an endogenous CB11 antagonist. Paper-12129477.
Elevated endocannabinoid tone might be expected to result in compensatory down-regulation of CB1 receptors or dampened signal transduction. Paper-13382949.
CB1 is expressed centrally in the hypothalamus and nucleus accumbens and peripherally in adipocytes and skeletal muscle. Paper-13139169.
However, oleamide has direct agonist actions at CB(1) cannabinoid receptors and also activates the TRPV1 vanilloid receptor. Paper-13188969.
These data suggest that CB2R is a critical regulator of the immune response to sepsis and may be a novel therapeutic target. Paper-13849164.
Anandamide was shown to induce programmed cell death in mouse blastocysts, through a pathway independent of type-1 cannabinoid receptor. Paper-8461070.
Evidence for the involvement of cannabinoid CB1 receptors in the bimatoprost-induced contractions on the human isolated ciliary muscle. Paper-13353291.
RESULTS: Activation of human T cells caused an induction of CB1 mRNA expression in primary human T cells (8-fold) and Jurkat cells (29-fold). Paper-12767356.
The reported 3D models of the CB1 receptor allowed us to construct a new 3D QSAR model based on theoretical calculations and molecular docking studies. Paper-12610354.
Regulation of peripheral cannabinoid receptor CB2 phosphorylation by the inverse agonist SR 144528. Implications for receptor biological responses. Paper-1940883.
This review discusses clinical and preclinical evidence that supports the use of cannabinoid receptor agonists for the management of multiple sclerosis. Paper-12528577.
We explored its analogues to discover compounds with a high affinity for the CB(2) receptor and with good oral bioavailability. Paper-12575330.
Finally, trans-resveratrol and curcumin share common structural motifs with other known cannabinoid receptor ligands. Paper-13852074.
Human cannabinoid receptor 1: 5' exons, candidate regulatory regions, polymorphisms, haplotypes and association with polysubstance abuse. Paper-10624367.
The synthetic cannabinoid R(+)WIN 55,212-2 inhibits the interleukin-1 signaling pathway in human astrocytes in a cannabinoid receptor-independent manner. Paper-11479211.
MCD reduces also cytochrome c release from mitochondria of C6 cells, and this effect is CB1R-dependent and partly mediated by activation of p42/p44 MAPK. Paper-10782486.
Cannabinoid CB(1) receptors in the basal ganglia and motor response to activation or blockade of these receptors in parkin-null mice. Paper-11181501.
The introduction of two methyl groups at the 2-position of anandamide led to no change in affinity for CB1 but somewhat enhanced metabolic stability. Paper-8997733.
In addition to neuronal cells, CB1 receptors are expressed in T lymphocytes, in which they are involved in cannabinoid-induced T helper cell biasing. Paper-12753958.
Chronic ethanol increases the cannabinoid receptor agonist anandamide and its precursor N-arachidonoylphosphatidylethanolamine in SK-N-SH cells. Paper-1716824.
When we reversed the order of drug application AM-630 blocked the effects of the CB2R agonist JWH-133, but not the CB1R inverse agonist LY320135. Paper-13944701.
Replacement of the central heterocyclic pyrazole ring in rimonabant yielded imidazoles, triazoles, and thiazoles as selective CB1 receptor antagonists. Paper-12858244.
Cannabinoid (CB) receptors are present in human skin and anandamide, an endogenous CB receptor ligand, inhibits epidermal keratinocyte differentiation. Paper-12432133.
The involvement of the CB1 cannabinoid receptor in the behavioural and biochemical processes underlying drug addiction has also been investigated. Paper-11516021.
The human gene for CNR1 is mapped to chromosome 6q14-15, and linkage studies have produced evidence for a schizophrenia-susceptibility locus in this region. Paper-8553158.
We found that overexpressed CNR1 protein localized on the cell surface of HEK293T cells and increased the calcium-dependent cell aggregation potential. Paper-10209223.
CNR1 gene is associated with high neuroticism and low agreeableness and interacts with recent negative life events to predict current depressive symptoms. Paper-13841889.
Conclusion We suggest that CB1 receptors in the STG are not involved in the pathology of schizophrenia and the auditory hallucination symptom of this disease. Paper-12636113.
Age-dependent effects of the cannabinoid CB1 antagonist SR141716A on food intake, body weight change, and pruritus in rats. Paper-13934320.
Activation of CB1 in sympathetic nerve terminals in bone inhibits norepinephrine release, thus balancing the tonic sympathetic restrain of bone formation. Paper-12697956.
The lowest p-value of 0.11 was detected for the A-allele of the CNR1 SNP rs1049353 for which the transmission rate was 59% (95% confidence interval 47%...70%). Paper-13503288.
When the CB(1) receptor antagonist AM281 was coapplied with ACPA, it reversed the effect of ACPA on caffeine-evoked tension. Paper-13843702.
OBJECTIVE: To review the pharmacology, pharmacokinetics, clinical efficacy, and safety of rimonabant, a new selective cannabinoid receptor antagonist. Paper-10750569.
Our findings suggest that R-MA induces cell death in MCL via CB1-mediated up-regulation of the de novo ceramide synthesis pathway. Paper-13893344.
Concurrent stimulation of cannabinoid CB1 and dopamine D2 receptors enhances heterodimer formation: a mechanism for receptor cross-talk? Paper-11213933.
The cannabinoid receptor type 2 promotes cardiac myocyte and fibroblast survival and protects against ischemia/reperfusion-induced cardiomyopathy. Paper-13866301.
OBJECTIVES: We aimed to evaluate, at the population level, the frequency of a genetic polymorphism of CB1 and to study its correlation with body mass index. Paper-13259994.
We investigated, whether a specific CNR1 G1422A genotype is associated with anthropometric markers of obesity and fat distribution in adult obese individuals. Paper-12495822.
In summary, up-regulation of CB1 in T lymphocytes in response to CBs themselves may facilitate or enhance the various immunomodulatory effects related to CBs. Paper-12381789.
Increased expression of CB1 receptors by DRG neurons ipsilateral to tumor-bearing limbs may contribute to the anti-hyperalgesic effect of elevated AEA levels. Paper-13063087.
The cannabinoid CB1 receptor antagonist, rimonabant, as a promising pharmacotherapy for alcohol dependence: preclinical evidence. Paper-12528583.
The CB1 antagonist, SR141716A, was effective in reducing the THC elevated levels of free arachidonate in these cells in agreement with the antisense data. Paper-987167.
These results further support the proposed role of the CB1 receptor in controlling intraocular pressure, helping to explain the antiglaucoma properties of marijuana. Paper-8486385.
Our results support that the (AAT)n polymorphism nearby the CNR1 gene could be associated with predisposition to cocaine dependency. Paper-11772276.
Cannabinoid ( CB) receptors are expressed in the enteric nervous system (ENS) and CB(1) receptor activity slows down motility and delays gastric emptying. Paper-13940136.
Using a staged-approach, we examined the contribution of the endocannabinoid receptor 1 gene ( CNR1) on obesity and body mass index (BMI) in the European population. Paper-12832296.
CB1 receptors have also been found in organs involved in the regulation of metabolic homeostasis, such as liver, white adipose tissue, muscle and pancreas. Paper-12507547.
HPLC analysis of oil of wormwood revealed that only the fractions having mobility close to thujone displaced [3H]CP55940 from the CB1 cannabinoid receptor. Paper-1826615.
It is well known that the CB1 cannabinoid receptor is down-regulated in states of cannabinoid tolerance along with uncoupling from its second messenger systems. Paper-11473780.
In a previous paper, we reported that sulfonamide derivative 1 acted as a potent CB(2) receptor agonist (IC(50)=65 nM, EC(50)=19 nM, E(max)=90%). Paper-12575330.
Plasma membrane and lysosomal localization of CB1 cannabinoid receptor are dependent on lipid rafts and regulated by anandamide in human breast cancer cells. Paper-11459231.
Both plant-derived cannabinoids and the endogenous ligands have been shown to elicit hypotension and bradycardia via activation of peripherally located CB1 receptors. Paper-1715165.
Interestingly, the cannabinoid receptor CB1 was not identified in first trimester placenta despite having previously been shown to be present in placental tissues at term. Paper-10864222.
A beneficial aspect of a CB1 cannabinoid receptor antagonist: SR141716A is a potent inhibitor of macrophage infection by the intracellular pathogen Brucella suis. Paper-2152217.
Second, (-)-CBD analogues which are devoid of cannabinoid receptor affinity but which inhibit intestinal motility, suggest the existence of a non-CB(1), non-CB(2) receptor. Paper-11495616.
The regional uptake was consistent with the distribution of CB(1) receptors, with high radioactivity in striatum and cerebellum and low in thalamus and pons. Paper-12660177.
RESULTS: Intracerebroventricular (icv) administration of cannabinoid receptor agonists, WIN55,212-2, ACEA or methanandamide, generated a dose-dependent analgesia. Paper-13671028.
Molecular modeling studies showed that compound 30 interacts with the CB(2) receptor through a combination of hydrogen bond and aromatic/ hydrophobic interactions. Paper-10809330.
Consistent with a novel role for CB2R in sepsis, CB2R-agonist treatment in wild-type mice increased the mean survival time in response to CLP. Paper-13849164.
The CB2 cannabinoid agonist AM-1241 prolongs survival in a transgenic mouse model of amyotrophic lateral sclerosis when initiated at symptom onset. Paper-12479843.
After correcting for multiple testing, no association of the A- or G-allele of CNR1 polymorphism with a history of alcohol withdrawal-induced seizures was detected. Paper-10096798.
Cannabinoid receptor type 1 protects against age-related osteoporosis by regulating osteoblast and adipocyte differentiation in marrow stromal cells. Paper-13916814.
Two possible physiological roles of the endocannabinoids and the CB1 receptor are discussed: the regulation of gestation and the regulation of gastrointestinal motility. Paper-8460346.
AIMS/HYPOTHESIS: Cannabinoid type 1 receptor ( CB1R) antagonists such as rimonabant ( Rim) represent a novel approach to treat obesity and related metabolic disorders. Paper-13634490.
Recent evidence obtained in rat models of Parkinson's disease showed that the density of cannabinoid CB1 receptors and their endogenous ligands increase in basal ganglia. Paper-10714570.
(1) We examined A3 adenosine and CB1 cannabinoid receptor-coupled signaling pathways regulating Cl(-) current in a human nonpigmented ciliary epithelial (NPCE) cell line. Paper-9900657.
This mechanism allows for the local release of beta-endorphin, where CB(2) receptors are present, leading to anatomical specificity of opioid effects. Paper-10772288.
A considerable number of these CB1 antagonists are bioisosteres that are derived from rimonabant by the replacement of the pyrazole moiety with an alternative heterocycle. Paper-10651823.
Functionally, CB1 receptor agonists reduced elevated cyclic AMP levels and slightly reduced proliferation of glioma cells in vitro, but did not induce apoptosis. Paper-12080816.
This summary seeks to define the pharmacology of endocannabinoids and to focus on the structure-activity relationships (SAR) of anandamide for the CB1 cannabinoid receptor. Paper-8432326.
These findings fail to replicate the original report of an association between SNPs adjacent to an alternative CNR1 exon 3 transcription start site and polysubstance abuse. Paper-12041671.
CB1 receptor is expressed in the hypothalamus and the pituitary gland, and its activation is known to modulate all the endocrine hypothalamic-peripheral endocrine axes. Paper-10820350.
Taken together, these results provide mechanistic insight into beneficial effects provided by cannabinoid receptor CB2 modulation in neurodegenerative diseases, particularly AD. Paper-11451987.
Bioisosteric replacement of the pyrazole 3-carboxamide moiety of rimonabant. A novel series of oxadiazoles as CB1 cannabinoid receptor antagonists. Paper-13003214.
The CB1 receptor antagonist rimonabant promotes weight loss and has favourable effects on aspects of the metabolic syndrome, including the hyperglycaemia of type 2 diabetes. Paper-13024940.
Therefore, we conclude that synthetic cannabinoids increase the spontaneous firing activity of noradrenergic neurons in the rat locus coeruleus through cannabinoid CB1 receptors. Paper-11313513.
The cytoplasmic helix of cannabinoid receptor CB2, a conformational study by circular dichroism and ( 1)H NMR spectroscopy in aqueous and membrane-like environments. Paper-9315840.
These findings suggest that selective cannabinoid CB(1) receptor inverse agonists such as Imidazole 24b have potential for the treatment of obesity. Paper-12681653.
By high-resolution NMR on the receptor in DPC micelles, it was determined that purified CB2 forms 1:1 complexes with the ligands CP-55,940 and anandamide. Paper-11220424.
The distribution and density of cannabinoid receptor binding and messenger RNA expression in aged human brain were examined in several forebrain and basal ganglia structures. Paper-7914651.
Palmitoylethanolamide (PEA) has been shown to act in synergy with anandamide (arachidonoylethanolamide; AEA), an endogenous agonist of cannabinoid receptor type 1 (CB(1)). Paper-9037452.
Effects of a cannabinoid receptor (CB) 1 antagonist AM251 on behavioral sensitization to nicotine in a rat model of novelty-seeking behavior: correlation with hippocampal 5HT. Paper-13618336.
Anandamide ( arachidonylethanolamide), a brain cannabinoid receptor agonist, reduces sperm fertilizing capacity in sea urchins by inhibiting the acrosome reaction. Paper-8023623.
The 5-HT-induced current was inhibited by the following cannabinoid receptor agonists (at decreasing order of potency): 9-THC, WIN55,212-2, anandamide, JWH-015 and CP55940. Paper-9632129.
Interaction Between Two Independent CNR1 Variants Increases Risk for Cocaine Dependence in European Americans: A Replication Study in Family-Based Sample and Population-Based Sample. Paper-13521722.
Cb2, the gene encoding the peripheral cannabinoid receptor, is located in a common virus integration site and is overex-pressed in retrovirally induced murine myeloid leukemias. Paper-10345913.
The intragenic CNR1 polymorphism 1359(G/A) should be useful for association studies in neuro psychiatric disorders which may be related to anandamide metabolism disturbances. Paper-8346980.
A considerable regression of thyroid tumors generated by inoculation of ARO/ CB2 cells was observed in nude mice following local administration of JWH133. Paper-12692639.
Like URB597 plus anandamide, the synthetic CB1-receptor ligand WIN 55,212-2 (50-300mug/kg, intravenous) produced dose-related conditioned place aversions. Paper-12674526.
These results suggest that high glucose concentrations are associated with decreased expression, but preserved function of CB(1) receptors in nerve cells. Paper-13781891.
At 2 weeks p.p., CB1 immunoreactivity was largely found in the primary spermatocytes as well as spermatogonia, and Leydig cells showed a weak signal. Paper-11763985.
1. Experiments were designed to determine whether anandamide affects cytosolic Ca2+ concentrations in endothelial cells and, if so, whether CB1 cannabinoid receptors are involved. Paper-1872363.
2-arachidonoylglycerol, an endogenous cannabinoid receptor ligand, induces the migration of EoL-1 human eosinophilic leukemia cells and human peripheral blood eosinophils. Paper-10858379.
Previous studies from our laboratory indicated that selective cannabinoid CB(2) agonists were able to attenuate cerebral ischemia/ reperfusion (I/R) injury. Paper-13839220.
In the presence of both the CB1 antagonist AM251 (10(-6)m) and CP 55,940 (10(-5)m), the contractile response to carbachol reached 84+/-3% (n=6) of the original level. Paper-11116221.
These results suggest that cannabinoids modulate transmitter release in the end-plate of the frog neuromuscular junction by activating CB1 cannabinoid receptors in the nerve ending. Paper-13190441.
The angiotensin II-induced, paracrine activation of CB(1) receptors was visualized by detecting translocation of green fluorescent protein-tagged beta-arrestin2. Paper-13838399.
Additionally, CB2R-deficiency led to increased neutrophil recruitment, decreased neutrophil activation, and decreased p38 activity at the site of infection. Paper-13849164.
Human vascular endothelial cells were found to generate and release 2-arachidonoylglycerol, an endogenous cannabinoid receptor ligand, upon stimulation with thrombin or A23187. Paper-1353197.
Salvinorin A reduced fatty acid amide hydrolase activity in amygdala but had very weak affinity for cannabinoid CB(1) receptors. Paper-13887468.
Central antinociception induced by mu-opioid receptor agonist morphine, but not delta- or kappa-, is mediated by cannabinoid CB1 receptor. Paper-13967245.
CB1 stimulation leads to modulation of the release of some hypothalamic anorexigenic and orexigenic mediators, as well as of dopamine in the nucleus accumbens shell. Paper-10740115.
Recent evidence has proved that CB1 is also present in the peripheral organs, such as the adipose tissue and gastrointestinal system, key organs in the regulation of energy metabolism. Paper-10740115.
This review discusses the role of rimonabant, a cannabinoid receptor 1 blocker, which has undergone Phase III clinical testing, in the treatment of obesity and tobacco dependence. Paper-11405105.
Herein we describe the discovery of a novel class of oxadiazole derivatives from which potent and selective CB2 agonist leads were developed. Paper-12916838.
These studies suggest the hypothesis that genetic variation in CB1 receptor function influences the risk of depression in humans in response to stressful life events. Paper-13841889.
Recent studies show that paracrine activation of hepatic cannabinoid receptor 1 by hepatic stellate cell-derived endocannabinoids also contributes to the development of alcoholic fatty liver. Paper-13594003.
We determined whether CB1 receptor splice variants and messenger RNA (mRNA) levels in perirenal and subcutaneous adipose tissues are associated with obesity and metabolic syndrome (MetS). Paper-13617707.
Cysteine residues in the human cannabinoid receptor: only C257 and C264 are required for a functional receptor, and steric bulk at C386 impairs antagonist SR141716A binding. Paper-11260965.
This cannabinoid receptor is localized with high concentrations in different brain areas, including hippocampus and amygdala, which play an important role in the modulation of memory. Paper-10066845.
CB1 is found in the central nervous system and in a variety of other organs including heart, vascular endothelium, uterus, vas deferens, testis and small intestine. Paper-8579678.
Structural requirements for selective CB1 receptor antagonistic activity of 5-thienyl pyrazole derivatives included the structural similarity with potent, specific antagonist rimonabant 1. Paper-13720440.
Rimonabant ( CB1 cannabinoid receptor antagonist; SR141716A; 3 microM) significantly inhibited relaxation induced by oleamide (EC50=3.5+/-0.3 microM, Rmax=75.1+/-1.9%; n=8; P<0.05). Paper-11317892.
The absolute configuration (4S) of eutomer 24 was established by X-ray diffraction analysis and 24 showed a close molecular fit with rimonabant in a CB1 receptor-based model. Paper-11086913.
CB1 receptors are abundant in basal ganglia, hippocampus and cerebellum, and their functional activity can be mapped during behaviors using cerebral metabolism as the neuroimaging tool. Paper-10947569.
Cannabinoid CB(1) receptors are expressed in this brain reward circuit and modulate the dopamine-releasing effects of Delta(9)-THC and nicotine. Paper-10773205.
For this purpose, rats (n = 12) were treated with either intravenous saline (control) or CB1 receptor antagonist SR141716A (1 mg/kg) 30 min after permanent middle cerebral artery occlusion. Paper-12191258.
The cannabinoid CB1 receptor antagonist SR 141716A (0.1, 0.5 and 1 microg) induces penile erection when injected into the paraventricular nucleus of the hypothalamus of male rats. Paper-11394578.
In electron microscopy studies of perfused monkey prefrontal cortex, CB1 immunoreactivity was predominantly found in axon terminals that exclusively formed symmetric synapses. Paper-12375400.
In overweight patients (OW), the increased peripheral activity of the endocannabinoid system in visceral adipose tissue (VAT) may be mediated by cannabinoid type 1 ( CB1) receptor expression. Paper-13617707.
In rat small mesenteric artery the response does not involve CB(1) cannabinoid receptors but another pertussis toxin-sensitive, G protein-coupled receptor, as yet unidentified. Paper-13188969.
Furthermore, H(2)O(2)-induced myofibroblast activation was increased in CB2(-/-) fibroblasts but decreased in 1 microM JWH133-treated WT fibroblasts, compared with that in WT cells. Paper-13866301.
Pertussis toxin treatment of striatal neurons prevented the inhibition of cAMP accumulation by D2 receptors but unmasked a cannabinoid receptor-mediated stimulatory effect on cAMP accumulation. Paper-1067887.
CONCLUSION: Our data predict that the cannabinoid receptor system present in the synovium may be an important therapeutic target for the treatment of pain and inflammation associated with OA and RA. Paper-12855966.
A newly isolated T-cell line ( CB1) derived from a T-acute lymphoblastic leukaemia ( T-ALL) patient contained cells (40% of total) which did not express the CD45 phosphotyrosine phosphatase. Paper-119203.
In addition, these findings suggest that CB1 receptor antagonists such as rimonabant may offer a potential new approach to managing obesity and associated cardiometabolic risk factors. Paper-12527355.
Rimonabant (SR141716), a CB(1) receptor antagonist, blocks both the dopamine-releasing and discriminative and rewarding effects of Delta(9)-THC in animals. Paper-10773205.
Reduction of bone cancer pain by activation of spinal cannabinoid receptor 1 and its expression in the superficial dorsal horn of the spinal cord in a murine model of bone cancer pain. Paper-13854577.
Stereochemical differences in the ethanolamide group influence the affinity for both cannabinoid receptor subtypes and the signal transduction capabilities of the methanandamide derivatives. Paper-1640958.
CB1 receptor was found to be present in all layers of the membrane, with particularly strong expression in the amniotic epithelium and reticular cells and cells of the maternal decidua layer. Paper-10190977.
Virodhamine also enhanced arachidonic acid release, which was insensitive to cannabinoid receptor antagonism, but sensitive to the phospholipase A(2) inhibitor quinacrine, and to capsazepine. Paper-13773183.
Presynaptic terminals of cerebellar granule neurons are primary targets of cannabinoids, which act through type 1 Galpha(i/o)-coupled cannabinoid receptors ( CB1) to modulate glutamate release. Paper-11821740.
The discovery of endogenous cannabinoid receptor ligands, anandamide (N-arachidonylethanolamine) and 2-arachidonylglycerol made the notion of a central cannabinoid neuromodulatory system plausible. Paper-1908773.
The CB1 cannabinoid receptor and its endogenous ligands, the endocannabinoids, are involved in energy balance control, stimulating appetite and increasing body weight in wasting syndromes. Paper-12929575.
Furthermore, our study allows us to identify, in the CB1-mediated inhibition of astroglial-derived NO, a new potential target to blunt tau hyperphosphorylation and the consequent related tauopathy in AD. Paper-12159419.
Several series of urea, carbamate, amide, sulfonamide and oxalamide derivatives based on 1-benzhydrylpiperazine scaffold were synthesized and tested for CB1 receptor binding affinity. Paper-12770085.
CONCLUSIONS: Several relevant metabolic processes appear to independently benefit from peripheral blockade of CB1, while CNS-CB1 blockade alone predominantly affects food intake and body weight. Paper-13061670.
Treatment with the CB1 receptor antagonist SR141716A decreased the wound-healing response to acute liver injury and inhibited progression of fibrosis in three models of chronic liver injury. Paper-12031935.
A second area of drug development at present is that of CB1 receptor antagonists/inverse agonists, spearheaded by rimonabant, for the treatment of obesity and as an aid for smoking cessation. Paper-11154246.
We also show that MCD reduces dose-dependently AEA-induced apoptosis in C6 cells but not in human CHP100 neuroblastoma cells, which mirror the endocannabinoid system of C6 cells but are devoid of CB1R. Paper-10782486.
In the present study, single-unit recordings from the rat medullary dorsal horn were performed to examine the effect of a cannabinoid receptor agonists on cold-specific lamina I spinothalamic tract neurons. Paper-12305563.
Since the cannabinoid receptor CB2 regulates innate immunity, the aim of the present study was to investigate its role in obesity-induced inflammation, insulin resistance and fatty liver. Paper-13831263.
Of the 25 successfully genotyped CNR1 SNPs, 12 showed nominal evidence of association with childhood obesity, class I and II and/or class III adult obesity (1.16 < OR < 1.40, 0.00003 < P < 0.04). Paper-12832296.
The results show that the patients with Dukes stage C and D had a 2.9 times (p = 0.04) and patients that were lymph node positive had 2.8 times (p = 0.05) greater probability of nucleotide change in CNR1 gene. Paper-13778687.
Moreover, we detected the presence of mRNA for the cannabinoid CB(1) receptor on fast and slow skeletal muscle fibers, which was significantly higher in fast compared to slow muscle fiber expression. Paper-13843702.
High glucose was associated with impaired NGF-induced neurite outgrowth (P < 0.01; n = 185-218) and reduced expression of CB(1) receptor mRNA (P < 0.01; n = 6) on day 6 of culture. Paper-13781891.
In the present study, we have explored the motor effects of rimonabant, a selective antagonist of CB1 receptors, in a rat model of PD generated by an intracerebroventricular injection of 6-hydroxydopamine. Paper-11327709.
Particular emphasis will be placed on the endocannabinoids anandamide and 2-arachidonylglycerol and CB1 receptor-mediated mechanisms in the neurovascular unit during stroke pathogenesis. Paper-12591930.
Dysregulation of the ECS has been associated with the development of dyslipidaemia, glucose intolerance, and obesity, and CB1 receptor blockade may have a role in ameliorating these metabolic abnormalities. Paper-12507547.
In the current study, the effects of WIN 55,212-2 (WIN), a synthetic and potent cannabinoid receptor agonist, are investigated in hepatoma HepG2 cells and a possible signal transduction pathway is proposed. Paper-13524329.
These CB1 knockouts have provided new findings to clarify the interactions between cannabinoids and the other drugs of abuse such as opioids, psychostimulants, nicotine and ethanol. Paper-11516021.
MEASUREMENTS: Anthropometric parameters, blood pressure, serum glucose and lipid levels were measured with standard methods; genotyping for the CB1 1359G/A polymorphism was performed using multiplex PCR. Paper-13259994.
We investigated CB(1) receptor function in PC12 cells differentiated into a neuronal phenotype with nerve growth factor (NGF, 50 ng/ml) in 5.5 and 50 mM concentrations of glucose. Paper-13781891.
However the nearly identical concentration response for 2-AG to inhibit excitatory postsynaptic currents (EPSCs) and IPSCs indicates that this difference is not due to differential cannabinoid receptor sensitivity. Paper-13935267.
To test this possibility, we employed alanine scanning mutagenesis of CB1 EC2 and identified two distinct regions critical for ligand binding, G protein coupling activity, and receptor trafficking. Paper-14004932.
In this study, we verified receptor gene expression in rodent islets and cell lines and examined the distribution of CB1 receptor in mouse, rat, and human islets by confocal immunofluorescence (IF) microscopy. Paper-12850434.
Influence of intracerebroventricular or intraperitoneal administration of cannabinoid receptor agonist (WIN 55,212-2) and inverse agonist (AM 251) on the regulation of food intake and hypothalamic serotonin levels. Paper-13777480.
Our study shows that treatment with the cannabinoid receptor agonists HU210 and Delta(9)-tetrahydrocannabinol lowers the viability of translocation-positive rhabdomyosarcoma cells through the induction of apoptosis. Paper-13890068.
AIM: The aim of our study was the assessment of cannabinoid receptor expression on the B-lymphocytes in bone marrow trephine biopsy from leukaemic patients at diagnosis and after purine analogue treatment. Paper-12544970.
New trials are supposed to confirm the potential role of rimonabant (and other CB1 neutral antagonists or inverse agonists) in overweight/obese patients with type 2 diabetes and high risk cardiovascular disease. Paper-13658317.
GTPgammaS binding assays with the Sf9 cell membranes containing CB1-417 and the G protein trimer showed that the receptor could constitutively activate the Galpha(i1) protein in the absence of agonists. Paper-12615869.
The CB2 receptor, with incorporated N-terminal FLAG and C-terminal HIS6 epitope tags, was functionally expressed in baculovirus cells and purified using a single step of anti-FLAG M2 affinity chromatography. Paper-13262489.
The recently discovered endogenous agonist for the cannabinoid receptor, anandamide ( arachidonylethanolamide), can be formed enzymatically by the condensation of arachidonic acid with ethanolamine. Paper-328758.
Furthermore, anandamide and a CB1 agonist, arachidonylcyclopropylamide (ACPA), inhibited glucose-induced insulin secretion from mouse pancreatic islets. Paper-12669727.
Importantly, THC treatment resulted in CB1-mediated inhibition of both RAS-MAPK/ERK and PI3K-AKT survival signalling cascades; two key cell survival pathways frequently deregulated in colorectal tumours. Paper-12509639.
Anandamide was measured by LC/MS/MS and was found in human and rat hippocampus (and human parahippocampal cortex), striatum, and cerebellum, brain areas known to express high levels of CB1 cannabinoid receptors. Paper-700750.
One of the sites of the orexigenic action of ECs involves activation of cannabinoid-1 ( CB1) receptors in the lateral hypothalamus, from which neurons involved in mediating food reward project into the limbic system. Paper-13406253.
Anandamide is an endogenous ligand for cannabinoid receptor and its protein-mediated transport across cellular membranes has been demonstrated in cells derived from brain as well as in cells of the immune system. Paper-9940508.
Pharmacological blockade of CB1 receptors stimulated adipocyte differentiation, inhibited osteoblast differentiation, and increased cAMP and pCREB in osteoblast and adipocyte precursors. Paper-13916814.
In the central nervous system (CNS), cannabinoid type 1 ( CB1) receptors and their respective ligands, the endocannabinoids, have a significant role in the modulation of food intake and motivation to consume palatable food. Paper-12507547.
We studied four single-nucleotide polymorphisms ( SNPs) in the CNR1 gene for association with having one or more symptoms of cannabis dependence in 541 adolescent subjects who had all tried cannabis five or more times. Paper-12333498.
The deduced amino acid sequence encodes a protein of 472 residues which shares 97.3% identity with the rat cannabinoid receptor cloned recently [Matsuda, Lolait, Brownstein, Young & Bronner (1990) Nature (London) 346, 561-564]. Paper-43139.
In this population based association study, we tested the hypothesis that a microsatellite polymorphism in the promoter region of the CNR1 gene confers susceptibility to mood disorders and psychotic features. Paper-8940036.
Significantly higher levels of CB1 mRNA levels were found in the ciliary body (0.84+/-0.05% of beta2m) than in the iris, (0.34+/-0.04% of beta2m), retina (0.07+/-0.005% of beta2m) and choroid (0.06+/-0.005% of beta2m). Paper-1550243.
In the recent Rimonabant in Obesity (RIO)-Europe study, treatment with the first CB1 receptor antagonist, rimonabant, led to sustained, clinically meaningful weight loss and a reduction in waist circumference. Paper-12527355.
Cannabinoid type 1 ( CB1) receptors are widely distributed in the central nervous system and are present in the periaqueductal gray (PAG), a midbrain structure closely involved in responses related to aversive states. Paper-13551285.
Pretreatment with cannabinoid receptor antagonists, SR144528 and/or SR141716A, led to an attenuation of delta(9)-THC-mediated elevation in [Ca(2+)](i) in splenic T cells and HPB-ALL cells but not in Jurkat E6-1 cells. Paper-10250820.
In immunohistochemical experiments, although mu-opioid receptor 1 expression was reduced in the superficial dorsal horn ipsilateral to the site of implantation of sarcoma cells, CB1 expression was preserved. Paper-13854577.
To further evaluate the properties of CB receptors, we have designed and efficiently prepared a series of substituted pyrimidines based on chemical structure of Merck's taranabant, a cannabinoid CB1 receptor inverse agonist. Paper-13901445.
Anandamide dose dependently attenuated the TNF-alpha-induced ICAM-1 and VCAM-1 expression, NF-kappaB activation in HCAECs, and the adhesion of monocytes to HCAECs in a CB(1)- and CB(2)-dependent manner. Paper-13368993.
Possible underlying mechanisms include presynaptic CB1 receptor mediated inhibition of norepinephrine release from peripheral sympathetic nerve terminals, and/or direct vasodilation via activation of vascular cannabinoid receptors. Paper-1715165.
Nandrolone pre-exposure blocked THC- and food-induced conditioned place preference and increased the somatic manifestations of THC withdrawal precipitated by the CB1 cannabinoid antagonist rimonabant (SR141617A). Paper-12113377.
CONCLUSIONS: Cannabinoid CB1 receptors are functionally present in the human ileum and colon; their pharmacological activation apparently results in inhibition of excitatory cholinergic pathways subserving smooth muscle contraction. Paper-9573691.
Finally, by contrast with the observations in motor structures, the status of CB1 receptors remained unaltered in cognition-related regions, such as the cerebral cortex and the hippocampus, during the different phases of CREAE. Paper-12182151.
Furthermore, an exciting development in this field has been the discovery of CB1 receptors in many peripheral tissues, including key organs involved in carbohydrate and lipid metabolism such as the adipose tissue and liver. Paper-13316934.
Finally, transfection experiments with human U937 immune cells, and the use of primary cells expressing CB1R or CB2R, ruled out that the cellular environment could account per se for the different modulation of CB receptor subtypes by MCD. Paper-12252211.
Previous autoradiographic studies in rats using [3H]CP55,940 have demonstrated the cannabinoid receptor to be located on the axon terminals of striatal efferent neurons projecting to the globus pallidus and substantia nigra. Paper-7849264.
To elucidate the mechanism of this response, we investigated the effect of the selective cannabinoid type 1 receptor ( CB1) cannabinoid agonist arachidonyl-2-chloroethylamide (ACEA) on [(3)H]GABA release in slices of the rat globus pallidus. Paper-13626663.
Finally, in rat pancreatic acinar cells, CB1- and CB2-receptors, expressed both in basal conditions and after CK-induced pancreatitis but inactive on amylase secretion, have an unknown role both in physiological and pathological conditions. Paper-13611692.
OBJECTIVES: The endocannabinoid system is an endogenous lipid signalling network comprising arachidonic-acid-derived ligands, cannabinoid ( CB) receptors, transporters and endocannabinoid degrading enzymes. Paper-13882106.
In patients with PD, the presence of two long alleles, with more than 16 repeated AAT trinucleotides in the CNR1 gene, was associated with a reduced prevalence of depression (Fisher's exact test: P=0.003). Paper-11022607.
We have recently shown that cannabinoids induce growth inhibition and apoptosis in mantle cell lymphoma (MCL), a malignant B-cell lymphoma that expresses high levels of cannabinoid receptor types 1 and 2 (CB(1) and CB(2)). Paper-12283943.
Peripheral treatment with CB1 antagonist ( Rimonabant) also reduced food intake and body weight but, in addition, independently triggered lipid mobilization pathways in white adipose tissue and cellular glucose uptake. Paper-13061670.
Transient ischemia significantly increased leukocyte/endothelial interactions, adhesion molecules expression and blood-brain barrier disruption which were all attenuated by pre-treatment with a CB(2) agonist. Paper-13839220.
CB1 was mainly expressed in the central nervous system and, to a lower extent, in several peripheral tissues such as adrenal gland, heart, lung, prostate, uterus, ovary, testis, bone marrow, thymus and tonsils. Paper-377011.
Although CB(1) receptors are more abundant in the central nervous system, rimonabant has many effects in the periphery, most of which are related to prejunctional modulation of transmitter release from autonomic nerves. Paper-12996495.
CONTEXT: Endocannabinoids control food intake via both central and peripheral mechanisms, and cannabinoid type-1 receptor ( CB1) modulates lipogenesis in primary adipocyte cell cultures and in animal models of obesity. Paper-13259994.
Furthermore, our finding of reduced mRNA expression along with a possible association between polymorphism genotypes of the CNR1 gene and EP, suggests a possible genetic predisposition to EP that warrants replication in a larger sample pool. Paper-13510964.
The high density of CB1 cannabinoid receptors within the basal ganglia suggests a potential role for endocannabinoids in the control of voluntary movement and in basal ganglia-related movement disorders such as Parkinson's disease. Paper-8382678.
With the input of CNR1 exons and 3' and 5' regions sequencing and HapMap database, we selected and genotyped 26 tagging single-nucleotide polymorphisms ( SNPs) in 1932 obese cases and 1173 non-obese controls of French European origin. Paper-12832296.
Application of the CB(1) agonist HU210 (1 microM) inhibited capsaicin-induced calcium transients to a similar degree in cells cultured in high glucose (40%) versus normal (43%) (P < 0.05; n = 33-50). Paper-13781891.
Other possible uses for CB1 receptor agonists include the suppression of muscle spasm/spasticity associated with multiple sclerosis or spinal cord injury, the relief of chronic pain and the management of glaucoma and bronchial asthma. Paper-2049131.
Radioimmunoassay analysis of circulating levels of ovarian steroid hormones revealed that premature birth resulting from CB1 inactivation is correlated with altered progesterone/ estrogen ratios prior to parturition. Paper-13020322.
INTRODUCTION: Great interest has been shown by the medical community and the public in the cannabinoid CB(1) receptor antagonists, such as rimonabant, for treatment of obesity, metabolic syndrome, and possibly drug addiction. Paper-13836534.
PDP CB1 was shown to mimic the biological properties of 13B8.2 mAb in two independent cellular assays, demonstrating inhibitory activities in the micromolar range on antigen presentation and human immunodeficiency virus promoter activation. Paper-9093040.
Clinical reports (RIO trials) have shown that chronic administration of a CB- cannabinoid receptor antagonist ( rimonabant) provides improvements of disturbed metabolic parameters observed in overweight and obese patients with type 2 diabetes. Paper-13186820.
Our results show that a CB(2) agonist ( JWH-015) is capable of inducing the removal of native beta-amyloid removal from human frozen tissue sections as well as of synthetic pathogenic peptide by a human macrophage cell line (THP-1). Paper-13788326.
Considering the antiobesity effect of SR141716, these results open new avenues to understand the mechanism by which the molecule may prevent weight gain through functional interaction between CB1 and other receptors involved in the control of appetite. Paper-9782979.
Marrow stromal cells from CB1(-/-) mice had an enhanced capacity for adipocyte differentiation, a reduced capacity for osteoblast differentiation, and increased expression of phosphorylated CREB (pCREB) and PPARgamma. Paper-13916814.
The cannabinoid 1 receptor ( CB1R) is highly expressed in the dorsolateral prefrontal cortex, is contained in the axon terminals of a subpopulation of perisomatic-targeting GABA neurons, and, when activated, suppresses the release of GABA. Paper-12871677.
The enhanced PGE(2) production caused by CP55,940 was abrogated by cotreatment with either SR141716A or NS398, illustrating that the cannabinoid action on prostaglandin production in fetal membranes is mediated by CB1 agonism and COX-2. Paper-12729740.
Further, cannabinoid receptor density was increased in the prelimbic prefrontal cortex, ventral tegmental area, and select regions of the hippocampus in adolescent male rats pretreated with nicotine compared to vehicle-treated controls. Paper-13650959.
C-terminal histidine (His)-tagged CB1 gave a Bmax higher than most other systems previously reported in the literature, and was selected for subsequent metal affinity chromatography purification and mass spectroscopic (MS) analysis. Paper-11239846.
Indeed, the presence of cannabinoid CB1 receptor markers, endocannabinoids such as anandamide and 2-arachidonoylglycerol (2-AG), their metabolic enzymes, and an endocannabinoid reuptake system have been confirmed in the gastrointestinal tract (GIT). Paper-11378400.
Both processes have been proposed as mediators of tolerance because of observations that chronic Delta(9)-tetrahydrocannabinol ( THC) treatment causes both region-specific decreases in CB(1) receptors and G-protein coupling in the brain. Paper-12674515.
Here, we test the hypothesis that CB(2) receptor activation stimulates release from keratinocytes of the endogenous opioid beta-endorphin, which then acts at opioid receptors on primary afferent neurons to inhibit nociception. Paper-10772288.
Such active substances and receptors include acetylcholine ( ACh) and the nicotinic ACh receptor (nAChR) for nicotine, anandamide and CB1 for delta 9-THC, and endomorphins (1 and 2) and the mu (OP3) opioid receptor for morphine, respectively. Paper-1800091.
Although most of these data are collected from animal studies, a role for cannabinoid receptors in the developing human brain has been suggested, based on the detection of "atypically" distributed CB1 receptors in several neural pathways of the fetal brain. Paper-10324927.
Anandamide specifically binds to membranes from cells transiently (COS) or stably ( Chinese hamster ovary) transfected with an expression plasmid carrying the cannabinoid receptor DNA but not to membranes from control nontransfected cells. Paper-7865435.
We therefore specifically assessed and compared the respective potential relevance of central nervous system (CNS) versus peripheral CB1 receptors in the regulation of energy homeostasis and lipid and glucose metabolism in diet-induced obese (DIO) rats. Paper-13061670.
It is conceivable that the endogenous ligand for the cannabinoid receptor, that is, 2-arachidonoylglycerol, affects natural killer cell functions such as migration, thereby contributing to the host-defense mechanism against infectious viruses and tumor cells. Paper-11280838.
Together, these findings suggest that prolonged activation of dopamine receptors could alter endocannabinoid levels and support the proposed involvement of the CB(1) receptor in amphetamine sensitization. Paper-12695533.
We also demonstrated significant increase in the induction of apoptosis in ARO/IL12 and ARO/ CB2 cells following incubation with 15 nM paclitaxel, indicating that tumor cells were sensitized to chemotherapy. Paper-12692639.
In view of the psychomotor slowing induced by cannabinoid agonists, we investigated the therapeutic potential of the cannabinoid receptor antagonist SR141716A in an early and advanced stage of 1-methyl-4-phenyl-1,2,5,6-tetrahydropyridine-induced parkinsonism. Paper-8861462.
We examined the association of 4 SNPs (rs6928499, rs806379, rs1535255, rs2023239) in the distal region of intron 2 of CNR1 both with individual substance dependence diagnoses (i.e., alcohol, cocaine, and opioids), as well as with polysubstance dependence. Paper-12041671.
Using electron microscopy, we demonstrated the postsynaptic localization of neuronal NOS at symmetrical synapses formed by CB1R-positive axon terminals on pyramidal cell bodies, whereas NO-sGC was found in the presynaptic terminals. Paper-12484669.
Moreover, many of these ligands exert prominent CB receptor-independent pharmacological effects, such as activation of the G-protein-coupled receptor GPR55, peroxisome proliferator-activated receptor gamma and the transient receptor potential vanilloid channels. Paper-13882106.
CONCLUSION: The abundant distribution of cannabinoid receptors on skin nerve fibers and mast cells provides implications for an anti-inflammatory, anti-nociceptive action of cannabinoid receptor agonists and suggests their putatively broad therapeutic potential. Paper-11183111.
The effect of intracerebroventricular or intraperitoneal administration of cannabinoid receptor agonist WIN 55,212-2 or inverse agonist AM 251 on food intake and extracellular levels of serotonin and acetic acid 5-hydroxy-indol from presatiated rats was studied. Paper-13777480.
Novel chemical entities having CB1 antagonistic properties have recently been disclosed by several pharmaceutical companies and some academic research groups, some of which are close structural analogs of the leading compound rimonabant ( SR-141716A; Sanofi-Synthélabo). Paper-10651823.
Impulsivity was significantly associated with the 6-repeat allele of the triplet repeat polymorphism (AATn/A6; p < .0001), as well as four SNPs in or near the CNR1 receptor gene: rs1535255 (p = .001), rs2023239 (p = .004), rs1049353 (p < .001) and rs806368 (p < .0006). Paper-13439728.
This inhibition was attenuated by 31.62 nM of the cannabinoid CB1 receptor selective antagonist SR141716A [N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-me thyl-1H-pyrazole-3-carboxamide hydrochloride] only in the myenteric plexus preparation. Paper-1316235.
Compound 3, that is, 2,2-dimethyl-N-(5-methyl-4-(morpholinomethyl)pyridin-2-yl)butanamide was identified as a potent and selective CB2 agonist exhibiting in vivo efficacy after oral administration in a rat model of neuropathic pain. Paper-14013282.
During the structural modification of 1, we found that a novel series of N-alkylidenearylcarboxamide, 4-1, had a moderate affinity for the CB(2) receptor (IC(50)=260 nM, EC(50)=86 nM, E(max)=100%) and good metabolic stability in human liver microsomes. Paper-12575330.
The involvement of the CB1 receptor in mediating reinforcing and physical dependence-producing effects of opioids has also been suggested, with the former being considered the result of interaction with the dopaminergic neurotransmission in the midbrain dopamine system. Paper-8569445.
In this short review, we describe the latest advances in this research field, including the antiobesity effect of the cannabinoid receptor CB1 antagonist rimonabant and the anorexic effect of N-oleoylethanolamine, an endocannabinoid-related, endogenous substance. Paper-12664670.
Custom designed analogs of the natural anti-bacterial peptide cecropin B (CB) have been synthesized; cecropin B-1 ( CB-1) was constructed by replacing the C-terminal segment (residues 26 to 35) with the N-terminal sequence of CB (positions 1 to 10 which include five lysine residues). Paper-1166504.
Stimulation of G(q/11)-coupled M(1), M(3), M(5) muscarinic, V(1) vasopressin, alpha(1a) adrenergic, B(2) bradykinin receptors, but not G(i/o)-coupled M(2) and M(4) muscarinic receptors, also led to paracrine transactivation of CB(1) receptors. Paper-13838399.
We have synthesized a novel series of N-alkyl isatin acylhydrazone derivatives and have identified and characterized several of them as novel analogues with high functional activity and selectivity at human CB2 receptors using [(35)S]GTP-gamma-S assays. Paper-12916826.
Behaviorally, our findings reflect the distribution of CB-1 cannabinoid receptors in the human neocortex, basal ganglia and brainstem and provide evidence for participation of the cannabinoidergic system in high level control of saccades and associated cognitive functions. Paper-9325999.
Moreover, PS inhibition of the capsaicin-induced nocifensive response was not significantly reduced by a nonselective opioid receptor antagonist or by cannabinoid receptor antagonists, indicating that neither an opioid- nor a cannabinoid-dependent mechanism mediated the effect of PS. Paper-12230912.
Cannabinoid actions on the cardiovascular system have been widely interpreted as being mediated by CB1 receptors although there are a growing number of observations, particularly in isolated heart and blood vessel preparations, that suggest that other cannabinoid receptors may exist. Paper-10220355.
Cannabinoid CB1-receptor stimulation in DDT1 MF-2 smooth muscle cells induces a rise in [Ca2+]i, which is dependent on extracellular Ca2+ and modulated by thapsigargin-sensitive stores, suggesting capacitative Ca2+ entry (CCE), and by MAP kinase. Paper-11214826.
Nevertheless, AM404 increases circulating anandamide levels and inhibits motor activity, an effect that is prevented by the CB1 cannabinoid antagonist N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide hydrochloride ( SR141716A). Paper-8991419.
Inverse agonist properties of N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2, 4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide HCl ( SR141716A) and 1-(2-chlorophenyl)-4-cyano-5-(4-methoxyphenyl)-1H-pyrazole-3-carboxyl ic acid phenylamide ( CP-272871) for the CB(1) cannabinoid receptor. Paper-8530499.
The most striking differences were high levels of CB1 receptor in the monkey substantia nigra pars compacta, cerebellar Purkinje cells, and the principal cells of the hippocampus, while few receptors were found in the globus pallidus or substantia nigra pars reticulata. Paper-2002003.
In addition, it considers preclinical findings that suggest that as well as ameliorating signs and symptoms of multiple sclerosis, cannabinoid CB(1) and/or CB(2) receptor activation may suppress some of the pathological changes that give rise to these signs and symptoms. Paper-12528577.
We examined the acute effects of endocannabinoid, anandamide, and of synthetic cannabinoid receptor antagonist, AM251[N-(piperidin-1-yl)-1-(2,4-dichlorophenyl)-5-(4-chlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide], on TSH, thyroxine (T(4)), and triiodothyronine (T(3)) secretions. Paper-13057225.
The allocortex contained very high concentrations of cannabinoid receptor binding sites in the dentate gyrus, Ammons's horn and subiculum of the hippocampal formation; high concentrations of receptors were also present in the entorhinal cortex and amygdaloid complex. Paper-1331311.
CONCLUSIONS: We conclude that pretreatment with EA increases the production of endocannabinoid 2-arachidonylglycerol and N-arach-idonoylethanolamine-anandamide, which elicits protective effects against transient cerebral ischemia through CB1 receptors. Paper-13804261.
Additional compounds, such as selective CB1 receptor agonists, ligands that do not cross the blood brain barrier, drugs interfering with synthesis, degradation or uptake of endogenous ligand(s) of CB receptors, are especially needed to understand when and how cannabinoid systems are activated. Paper-8268991.
A pyridone analogue (5) of the potent bicyclic cannabinoid CP 47,497 (6) has been synthesized as a model for one conformational isomer of anandamide and to test the hypothesis that an amide carbonyl may serve as a hydrogen bond acceptor in interactions with the CB(1) cannabinoid receptor. Paper-8928737.
Preclinical studies have shown that rimonabant, the first CB1-receptor blocker to be available in clinical practice, could not only induce a reduction in food intake, but could also produce body weight loss beyond what could be explained by its effect on food intake. Paper-13316934.
However, the consistent finding of higher binding in the substantia nigra pars reticulata and medial part of the globus pallidus over its lateral segment suggests cannabinoid receptor enrichment on the striatal substance P neurons which express selectively the dopamine D1 receptor. Paper-7538507.
Mass spectrometric identification of all amino acid residues in the cannabinoid CB2 receptor is a key step toward the "Ligand Based Structural Biology" approach developed in our laboratory for characterizing ligand binding sites in GPCRs using a variety of covalent cannabinergic ligands. Paper-13262489.
In Parkinson's disease, WIN55,212-2-stimulated [35S]GTPgammaS binding in the caudate nucleus, putamen, lateral globus pallidus and substantia nigra was increased, thus indicating a more effective activation of GTP-binding protein-coupled signalling mechanisms via CB1 receptors. Paper-10714570.
In conclusion, our results showed that anandamide has a potentiating effect on NANC-mediated relaxation of rat corpus cavernosum through both CB1 and vanilloid receptors and the NO-mediated component of the NANC relaxant responses to electrical stimulation is involved in this enhancement. Paper-12165834.
In the presence of rauwolscine, clonidine-induced inhibition of electrically evoked [3H]noradrenaline release was counteracted by 1 microM of the selective CB1 receptor antagonist SR141716A (N-[piperidin-1-yl]-5-[4-chlorophenyl]-1-[2,4-dichlorophenyl] -4-methyl-1H-pyrazole-3-carboxamide). Paper-1606607.
Depolarization-induced suppression of excitation and inhibition (DSE/DSI) appears to be an important form of short-term retrograde neuronal plasticity involving endocannabinoids (eCBs), the activation of presynaptic cannabinoid CB1 receptors, and the suppression of neurotransmitter release. Paper-13935267.
Recent physiological, pharmacological, and high-resolution anatomical studies provided evidence that the major physiological effect of cannabinoids is the regulation of neurotransmitter release via activation of presynaptic CB1 receptors located on distinct types of axon terminals throughout the brain. Paper-9757978.
To do so, we first investigated the presence of the cannabinoid receptors CB(1) and CB(2) mRNAs in the human Kaposi's sarcoma cell line KS-IMM by RT-PCR and, subsequently, the effects of the mixed CB(1)/CB(2) agonist WIN-55,212-2 (WIN) on cell proliferation in vitro. Paper-13908641.
This was unaltered following pretreatment with the cannabinoid CB(1) receptor-selective antagonist AM251 (10(-7) M), however in isolation AM251 elicited a significant rightward shift in the potency of acetylcholine-evoked contraction in both longitudinal muscle and circular muscle preparations. Paper-12579026.
To this extent, male Sprague-Dawley rats were exposed to 21 days of restraint stress (6 h/day), after which autoradiographical analysis of cannabinoid CB(1) receptor binding site densities were examined in the CA1, CA3 and dentate gyrus subfields of the hippocampus. Paper-13827797.
Rimonabant hydrochloride, the first drug in a new class of selective cannabinoid type 1 ( CB1) receptor antagonists, is showing promise in clinical trials for the treatment of obesity and related metabolic risk factors, in addition to tobacco dependence. Paper-11495361.
The stimulatory effect of WIN55,212-2 on the evoked tritium efflux was inhibited by the selective CB1 cannabinoid receptor antagonist N-(piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (AM251, 100 nM) and by the GABA(A) receptor antagonist bicuculline (10 microM). Paper-13764125.
Over the past 15 years, research on the endogenous cannabinoid ( CB) system-now usually referred to as the endocannabinoid system (ECS)-has identified the significant effects of the ECS on the regulation of food intake and lipid and glucose metabolism in animals and humans. Paper-12527355.
Weight-loss interventions, such as a hypocaloric diet and physical exercise, in addition to agents such as orlistat, sibutramine and cannabinoid receptor antagonists, may have favourable effects upon fat storage, nutrient metabolism and ultimately glucose tolerance or type-2 diabetes. Paper-12994745.
Several lines of preclinical evidence indicate the ability of the prototypic cannabinoid CB(1) receptor antagonist, rimonabant, to suppress various alcohol-related behaviors, including alcohol drinking and seeking behavior and alcohol self-administration in rats and mice. Paper-12528583.
OBJECTIVE: To determine whether CB1 receptor blockade is equipotent at modulating food and water intake, body weight, and scratching behavior, the effect of a range of SR141716A doses on these behaviors in food-restricted postnatal day (P) 18, 28, and 60 male rats was investigated. Paper-13934320.
In MPTP-lesioned marmosets previously treated with levodopa to establish LID, attenuation of CB1 signaling by systemic administration of rimonabant (1 and 3 mg/kg) had anti-parkinsonian actions, equivalent to a 71% increase in motor activity at 3 mg/kg. Paper-11180412.
As the endogenous cannabinoid receptor agonist, anandimide, has been shown to modulate dopamine neurotransmission within the basal ganglia, the loss of cannabinoid receptors may contribute to the development of motor symptoms or cognitive decline or both seen in Huntington's disease patients. Paper-8435549.
Our results demonstrate that only 10(-8) mol/L of 17beta-estradiol was able to induce significantly higher levels of CB1A mRNA, while no effects were found after treatment with 4-nonylphenol (10(-8) or 10(-6) mol/L); moreover, mRNA expression titers of CB1B did not show any significant change. Paper-13798219.
No significant differences in cannabinoid receptor agonist (CP55,940 approximately WIN55,212-2 > JWH015) or antagonist(SR144528 approximately AM1241 > AM630 > AM251 approximately SR141617A) profiles were observed in HEK-hCB(2)-G(qo5) and HEK-hCB(2)-G(qi5) cells as determined using intracellular Ca(2+) measurements. Paper-13587415.
Here we show that treatment of rat C6 glioma cells with the raft disruptor methyl-beta-cyclodextrin (MCD) doubles the binding efficiency (i.e. the ratio between maximum binding and dissociation constant) of type-1 cannabinoid receptors ( CB1R), which belong to the rhodopsin family of G protein-coupled receptors. Paper-10782486.
The purpose of this investigation was to investigate the antiemetic potential of the aminoalkylindole cannabinoid receptor agonist WIN 55, 212-2 [R(+)-[2,3-dihydro-5-methyl-3-[(morpholinyl) methyl] pyrolol [1,2,3-de]-1,4-benzoxazin-yl]-(1-naphthalenyl) methanone mesylate] against cisplatin-induced vomiting. Paper-9110070.
Recently, it has been shown that rimonabant prevents indomethacin-induced intestinal injury by decreasing the levels of pro-inflammatory cytokine tumour necrosis factor alpha (TNFalpha), thus indicating that CB1 receptor antagonists might exhibit potential anti-inflammatory activity in acute and chronic diseases. Paper-12254479.
In both disorders, the key mechanisms involved in the neuroprotection provided by cannabinoids include cannabinoid receptor-independent effects aimed at reducing the oxidative injury, and also cannabinoid 2 receptors (CB2)-mediated effects exerted by regulating the influence of reactive microglia on neuronal homeostasis. Paper-13446795.
Disruption of lipid rafts following cholesterol depletion with methyl-beta-cyclodestrin (MCD) failed to affect synthesis and degradation of anandamide, while it caused a marked increase in the synthesis and concentration of 2-arachidonoylglycerol (2-AG), as well as in the binding activity of cannabinoid CB1 receptors. Paper-13696244.
Moreover, cells expressing C-terminal His-tagged CB1 were shown to inhibit forskolin-stimulated cyclic adenosine 3',5'-monophosphate (cAMP) production in a concentration-dependent manner in the presence of CP-55,940, confirming the expressed receptor's functional characteristics. Paper-11239846.
Nevertheless, it was possible to conclude that the antiproliferative effects of anandamide were not solely mediated by either its hydrolysis to produce arachidonic acid or its CB receptor-mediated activation of phospholipase A(2) since palmitoyltrifluoromethyl ketone did not prevent the response to anandamide. Paper-10028880.
This study reveals that certain endogenous lipids, phytocannabinoids, and related ligands are potent inhibitors of human neutrophil migration, and it implicates a novel pharmacological target distinct from cannabinoid CB(1) and CB(2) receptors; this target is antagonized by the endogenous compound N-arachidonoyl l-serine. Paper-12705886.
Important advances have been made in our understanding of cannabinoid receptor signaling pathways, their modulation of synaptic transmission and plasticity, the cellular targets of cannabinoids in different central nervous system (CNS) regions and, in particular, the role of the endogenous brain cannabinoid (endocannabinoid) system. Paper-10685381.
This effect was completely blocked by the cannabinoid receptor antagonist rimonabant (0.5 mg/kg, i.v.). In addition, the blockade of excitatory amino acids receptors by kynurenic acid (0.5 muM, i.c.v.) or a chemical lesion of the subthalamic nucleus (STN) with ibotenic acid abolished Delta(9)-THC effect. Paper-12725577.
Furthermore, CB1 receptor protein-immunoreactivity as well as inhibitory effects of AEA and URB597 on the depolarization-evoked Ca(2+) transient were increased in small DRG neurons cocultured with fibrosarcoma cells indicating that fibrosarcoma cells are sufficient to evoke phenotypic changes in AEA signaling in DRG neurons. Paper-13063087.
Specifically, pharmacological and genetic blockade of the cannabinoid CB1 receptor induces a phenotypic state that is analogous to melancholic depression, including symptoms such as reduced food intake, heightened anxiety, increased arousal and wakefulness, deficits in extinction of aversive memories and supersensitivity to stress. Paper-11523868.
The CB(1) receptor antagonist SR141716 ( rimonabant; 0.12-1.0 mg/kg, i.m.) and the stimulant anorectic drug d-amphetamine (0.12-1.0 mg/kg, i.m.) were administered to non-food deprived baboons for the purpose of measuring the effect of each drug on consumption of the normal diet, and a large single meal of a high-carbohydrate candy. Paper-13273001.
To test the importance of these residues for receptor recognition, recombinant human CB(1) receptors, stably expressed in human embryonic kidney 293 cells, were used to investigate the consequences of mutating Ser2.60 (to S2.60A) or Ser7.39 (to S7.39A) in radioligand binding and guanosine 5'-3-O-(thio)triphosphate functional assays. Paper-13253139.
The selective CB1 receptor antagonist SR141716A (10nM) counteracted the WIN 55,212-2-induced increase in extracellular glutamate levels in cultures exposed to vehicle or carbon monoxide during gestation, but failed to antagonise it in cultures from rats born to mothers exposed to WIN 55,212-2 alone or in combination with carbon monoxide. Paper-12276934.
Selective CB1 receptor antagonists are in development for the treatment of obesity and tobacco smoking, and could be tested for antidepressant efficacy because recent results of clinical studies suggest that they would also treat comorbid symptoms of depression such as cognitive deficiencies, weight gain, impulsivity and dependence disorders. Paper-11208985.
METHODS: CB2 receptors were characterized in biopsy specimens of normal human liver and active cirrhosis by immunohistochemistry, and in cultures of hepatic stellate cells and hepatic myofibroblasts by reverse-transcription polymerase chain reaction ( RT-PCR), immunocytochemistry, and GTPgammaS assays. Paper-11005741.
6. Pretreatment of the cells with either 200 microM phenylmethylsulphonyl fluoride (to inhibit the conversion of anandamide into arachidonic acid) or 400 ng ml(-1) pertussis toxin (to uncouple CB1 cannabinoid receptors from Gi/o proteins) had no significant effect on the mobilization of cytosolic Ca2+ evoked by either anandamide, or histamine. Paper-1872363.
The endogenous C18 N-acylethanolamines (NAEs) N-linolenoylethanolamine (18:3 NAE), N-linoleoylethanolamine (18:2 NAE), N-oleoylethanolamine (18:1 NAE), and N-stearoylethanolamine (18:0 NAE) are structurally related to the endocannabinoid anandamide (20:4 NAE), but these lipids are poor ligands at cannabinoid CB(1) receptors. Paper-11474135.
Moreover, using pharmacological and genetic tools, we found that THC long-term memory deficits were mediated by CB1Rs expressed on GABAergic interneurons through a glutamatergic mechanism, as both the amnesic-like effects and p70S6K phosphorylation were reduced in GABA- CB1R knockout mice and by NMDA blockade. Paper-13956075.
These synonyms are used for gene CNR1 (cannabinoid receptor 1 (brain)): CNR, CB-R, CB1R, CB1K5, CB1A, CB1, Cannabinoid receptor 1, CANN6.
These accession numbers are used for gene CNR1: Q9UNN0 (UNIPROT__AC), Q5UB37 (UNIPROT__AC), CAA57018 (NCBI_GENBANK__AC), AAD34320 (NCBI_GENBANK__AC).
CNR1 is a homologue of CNR1 (cannabinoid receptor 1 (brain)) from Pan troglodytes.
CNR1 is a homologue of CNR1 (cannabinoid receptor 1 (brain)) from Gallus gallus.
CNR1 is a homologue of CNR1 (cannabinoid receptor 1 (brain)) from Canis lupus familiaris.
CNR1 is a homologue of Cnr1 (cannabinoid receptor 1 (brain)) from Mus musculus.
CNR1 is a homologue of Cnr1 (cannabinoid receptor 1 (brain)) from Rattus norvegicus.
CNR1 is a homologue of cnr1 (cannabinoid receptor 1) from Danio rerio.
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iHOP - Information Hyperlinked over Proteins .
Concept & Implementation by Robert Hoffmann.