Click here for the function of PDE5A.
Edit this page in Wiki Genes - PDE5A or see Wiki Gene.
Phosphodiesterase type 5 ( PDE5) inhibitors. Paper-9703623.
Comparison of phosphodiesterase type 5 ( PDE5) inhibitors. Paper-12166977.
SCH 51866 is a potent and selective PDE1 and PDE5 inhibitor. Paper-940545.
Together, PDE5 and PDE1A lower cGMP sufficiently to allow contraction. Paper-9951424.
Phosphodiesterase type 5 ( PDE5) inhibitor "on-demand" use was applied. Paper-13094160.
Cardiac safety of phosphodiesterase type 5 ( PDE5) inhibitors validated. Paper-11849453.
PDE4 and PDE5 selectively hydrolyze cAMP and cGMP, respectively. Paper-10456191.
PDE4 and PDE5 were detected in lysates of all cell types studied. Paper-1748705.
Effects of icariin on cGMP-specific PDE5 and cAMP-specific PDE4 activities. Paper-10016720.
The PDE5 inhibitor was as effective as cpt-cyclic AMP or a selective PDE4 inhibitor. Paper-2067491.
PDE5 inhibition did not alter relaxation of omental arteries from women with PE. Paper-12136424.
Oral phosphodiesterase type 5 ( PDE5) inhibitor therapy did not improve erectile function. Paper-12144834.
The phosphodiesterase-5 ( PDE-5) inhibitors are a relatively new form of treatment for PAH. Paper-12134859.
In the kidney, PDE5 is involved in the regulation of sodium excretion and renin secretion. Paper-9538081.
Longer term, both PDE5 and PDE1A mRNA are induced by chronic stimulation of guanylyl cyclase. Paper-9951424.
We aimed to assess whether the effect of PDE5 inhibition in PE was myometrial artery specific. Paper-12136424.
A549 cells expressed a high level of PDE4, lower levels of PDE1 and PDE3, and minor PDE5 activity. Paper-1714542.
The expression of PDE5 and NOX-1 was assessed using Western blotting and superoxide measured. Paper-13087781.
PDE5 inhibitors may also be useful in situations of temporary ED in couples undergoing IVF. Paper-10175950.
Sildenafil, a phosphodiesterase type 5 ( PDE5) inhibitor, enhances neurogenesis in young rats. Paper-11821235.
No head-to-head studies have been conducted with the phosphodiesterase type 5 ( PDE5) inhibitors to date. Paper-10230160.
The phosphodiesterase type 5 ( PDE-5) inhibitors are effective in treating erectile dysfunction (ED). Paper-13765603.
The hPDE5 GAF domain has an inhibitory effect on AC activity, which is released upon cGMP activation. Paper-12066042.
We used phosphodiesterase type 5 ( PDE5) inhibitors to study the role of cGMP in object- and spatial memory. Paper-10523207.
Phosphodiesterase type 5 ( PDE5) inhibitors are the first-line treatment for erectile dysfunction (ED). Paper-13615020.
Vardenafil and sildenafil are potent and specific phosphodiesterase type 5 ( PDE 5) inhibitors. Paper-9454807.
Phosphodiesterase type 5 ( PDE5) is responsible for the degradation of cGMP and regulation of CC muscle tone. Paper-10581185.
Recreational Use of PDE5 Inhibitors by Young Healthy Men: Recognizing This Issue Among Medical Students. Paper-13068985.
However, YC-1 has also been shown to inhibit the major cGMP-degrading enzyme phosphodiesterase type 5 ( PDE5). Paper-10348162.
RESULTS: Icariin and papaverine showed dose-dependent inhibitory effects on PDE5 and PDE4 activities. Paper-10016720.
Compound 5v also showed preference for PDE4 with selectivity of >2000-fold over PDE7, PDE9, PDE2, and PDE5. Paper-13511185.
The exon organization of the PDE11A catalytic domain was very similar to those of PDE5A and PDE6B. Paper-8689020.
The PDE5 inhibitor sildenafil increases circulating endothelial progenitor cells and CXCR4 expression. Paper-13541592.
Vardenafil ( Levitra) is a potent and highly selective oral phosphodiesterase type 5 ( PDE5) inhibitor. Paper-10129779.
INTRODUCTION: Phosphodiesterase type 5 ( PDE5) hydrolyses cyclic guanylate monophosphate (cGMP) specifically to 5' GMP. Paper-13092863.
Expression levels of HO-1, HO-2, sGC, and phosphodiesterase type 5 ( PDE5) were examined with Western blot. Paper-12144822.
RESULTS: The treatment of ED was revolutionized by the introduction of phosphodiesterase type 5 ( PDE5) inhibitors in 1998. Paper-11609808.
The selectivity ratio vs PDE-5 is more than 10 000 for PDE-1 through PDE-4 and PDE-7 through PDE-10 and 780 for PDE-6. Paper-9187184.
A continuous phosphodiesterase type-5 inhibitor ( PDE5) was started and the patient had no recurrences at 3-month follow-up. Paper-13510919.
Among them are Rho-kinase inhibitors, soluble guanylate cyclase activators and nitric oxide-releasing PDE5 inhibitors. Paper-9643407.
Docking of the PDE5 inhibitor sildenafil into the PDE4 catalytic pocket further helps understand inhibitor selectivity. Paper-9915419.
Tadalafil (Cialis((R))) is a long-acting phosphodiesterase type-5 ( PDE-5) inhibitor used to treat erectile dysfunction. Paper-13587888.
The results thus suggest that cognitive impairment might be due to the modulatory effect of nNOS or PDE5 enzyme on cGMPlevels. Paper-12145672.
Through phosphodiesterase type 5 ( PDE5) inhibition, it induces relaxation in penile smooth muscle, resulting in erection. Paper-12144826.
Phosphodiesterase type 5 ( PDE-5) inhibitors are a class of drugs used primarily in the treatment of erectile dysfunction. Paper-12183649.
Systemic treatment with oral phosphodiesterase type-5 ( PDE-5) inhibitors is the current standard of care for patients with ED. Paper-10225904.
We demonstrate functional coupling between the hPDE5 GAF ensemble and the AC resulting in a chimera stimulated 10-fold by cGMP. Paper-12066042.
OBJECTIVE: To evaluate the efficacy of the phosphodiesterase type 5 ( PDE5) inhibitors in the treatment of Raynaud's phenomenon. Paper-12162092.
First-dose success of phosphodiesterase type 5 ( PDE5) inhibitors may be adversely affected in patients with comorbidities. Paper-12297117.
Exposure of CF cells to an inhibitor of cGMP-specific phosphodiesterase PDE5, Sildenafil, normalized the endosomal pH. Paper-11834737.
Phosphodiesterase type 5 ( PDE 5) is the predominant enzyme responsible for cGMP hydrolysis in trabecular smooth muscle. Paper-8824540.
INTRODUCTION: Phosphodiesterase type 5 ( PDE5) inhibitors are widely used as first-line therapy for erectile dysfunction (ED). Paper-13665308.
Primary HBE cultures expressed PDE4 and PDE1 activity at approximately equal levels with small additional PDE3 and PDE5 activities. Paper-1714542.
AIM: To assess the effects of sildenafil (a type 5 phosphodiesterase [ PDE5] inhibitor) administration in 20 healthy young men. Paper-13541592.
Vardenafil is a phosphodiesterase type-5 ( PDE-5) inhibitor developed as an oral therapy for erectile dysfunction (ED). Paper-10077795.
Phosphodiesterase type 5 ( PDE5) is the predominant enzyme in the corpus cavernosum, and plays a crucial role in penile erection. Paper-9701003.
Under stimulation with 8-bromo-cAMP or 8-bromo-cGMP, however, inhibitors of PDE2, PDE3, PDE4 and PDE5 enhanced activation of CRE. Paper-12146273.
The peripherally acting oral phosphodiesterase type 5 ( PDE5) inhibitors are the mainstay of oral medical treatment of ED in diabetics. Paper-12324597.
Patients should be advised that many treatment options are available for ED, including the phosphodiesterase type 5 ( PDE5) inhibitors. Paper-10295429.
Expression of HO-1 and sGC was upregulated and that of PDE5 downregulated in hemin-treated, but not hydralazine-treated, SHR. Paper-12144822.
PDE-5 inhibition impedes TSP-1 expression, TGF-beta activation and matrix accumulation in experimental glomerulonephritis. Paper-13037524.
Phosphodiesterase type 5 ( PDE5) inhibitors are recommended as first-line therapy for erection problems of all etiologies and severities. Paper-13598147.
Both subdomains are structurally and functionally interdependent and act in concert in regulating cycaB1 AC and, most likely, also hPDE5. Paper-12066042.
These data suggest that the PDE-5 inhibitors are effective in treating PAH and that it is likely that their usage will increase over time. Paper-12134859.
We have previously demonstrated that PDE5 inhibition can improve endothelial function in myometrial small arteries from women with PE. Paper-12136424.
There is now an expanding armamentarium for the management of ED, including oral agents such as phosphodiesterase type 5 ( PDE5) inhibitors. Paper-10175950.
SCH 51866 inhibited PDE1 and PDE5 isozymes with a 50% inhibitory concentration ( IC50) of 70 and 60 nM, respectively. Paper-940545.
Pretreatment of neutrophils with the PDE3 inhibitor ORG 9935 or the PDE5 inhibitor zaprinast had no effect on IL-8 generation. Paper-1420038.
Orally administered phosphodiesterase type 5 ( PDE5) inhibitors have become the first-line treatment option for erectile dysfunction (ED). Paper-10231391.
AIM: To investigate the role of hypogonadism on phosphodiesterase type 5 ( PDE5) expression and sildenafil responsiveness in diabetes. Paper-11345292.
Treatment options have widened since the launch of the phosphodiesterase type 5 ( PDE5) inhibitor, sildenafil citrate (Viagra trade mark ). Paper-9643407.
Phosphodiesterase type-5 ( PDE-5) inhibitors have revolutionized the treatment of post-radical prostatectomy erectile dysfunction. Paper-12103386.
PDE9A lacks a region homologous to the allosteric cGMP-binding regulatory regions found in the cGMP-binding PDEs: PDE2, PDE5, and PDE6. Paper-1469303.
In conclusion, the data suggest that inhibition of PDE1 and PDE5 isozymes by SCH 51866 exerts antiplatelet and vascular protective effects. Paper-940545.
Most of the talks focused on PDE4 and PDE5. two members of the 11-member PDE family that have attracted much interest over the last several years. Paper-8591011.
For example, we have recently found that PDE5 is expressed in all Purkinje neurons while PDE1B is expressed in only a subset of these neurons. Paper-10523200.
The potencies of selectivity of icariin and papaverine on PDE5 ( PDE4/ PDE5 of IC(50)) were 167.67 times and 4.54 times, respectively. Paper-10016720.
The antiplatelet, antiproliferative, and hemodynamic effects of SCH 51866 were compared with those of E4021, a highly selective PDE5 inhibitor. Paper-940545.
Expression of PDE5A1 and A2 mRNA in various tissues was examined by Northern blotting and reverse transcription-polymerase chain reaction. Paper-9892189.
Therefore, the GAFa domain of PDE5A adopts a structure similar to the GAFb domain of PDE2A, and provides the sole site for cGMP binding in PDE5A. Paper-9860369.
CONCLUSION: Use of PDE5 inhibitors does not significantly alter endothelial-dependent relaxation in omental or placental small arteries from PE women. Paper-12136424.
Prolonged upregulation of HO-1 and sGC as well as lowered expression of PDE5 may at least partially explain the effect of hemin treatment on ICP. Paper-12144822.
Phosphodiesterase type 5 ( PDE5) inhibitors, sildenafil, vardenafil, and tadalafil, provide effective treatment of erectile dysfunction. Paper-12163143.
This phosphodiesterase type-5 ( PDE-5) inhibitor is selective for corpus cavernosum smooth muscle tissue and produces excellent erectile function. Paper-10077796.
The upstream PDE5A promoter is expected to direct the expression of all three PDE5 isoforms while the intronic PDE5A2 promoter only the A2 isoform. Paper-9403134.
Among the newer treatments for PAH, endothelin receptor antagonists and phosphodiesterase type 5 ( PDE5) inhibitors have reshaped clinical practice. Paper-11483589.
As such, sildenafil (and, likely, other new phosphodiesterase type 5 [ PDE5] inhibitors) is contraindicated in men who use nitrate medications. Paper-9701005.
The scientific rationale of pharmacologically inhibiting phosphodiesterase type 5 ( PDE5) in the treatment of erectile dysfunction (ED) is reviewed. Paper-9559537.
Examples are milrinone and trequinsin (PDE3); rolipram and Ro 20-1724 ( PDE4); and zaprinast, sildenafil and didyridamole ( PDE5). Paper-8341078.
The inhibitory effects of icariin on PDE5 and PDE4 activities were investigated by the two-step radioisotope procedure with [(3)H]-cGMP/[(3)H]-cAMP. Paper-10016720.
Daily treatment with phosphodiesterase type 5 ( PDE5) inhibitors has beneficial effects on endothelial function in men with increased cardiovascular risk. Paper-13049117.
Phosphodiesterase type-5 ( PDE-5) inhibitors are a new class of vasoactive drugs that have been developed for treatment of erectile dysfunction (ED). Paper-10685998.
A Rho-kinase inhibitor, soluble guanylate cyclase activator and nitric oxide-releasing PDE5 inhibitor: novel approaches to erectile dysfunction. Paper-9643407.
The PDE5A promoter overlaps with the A1-specific exon, while the PDE5A2 promoter is located between the A3- and A2-specific exons. Paper-10456187.
Phosphorylation of PDE5 increases its enzymatic activity as well as the affinity of its allosteric (noncatalytic/ GAF domains) sites for cGMP. Paper-10456186.
In addition to increasing PDE5 activities, IL-1 treatment reduced the sensitivity of PDE5 to several pharmacological inhibitors by up to 50-fold. Paper-1605391.
Inhibition of cGMP-specific phosphodiesterase type 5 ( PDE5) has been shown to improve penile erection in patients with erectile dysfunction. Paper-9892189.
BACKGROUND: The cardiovascular effects of sildenafil (Viagra), a selective inhibitor of phosphodiesterase type 5 ( PDE5), have been extensively studied. Paper-9363367.
There is evidence demonstrating the protective effect of cGMP-specific phosphodiesterase type 5 ( PDE5) inhibitors against ischemic injury in certain tissues. Paper-13739219.
5. Our results show that increased expression of PDE3 and PDE5 might explain some changes in vascular reactivity of pulmonary vessels from rats with PHT. Paper-9650726.
Of the current options available to treat erectile dysfunction, oral phosphodiesterase type 5 ( PDE5) inhibitors are the recommended first-line treatment. Paper-12166977.
The purpose of this study was to determine the effect of sildenafil, an inhibitor of phosphodiesterase type 5 ( PDE5), on endothelial function in smokers. Paper-9684401.
Recently, we showed that within the NO-induced cGMP response in human platelets, activation and phosphorylation of phosphodiesterase type 5 ( PDE5) occurred. Paper-9855151.
A recently shown direct activation of PDE5 by cGMP binding to the GAF A domain suggests that this regulatory site might be a target for new drug development. Paper-9951424.
MAIN OUTCOME MEASURES: Expression of PDE5 and AR messenger RNA (mRNA) and protein have been measured by RT-PCR and Western blot, respectively. Paper-13615029.
However, the PDE5 inhibitor had no effect on basal or isoproterenol- stimulated cyclic AMP levels and did not stimulate mucin secretion. Paper-2067491.
INTRODUCTION: Oral treatment with phosphodiesterase type 5 inhibitor ( PDE5) is considered the first-line treatment for patients with erectile dysfunction (ED). Paper-13487209.
The purpose of this review is to present a current view of the pathogenesis and treatment of PAH, with an emphasis on the use of PDE-5 inhibitors in these patients. Paper-12134859.
METHODS: PDE5 was isolated from the human platelet and PDE4 from the rat liver tissue using the FPLC system (Pharmacia, Milton Keynes, UK) and the Mono Q column. Paper-10016720.
PDE11A exhibits </=50% amino acid identity with the catalytic domains of all other PDEs, being most similar to PDE5, and has distinct biochemical properties. Paper-2174094.
In contrast to the distribution of PDE4, immunoactivity indicating PDE5 (cGMP-PDE) and 11 (dual substrate PDE) was mainly observed in glandular and subglandular areas. Paper-11313784.
In this study, we compared the inhibition of cGMP hydrolysis by vardenafil and sildenafil; two inhibitors selective for phosphodiesterase type 5 ( PDE5). Paper-9069471.
Cardiovascular effects of sildenafil in hypertensive men with erectile dysfunction and different alleles of the type 5 cGMP-specific phosphodiesterase ( PDE5). Paper-10924541.
Sildenafil, a selective inhibitor of phosphodiesterase type 5 ( PDE5), is the first in a new class of orally effective treatments for erectile dysfunction. Paper-1759732.
Phosphodiesterase type 5 ( PDE5) inhibitors are potent vasodilators of penile resistance arteries and increase the content and effects of basally released endothelial NO. Paper-12688472.
PDE5A gene encodes type 5 phosphodiesterase ( PDE5), the principal cGMP-catalyzing enzyme in the penis and the primary target of sildenafil (Viagra). Paper-8691827.
PDE5A gene encodes type 5 phosphodiesterase ( PDE5), the principal cGMP-catalyzing enzyme in the penis and the primary target of sildenafil (Viagra). Paper-8691828.
Nor did the PDE4-selective inhibitor rolipram or the PDE5-selective inhibitor dipyridamole influence the insulin-induced decrease in muscle tissue glycerol. Paper-1506638.
The findings suggested that PDE11A has a common ancestral gene with PDE5A and PDE6s, whereas PDE2A and PDE10A are generated separately from these three GAF-PDEs. Paper-8689020.
Sildenafil is a selective inhibitor of phosphodiesterase type 5 ( PDE5), which has been shown to be a clinically effective treatment for erectile dysfunction. Paper-1759728.
The distribution pattern of the mRNA for the isoenzymes PDE3A and PDE5A may explain the pharmacological effects as well as the side effects of milrinone and sidenafil. Paper-8359474.
Management featured use of a long-term, on-demand phosphodiesterase type 5 ( PDE5) inhibitor regimen for ED, and close surveillance with no immunosuppressive therapy for PAN. Paper-13698949.
Protein kinase G (PKG)-mediated phosphorylation and allosteric cGMP binding upregulate PDE5 activity, while PP1 phosphatase-mediated dephosphorylation downregulates. Paper-12254497.
Vardenafil selectively inhibits phosphodiesterase type 5 ( PDE5), an enzyme which hydrolyses cyclic guanosine monophosphate in the cavernosum tissue of the penis. Paper-9186505.
Analysis of phosphodiesterase (PDE) isozymes in HT1376 cells showed PDE5 and PDE4 isozymes that were inhibited by exisulind with IC(50)s of 112 and 116 microM, respectively. Paper-8964835.
One method of intervention is inhibition of the phosphodiesterase type 5 ( PDE5) enzyme, which has already been exploited with a considerable degree--though not complete--success. Paper-9802567.
Erectile dysfunction (ED) pharmacotherapy has undergone dramatic advances over the past decade, since the introduction of phosphodiesterase type 5 inhibitors ( PDE5). Paper-9643410.
BACKGROUND: In clinical practice, we commonly encounter sexually healthy males who use phosphodiesterase type 5 ( PDE5) inhibitors and report a beneficial effect to their sex life. Paper-13074854.
The recent addition of vardenafil and tadalafil to the market has increased the number of phosphodiesterase type 5 inhibitors ( PDE5) to three agents used throughout the world. Paper-11382779.
The relaxing effect of the phosphodiesterase type 5 ( PDE5) inhibitors on vascular smooth muscle has attracted much attention, especially in persons with cardiovascular disease. Paper-10295432.
Vardenafil inhibits the activity of phosphodiesterase type 5 ( PDE-5), which degrades cyclic guanossine monophosphate (cGMP) and results in relaxation of smooth muscle. Paper-13748388.
The IC(50) of Icariin and papaverine on PDE5 were 0.432 micromol/L and 0.680 micromol/L, respectively and those on PDE4, 73.50 micromol/L and 3.07 micromol/L, respectively. Paper-10016720.
This action on renin secretion may help explain why sildenafil only has minor effect on blood pressure despite the widespread distribution of PDE5 in vascular tissues. Paper-9538081.
Phosphodiesterase type 5 ( PDE 5) is the major cGMP hydrolyzing enzyme in penile corpus cavernosum and is an important regulator of nitric oxide-mediated smooth muscle relaxation. Paper-10145947.
Rat clitorises express components of the proposed pathway: neuronal and endothelial NO synthases, soluble guanylyl cyclase (sGC), type 5 phosphodiesterase ( PDE-5), and BK(Ca) channels. Paper-10642626.
Tadalafil (Cialis; Eli Lilly & Co., ICOS) and vardenafil ( Levitra; Bayer Pharmaceuticals, GlaxoSmithKline) are new PDE5 inhibitors that have recently been approved worldwide. Paper-10856438.
Phosphodiesterase type-5 ( PDE-5) inhibitors are well tolerated and efficacious treatments for male erectile dysfunction that currently rank among the best-selling drugs worldwide. Paper-13080525.
The nonselective inhibitor 3-isobutyl-1-methylxanthine (IBMX) binds to a similar subpocket in the active sites of PDE4, PDE5, and PDE9 and has a common pattern of the binding. Paper-10339924.
An overview is given of the different PDEs that are known and we focus on three PDEs which have been identified as possible relevant targets for memory improvement: PDE2, PDE4 and PDE5. Paper-12064597.
5. ANP is capable of inhibiting collagen synthesis in adult rat and human cardiac fibroblasts via cyclic GMP, a property unmasked and enhanced by inhibition of PDE5. Paper-1611755.
PDE5 inhibitor therapy, has been found to be effective in special clinical populations, such as those with prostate cancer, diabetes, and cardiovascular disease. Paper-12254498.
The modulation of ROS and cyclooxygenase-derived vasoconstrictors generation by a chronic treatment with sildenafil may represent an added benefit beyond PDE5 inhibition. Paper-13049117.
In the enzyme assays, it has been shown that all the target compounds 9a-l proved to be more potent in inhibiting phosphodiesterase type 5 ( PDE5) than sildenafil by 4-38-fold. Paper-8928754.
Sildenafil is a potent and selective inhibitor of phosphodiesterase type 5 ( PDE5), the enzyme responsible for the degradation of cyclic guanosine monophosphate ( cGMP). Paper-8564523.
We have also investigated the effects of some specific inhibitors of phosphodiesterases (PDE1, PDE3, PDE4 and PDE5) on human neuroblastoma (LAN5 and SHEP) growth and differentiation. Paper-10871505.
In the presence of 1 mM EGTA, gustin activated cAMP PDE 5- to 6-fold, but the activating ability was completely lost after gustin was heated at 100 degrees C for 5 min. Paper-5567126.
In extracts of human platelets, three isoenzymes of cyclic nucleotide phosphodiesterase (PDE), namely, PDE2, PDE3, and PDE5, were identified; activities of PDE1 and PDE4 were not detected. Paper-953582.
[3H]Sildenafil binding isotherm of PDE5 indicated KD was 8.3 to 13.3 nM, and low cGMP decreased the KD to 4.8 nM but only slightly increased Bmax to a maximum of 0.61 mol/ mol-subunit. Paper-9709983.
Phosphodiesterase type 5 ( PDE5) is one of the members of the superfamily that specifically cleaves cyclic guanosine monophosphate ( cGMP), a key intracellular secondary messenger. Paper-10639566.
Increased myocardial cGMP, achieved by enhancing cyclase activity or impeding cGMP hydrolysis by phosphodiesterase type-5 ( PDE5A), suppresses cellular and whole organ hypertrophy. Paper-13656843.
BACKGROUND AND PURPOSE: Orthostatic hypotension has been observed when PDE 5 (cGMP-specific phosphodiesterase type 5) inhibitors are co-administered with alpha-adrenoceptor antagonists. Paper-13717145.
ABSTRACT: BACKGROUND: Vardenafil (Levitra(R)) represents a potent and highly selective phosphodiesterase type 5 ( PDE5) inhibitor, which is established for treatment of various diseases. Paper-13644931.
The immediate objective of phosphodiesterase type 5 ( PDE5) inhibitor treatment is to restore the ability of a man to achieve and/or maintain an erection adequate for sexual intercourse. Paper-13742839.
INTRODUCTION: Phosphodiesterase type 5 inhibitor ( PDE5) use is a treatment strategy for prostate cancer patients with post-radiation therapy (RT) erectile dysfunction (ED). Paper-13698960.
Decreased expression or activity of neuronal or endothelial NO synthase ( NOS), impaired NO release, or NO destruction will preclude sufficient cGMP formation to permit PDE5 inhibitor efficacy. Paper-10456195.
Human platelets were found to contain PDE5, which was inhibited by 50% ( IC50) by sildenafil at a concentration of 6.3 nM, consistent with the IC50 value in the corpus cavernosum. Paper-1759728.
BACKGROUND AND OBJECTIVES: The Department of Health issued guidelines for the NHS treatment of erectile dysfunction (ED) with phosphodiesterase type 5 inhibitors ( PDE 5 inhibitors) in 1999. Paper-11091167.
Cloning and sequencing of the PDE5A gene showed that the isoform-specific 5'-ends of the PDE5 mRNAs are encoded from three alternative first exons arranged in the order of A1-A3- A2. Paper-9403134.
Introduction. Recent reports have linked the use of phosphodiesterase type 5 ( PDE-5) inhibitors with increased rates of high-risk sexual behavior and HIV transmission in some individuals. Paper-12314549.
Modeling interactions of the PDE5 inhibitor sildenafil with the PDE4 active site may help explain inhibitor selectivity and provide useful information for the design of new inhibitors. Paper-10456191.
Many of the physiological responses to nitric oxide (NO) are mediated by cyclic 5'-guanosine monophosphate (cGMP), the intracellular levels of which are regulated by phosphodiesterase type 5 ( PDE5). Paper-12151357.
Cilostazol phosphorylated VASP at both Ser157 and Ser239 in a concentration-dependent manner, but EHNA (PDE2 inhibitor), dipyridamole and zaprinast ( PDE5 inhibitors) did not. Paper-10124797.
In conclusion, the concentrations of the PDE5 inhibitors required to evoke a 50% inhibition of the HERG current were well above reported therapeutic plasma concentrations of free and total compound. Paper-10605729.
Activation of platelet PKG promoted phosphorylation and activation of the PDE5 fraction tethered to the IP(3)R1- PKG complex, an effect not observed for the nontethered PDE5. Paper-12931001.
The SAR of a series of beta-carboline derived type 5 phosphodiesterase inhibitors has been explored and we have discovered compounds with excellent levels of PDE5 potency and selectivity over PDE6. Paper-10012470.
By real-time RT-PCR and Western blot analysis, we found that phosphodiesterase type 5 ( PDE5) mRNA and protein abundance was several fold higher in human male than in female reproductive tracts. Paper-10206935.
A cyclic nucleotide PDE5 inhibitor corrects defective mucin secretion in submandibular cells containing antibody directed against the cystic fibrosis transmembrane conductance regulator protein. Paper-2067491.
The development of newer and potentially more efficacious phosphodiesterase type 5 ( PDE5) inhibitors will serve to treat an even greater number of patients, allowing once daily and more convenient dosing. Paper-10417473.
The introduction of sildenafil citrate, the first oral phosphodiesterase type 5 ( PDE5) isoenzyme inhibitor, has helped to restore erectile function and improve overall health and quality of life. Paper-9324424.
PDE 4 and 5 appear to predominate in the prostate, PDE 1 and 4 are thought to influence detrusor smooth muscle function, and PDE 5 may be functionally important in the urethra and vasculature. Paper-12561931.
Although active sites of PDEs are apparently structurally similar, PDE4 is specifically inhibited by selective inhibitors such as rolipram, while PDE5 is preferentially blocked by sildenafil. Paper-10456191.
Sildenafil citrate, an inhibitor of the enzyme phosphodiesterase type 5 ( PDE5), is the most widely prescribed oral agent and has a very satisfactory efficacy-safety profile in all patient categories. Paper-10856438.
Vardenafil is a type 5 phosphodiesterase ( PDE5) inhibitor that potentiates the nitric oxide (NO)/cGMP pathway facilitating penile smooth muscle relaxation and improving penile erection in men. Paper-9895652.
Finally, experiments with calyculin A and okadaic acid suggest that PP1 phosphatase, the catalytic subunit of myosin phosphatase, can regulate PDE5 dephosphorylation. Paper-9155322.
Among these agents are 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors (statins), erythropoietin ( EPO), and phosphodiesterase type 5 ( PDE-5) inhibitors and nitric oxide (NO) donors. Paper-12249862.
The role of phosphodiesterase type 5 ( PDE5) in the mechanism of male erection has been well understood, and several drugs inhibiting this enzyme are being used for the treatment of erectile dysfunction (ED). Paper-11389129.
Phosphodiesterase type 5 ( PDE-5) inhibitors ( sildenafil, vardenafil and tadalafil) have been in widespread use for the safe and effective treatment of erectile dysfunction (ED) for nearly a decade. Paper-13568245.
Sildenafil, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 ( PDE5), is a well-tolerated and highly effective treatment for erectile dysfunction. Paper-1759730.
Aim: To examine the changes in the erectile function in diet-induced obese rats and investigate the oral efficacy of DA-8159, a new phosphodiesterase type 5 ( PDE5) inhibitor, on penile erection in obese rats. Paper-11810779.
Increasing intracellular levels of cGMP reduce the contractile status of VSM; on the contrary, type 5 cGMP-specific phosphodiesterase ( PDE5, codified by PDE5A gene) regulates cGMP levels through its clearance. Paper-10924541.
It inhibits PDE4 activity from human neutrophils with an IC(50) of 0.8 nM without affecting PDE1 (bovine brain), PDE2 (rat heart), and PDE3 and PDE5 (human platelets) even at 10,000-fold higher concentrations. Paper-8671946.
Comorbid LUTS and ED are treated with an alpha1- AR antagonist and a PDE-5; however, this combination must be used with caution because of vasodilatory adverse events associated with both classes of drugs. Paper-12355086.
Comorbid LUTS and ED are treated with an alpha1- AR antagonist and a PDE-5; however, this combination must be used with caution because of vasodilatory adverse events associated with both classes of drugs. Paper-12420689.
The ability of inhibitors selective for the type 5 phosphodiesterase isozyme ( PDE5) to act on the photoreceptor PDE isozyme (PDE6, the central effector enzyme for visual transduction) is poorly understood. Paper-1767818.
When SW982 cells were pretreated with sildenafil citrate (Viagra), a PDE5 specific inhibitor, sildenafil citrate significantly inhibited IL-1beta-induced NO synthesis and iNOS expressions. Paper-12858455.
Introduction. In recent years, recreational use of phosphodiesterase type 5 ( PDE5) inhibitors has become popular as a sexual enhancement aid among some men without erectile dysfunction (ED) and even among women. Paper-13068985.
Thus, the endosomal hyperacidification and excessive proinflammatory response in CF are in part due to deficiencies in NO- and cGMP- regulated processes and can be pharmacologically reversed using PDE5 inhibitors. Paper-11834737.
Phosphodiesterase type-5 ( PDE-5) inhibitors including sildenafil, vardenafil and tadalafil are a new class of vasoactive drugs that have been developed for treatment of erectile dysfunction in patients. Paper-10471902.
Sildenafil citrate, an orally active, selective inhibitor of phosphodiesterase type 5 ( PDE5), has demonstrated excellent efficacy and safety profiles in men with erectile dysfunction of various etiologies. Paper-1759731.
Viagra ( sildenafil citrate) improves penile erections in men with erectile dysfunction (ED) by selectively inhibiting cGMP-specific phosphodiesterase type 5 ( PDE5), which is present in all vascular tissue. Paper-9585053.
Sildenafil citrate (Revatio((R))), an inhibitor of phosphodiesterase type 5 ( PDE5), is approved for use in the US, Europe and other countries for the treatment of pulmonary arterial hypertension (PAH). Paper-12730245.
Activation of central mechanisms may open a window for phosphodiesterase type 5 inhibitors ( PDE5) to be effective; as a consequence, the combination of testosterone and a PDE5 inhibitor will restore sexual function. Paper-13665330.
The advent of oral phosphodiesterase type 5 ( PDE-5) inhibitors, however, has greatly enhanced erectile dysfunction treatment; patients have demonstrated high tolerability and success rates for improved erectile function. Paper-12356323.
Yet even with a portfolio of effective treatment modalities, such as phosphodiesterase type 5 ( PDE5) inhibitors, nonpharmacologic interventions should be considered as means to support and augment the effects of these agents. Paper-10230161.
This article provides an overview of the current laboratory and clinical evidence, as well as the cellular mechanisms by which the inhibitors of PDE3, PDE4 and PDE5 exert their beneficial effects on normal and ischemic hearts. Paper-13564601.
To evaluate the use of a long-term, continuous phosphodiesterase type 5 ( PDE5) inhibitor therapeutic regimen in controlling recurrent ischemic priapism and its feasibility in a clinical management program for the disorder. Paper-12314562.
RESULTS: As shown by RT-PCR and Northern blotting, PDE3A and PDE5A mRNAs exhibit a distinct distribution throughout the tissues examined but were 2-fold higher in cavernous tissue than in all other tissues investigated. Paper-8359474.
The mechanism of action of the phosphodiesterase type 5 ( PDE5) inhibitors (i.e., sildenafil, tadalafil, and vardenafil) involves inhibition of the PDE5 isoenzyme located in penile vascular smooth muscle cells. Paper-10295431.
The aim of the present study was to evaluate the effects of the phosphodiesterase type 5 ( PDE5) inhibitor, vardenafil, on inhibition of genital vascular responses (GVR) induced by SRI or SNRI administration in female rabbits. Paper-12314552.
Two novel PDE5 inhibitors, tadalafil (Lilly ICOS) and vardenafil (Bayer), have recently completed efficacy and safety clinical trials in 'general' and diabetic study populations and are now candidates for US FDA approval. Paper-9592159.
Increased cyclic guanosine monophosphate levels in these cells provoked by sodium nitroprusside and the PDE5 inhibitor zaprinast reduced the PGE2 synthesis, whereas 15-HETE and IL-8 formation were unchanged. Paper-1748705.
The selective PDE4 inhibitors Piclamilast and Roflumilast partially attenuated IL-1beta-induced NO production whereas selective inhibitors of PDE2 ( EHNA), PDE3 ( Motapizone) or PDE5 ( Sildenafil) were inactive. Paper-9372253.
D-22888 was a selective inhibitor of PDE4, exhibiting an IC50 against human neutrophil PDE4 of 0.15 microM, compared to IC 50 values of 4.4 microM and 1.1 microM for human platelet PDE3 and PDE5, respectively. Paper-1714538.
PKA and PKG, which mediate relaxation, act upstream to desensitize the receptors (VPAC(2) and NPR-C), inhibit adenylyl and guanylyl cyclase activities, and stimulate cAMP-specific PDE3 and PDE4 and cGMP-specific PDE5 activities. Paper-11365298.
The compounds inhibited some of the CYP450 enzymes and the human ether-a-go-go ( HERG) channel at much higher concentrations than that required to inhibit PDE5, thus, no cross inhibition would be expected at therapeutic doses. Paper-12209869.
By sequence homology in the catalytic domain, PDE9A is almost equidistant from all eight known mammalian PDE families but is most similar to PDE8A (34% amino acid identity) and least like PDE5A (28% amino acid identity). Paper-1469303.
At the N terminus PDE11A1 has a single GAF domain homologous to that found in other signaling molecules, including PDE2, PDE5, PDE6, and PDE10, which constitutes a potential allosteric binding site for cGMP or another small ligand. Paper-2174094.
Nonetheless ANP (10(-9) to 10(-6) M), in the presence of zaprinast, an inhibitor of phosphodiesterase 5 ( PDE5), increased fibroblast cyclic GMP levels 3-5 fold in a concentration-dependent manner (P < 0.05). Paper-1611755.
Vardenafil Improves Sexual Function and Treatment Satisfaction in Couples Affected by Erectile Dysfunction (ED): A Randomized, Double-Blind, Placebo-Controlled Trial in PDE5 Inhibitor-Na??ve Men with ED and Their Partners. Paper-12314557.
The results showing, for the first time, correction of the CFTR mucin secretion defect by a PDE5 inhibitor, which may involve cyclic GMP, will have a major impact in development of a rational drug treatment for cystic fibrosis. Paper-2067491.
We describe the high-resolution crystal structures of the catalytic domains of PDE4B, PDE4D, and PDE5A with ten different inhibitors, including the drug candidates cilomilast and roflumilast, for respiratory diseases. Paper-10613801.
However, glibenclamide significantly reduced the relaxation to both PGE1 and rolipram, but not those induced by the selective inhibitor of the type 5 cyclic guanosine monophosphate-specific phosphodiesterase ( PDE5). Paper-10318778.
Due to PDE-5 inhibition, the endogenous TGF-beta- activating protein TSP-1 and the TGF-beta-signalling protein p-smad-2/3 were decreased suggesting this as an antifibrotic mechanism of action of vardenafil in this model. Paper-13037524.
A liquid chromatography-electrospray ionisation-mass spectrometry (LC-ESI-MS) method was developed to screen for the presence of synthetic phosphodiesterase type 5 ( PDE-5) inhibitors including sildenafil, tadalafil and vardenafil. Paper-10953867.
Based on these findings, we elaborate a model in which PKG selectively activates PDE5 within a defined microdomain in platelets and propose that this mechanism allows spatial and temporal regulation of cGMP signaling in these cells. Paper-12931001.
Methods. Patient with a 5-year history of erectile dysfunction refractory to therapy with PDE5 inhibitors, injection therapy, and vacuum erection device therapy underwent placement of an Alpha-1 Mentor inflatable penile prosthesis. Paper-13075909.
Clinical evidence in men with erectile dysfunction (ED) shows that the phosphodiesterase type 5 ( PDE5) inhibitors sildenafil citrate, tadalafil, and vardenafil hydrochloride have favorable safety and efficacy profiles. Paper-10230162.
Newly developed sildenafil citrate (SC), a selective inhibitor of cyclic guanosine monophosphate (c-GMP) specific phosphodiesterase type 5 ( PDE 5) in the corpus cavernosum is used for the oral treatment of erectile dysfunction. Paper-10911724.
The replacement of the PDE6 H-loop into the PDE5 catalytic domain increases the catalytic rate and the K(m) value for cGMP hydrolysis, whereas the substitution of the M-loop produces catalytic PDE domains responsive to Pgamma. Paper-10566561.
The expression of key proteins of the NO pathway, such as the endothelial and neuronal nitric oxide synthase ( eNOS, nNOS), cGMP-degrading phosphodiesterase type 5 ( PDE5) and cGMP-binding protein kinase (cGK), has also been demonstrated. Paper-13089574.
Nitric oxide (NO) is the primary mediator of blood flow in female genital tissues and drugs that enhance the activity of nitric oxide, such as phosphodiesterase type-5 ( PDE-5) inhibitors, increase vaginal blood flow in anesthetized rats. Paper-13579880.
Protein expression of neural nitric oxide synthase (nNOS) and phosphodiesterase type 5 ( PDE 5) was reduced in penile tissue from orchiectomized animals and increased in testosterone-infused animals, as assessed by Western blot analyses. Paper-12148263.
The PDE5 inhibitory activities of these compounds, their selectivities against PDE1, PDE2, PDE3, PDE4 and PDE6, the preclinical pharmacokinetic assessments and the in vivo efficacy in increasing intracavernosal pressure are presented and discussed. Paper-10541964.
CONCLUSIONS: Very high expression levels of PDE3A and PDE5A in human cavernous tissue underscore the physiological importance of these enzymes for the regulation of penile erection, emphasizing their therapeutical and pharmacological relevance. Paper-8359474.
In the present study, we investigated the effects of tadalafil (Cialis), a long acting PDE5 inhibitor, on brain cGMP levels, neurogenesis, angiogenesis, and neurological function during stroke recovery in a rat model of embolic stroke. Paper-12344611.
Sildenafil, which selectively inhibits phosphodiesterase type 5 ( PDE5) found predominantly in the corpora cavernosa of the penis, effectively blocks the degradation of cGMP and enhances erectile function in men with erectile dysfunction. Paper-1759729.
The PDE type-3, -4, and -5 (PDE3, PDE4, PDE5) are localized to specific regions of the cardiomyocyte, such as the sarcoplasmic reticulum and Z-disc, where they are likely to influence cAMP/cGMP signaling to the end effectors of contractility. Paper-13564601.
OBJECTIVE: This study was undertaken to determine whether Viagra (Pfizer, New York, NY), a type 5 phosphodiesterase ( PDE-5) inhibitor, increases baseline coronary and uterine blood flow or potentiates estrogen-induced increases in blood flow. Paper-10288196.
Of the currently available treatment options for ED, the most commonly prescribed therapies are oral PDE5 inhibitors, which include sildenafil citrate (Viagra, Pfizer Inc), tadalafil (Cialis, Lilly ICOS), and vardenafil ( Levitra, Bayer). Paper-11393954.
PDE9A is insensitive (up to 100 microM) to a variety of PDE inhibitors including rolipram, vinpocetine, SKF-94120, dipyridamole, and 3-isobutyl-1-methyl-xanthine but is inhibited ( IC50 = 35 microM) by zaprinast, a PDE5 inhibitor. Paper-1469303.
MAIN OUTCOME MEASURES: To measure the inhibition exerted by PDE inhibitors vinpocetine (PDE1-inhibitor), rolipram ( PDE4-inhibitor), sildenafil, and vardenafil ( PDE5-inhibitors) on the phasic contractile response of isolated SV tissue. Paper-13487205.
OBJECTIVE: This study evaluated whether sildenafil citrate, an oral treatment for erectile dysfunction and a selective inhibitor of phosphodiesterase type 5 ( PDE5) with modest vasodilating properties, affects cardiac contractility in vitro. Paper-10177023.
Sildenafil citrate, an oral therapy for erectile dysfunction, is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 ( PDE5), the predominant isozyme metabolizing cGMP in the corpus cavernosum. Paper-1769919.
OBJECTIVES: We sought to assess the effect of sildenafil, a highly-specific type 5 phosphodiesterase ( PDE5) inhibitor, on platelet-mediated cyclic coronary flow reductions occurring in a canine model of coronary thrombosis despite aspirin therapy. Paper-11370516.
Thus cGMP is a key second messenger and targeting this pathway by increasing intracellular cGMP levels is a very successful approach in pharmacology as shown for nitrates, PDE5 inhibitors and more recently for stimulators of the guanylate cyclase. Paper-13497206.
In our efforts to minimize the side effects associated with low selectivity against the other PDE isozymes, a novel class of 2-phenylquinazolin-4(3H)-one derivatives were designed and prepared as potent PDE5 inhibitors with high selectivity against PDE6. Paper-13747922.
Together, the data suggest that phosphorylation and activation of PDE5 by PKG I and its subsequent dephosphorylation by myosin phosphatase may be key steps in the regulation of relaxation/contraction cycles of smooth muscle. Paper-9155322.
Furthermore, indications of side effects of specific inhibitors in certain tissues as well as of a possible relation between the level of PDE3A and PDE5A gene expression and erectile dysfunction should have been deduced from the results obtained. Paper-8359474.
AIM: Vardenafil is a selective and highly potent phosphodiesterase type 5 ( PDE5) inhibitor for the treatment of erectile dysfunction (ED), with improved selectivity for PDE5 and demonstrated efficacy for improving sexual function in men with ED. Paper-10535672.
In a retrospective cohort study using a large, aggregated health claims database, the costs associated with switching from sildenafil to another phosphodiesterase type 5 ( PDE-5) inhibitor were compared with those for patients refilling sildenafil. Paper-12339906.
As it has been demonstrated that androgens control PDE5 expression and that PDE5 inhibitors need an optimal androgenic milieu to act perfectly on erection, the expression of AR protein in rat corpus cavernosum cells was then tested by Western blot. Paper-13615029.
To validate the microarray data, quantitative real-time PCR of six candidate target genes was conducted, whereby it was found that three genes were up-regulated (AKAPA8L, PMPCB and PDE5A) and three were down-regulated ( PITPNA, DUS2L and RIC8A). Paper-12788303.
Sildenafil citrate (Viagra) is a potent orally active cGMP-specific phosphodiesterase type 5 ( PDE5) inhibitor that is effective as a peripheral conditioner in the treatment of male erectile dysfunction (ED) of organic, psychogenic or mixed aetiology. Paper-9907007.
Hypergravity also stimulated cGMP transport in the presence of 1 microM trequinsin, an inhibitor of cGMP-binding PDE ( PDE5) and of transport by multidrug resistance proteins MRP4/5, whereas 50 microM trequinsin partially inhibited cGMP transport. Paper-10941339.
METHODS: AR and PDE5 expression was tested on ribonucleic acids (RNAs) and proteins extracted from the whole penis or from primary cultures of smooth muscle cells obtained from the corpora cavernosa of 3- (rCC3), 20- (rCC20), and 60- (rCC60) day-old rats. Paper-13615029.
Sildenafil, a type 5 phosphodiesterase isoenzyme ( PDE5) inhibitor with a short half-life, increases brain cyclic guanosine monophosphate ( cGMP) levels and improves neurological functional recovery when administered after stroke. Paper-12344611.
1. Chronic hypoxic treatment of rats (to induce pulmonary hypertension, PHT) for 14 days increased cGMP-inhibited cAMP specific phosphodiesterase ( PDE3) and cGMP binding cGMP specific phosphodiesterase ( PDE5) activities in pulmonary arteries. Paper-9650726.
Although three-dimensional x-ray crystal structures of PDE4 and PDE5 have been reported, it is uncertain whether a critical, second bridging ligand (BL2) in the active site is H2O or HO- because hydrogen atoms cannot be determined by x-ray diffraction. Paper-12178920.
A number of laboratory and human studies have shown the combination of testosterone and other ED treatments, such as phosphodiesterase type 5 ( PDE5) inhibitors, to be beneficial in patients with ED and hypogonadism, who fail PDE5 inhibitor therapy alone. Paper-12201109.
In an effort to minimize side effects associated with low selectivity against PDE isozymes, we have successfully identified a series of 6,7,8-substituted quinzaolines as potent inhibitors of PDE5 with high level of isozyme selectivity, especially against PDE6 and PDE11. Paper-13092651.
Erythropoietin-treated patients demonstrated significantly higher postoperative International Index of Erectile Function-5 questionnaire scores than control group patients at 3, 6, and 12 months postoperatively with or without use of PDE5 inhibitors (P < 0.05). Paper-13094160.
Considering the role of the vagina in the female sexual response and the anatomic connection between the clitoris and the anterosuperior vaginal wall, our aim was to study the distribution of type 5 phosphodiesterase ( PDE5) in the anterosuperior wall of the human vagina. Paper-9505068.
A selective cyclic nucleotide PDE5 inhibitor corrected the defective mucin secretion response to the beta-agonist isoproterenol in submandibular acinar cells inhibited by antibody directed against the cystic fibrosis transmembrane conductance regulator. Paper-2067491.
BACKGROUND: Sildenafil, a treatment for erectile dysfunction, is a specific phosphodiesterase type 5 ( PDE 5) inhibitor that enhances nitric oxide (NO)-mediated vasodilation in the corpus cavernosum by inhibiting cyclic guanosine monophosphate breakdown. Paper-8944604.
Incubation of primary cultures of HCC smooth muscle cells with either the NO donor sodium nitroprusside ( SNP, 10 microM) or the phosphodiesterase type 5 ( PDE 5) inhibitor sildenafil (50 nM) produced little or no changes in the intracellular cGMP levels. Paper-8549134.
INTRODUCTION AND OBJECTIVES: To systematically analyze and review the available evidence about the potential role of chronic administration of phosphodiesterase type 5 ( PDE-5) inhibitors for the cure of erectile dysfunction (ED) based on clinical and basic science data. Paper-12106666.
To test if this type of regulation is important in the intact cell, we have generated phospho- PDE5-specific antisera and have utilized isolated smooth muscle cells from mice having a disruption in the PKG I gene as well as cells from normal human smooth muscle. Paper-9155322.
Inhibition of MEK by PD98059 and p38 with SB203580 blocked sildenafil-induced proliferation and migration, respectively, suggesting that these MAPK members are downstream of PDE5 and mediate the angiogenic effects of sildenafil. Paper-12451904.
INTRODUCTION: The International Index of Erectile Function (IIEF), Sexual Encounter Profile (SEP), and Erectile Dysfunction Inventory of Treatment Satisfaction (EDITS) assess efficacy of phosphodiesterase type 5 ( PDE5) inhibitor treatment of erectile dysfunction (ED). Paper-13590341.
Objective: The ENDURANCE study evaluated the efficacy of vardenafil, a phosphodiesterase type 5 ( PDE5) inhibitor, in men with erectile dysfunction (ED), by measuring the duration of erection leading to successful intercourse using a stopwatch as the assessment instrument. Paper-13566301.
In other forms of pulmonary vascular disease with increased PVR, an elevated activity of a phosphodiesterase type 5 ( PDE-5), responsible for the degradation of cyclic guanidine monophosphate (cGMP), the second messenger of endothelially produced NO, has been demonstrated. Paper-9836279.
AIM: The aim of this article was to study the expression pattern of androgen receptor ( AR) and the major cyclic guanosine monophosphate-hydrolyzing enzyme present in the corpora cavernosa, type 5 phosphodiesterase ( PDE5), in the rat penis during development. Paper-13615029.
Introduction. Data from head-to-head clinical trials of phosphodiesterase type 5 ( PDE5) inhibitors are scarce, making it difficult for clinicians to differentiate among these agents to select the most appropriate treatment for their patients with erectile dysfunction (ED). Paper-12314558.
The effects of rolipram (inhibiting a cAMP specific PDE ( PDE4), milrinone (inhibiting a cGMP inhibited PDE (PDE3)) and zaprinast (inhibiting a cGMP specific PDE ( PDE5)) were investigated in in vitro preparations from the rabbit maxillary sinus and trachea. Paper-1704816.
This review focuses on the development of PDE3 inhibitors for congestive heart failure, PDE4 inhibitors for inflammatory airways disease and most successfully, PDE5 inhibitors for erectile dysfunctionBritish Journal of Pharmacology (2006) 147, S252-S257. doi:10.1038/sj.bjp.0706495. Paper-11336970.
We applied SSM to the FlexX scoring function, that is, F-Score, with five different target proteins: thymidine kinase (TK), estrogen receptor ( ER), acetylcholine esterase (AChE), phosphodiesterase 5 ( PDE5), and peroxisome proliferator-activated receptor gamma ( PPARgamma). Paper-12505691.
Other published reports indicated that phosphodiesterase type 5 ( PDE-5), NO synthase, and guanylyl cyclase are present at highest activities in areas of the brain responsible for behavior, sexual drive, and emotion, and that NO modulates aggression and sexual behavior in male mice. Paper-9561022.
Finally, cGK-dependent phosphorylation of substrates such as vasodilator stimulated phosphoprotein (VASP) and phosphodiesterase 5 ( PDE 5) is described as a useful monitor of cGK presence and activity associated with physiological functions or dysfunctions of signaling pathways. Paper-11504225.
The PDE6 catalytic subunits resemble PDE5 in amino-acid sequence as well as in three-dimensional structure of the catalytic dimer; preference for cGMP over cyclic adenosine monophosphate (cAMP) as a substrate; and the ability to bind cGMP at the regulatory GAF domains. Paper-10456192.
The effects of the isoform-selective inhibitors, 8-methoxymethyl-IBMX (PDE 1 inhibitor), siguazodan (PDE3 inhibitor), rolipram ( PDE4 inhibitor), denbufylline ( PDE4 inhibitor), Org 30029 (mixed PDE3 and 4 inhibitor) and zaprinast ( PDE5 inhibitor), were studied. Paper-10536607.
Results from the two experimental procedures were largely in good agreement and indicated that PDE5A1 and A2 mRNA were expressed in a tissue-specific manner with PDE5A2 being the dominant isoform.International Journal of Impotence Research (2003) 15, 129-136. doi:10.1038/sj.ijir.3900983 Paper-9892189.
The FINDER study aimed to evaluate the efficacy and tolerability of the phosphodiesterase type-5 ( PDE5) inhibitor, vardenafil, in a broad population of PDE5-na??ve men with ED of different etiologies and severity and included their partners' assessments of treatment with vardenafil. Paper-12314557.
METHODS: Total ribonucleic acid was isolated from different human tissues (urogenital tract, gastrointestinal tract, cardiovascular system and central nervous system) and subjected to RTPCR analysis and Northern blotting using primers and probes specific for PDE3A and PDE5A. Paper-8359474.
OBJECTIVES: To review molecular mechanisms underlying androgen action upon its receptor and phosphodiesterase type 5 ( PDE5) expression and regulation by testosterone in cavernous tissue and their clinical implication in the treatment of ED refractory to PDE5 inhibitors (PDE5-Is). Paper-12260556.
3. The PDE1/ PDE5 inhibitor zaprinast inhibited both cyclic AMP and cyclic GMP PDE activity in both pellet and supernatant fractions of cell homogenates by a maximum of around 25% (IC(50) 1 - 5 microM), while rolipram ( PDE4 selective) inhibited only cyclic AMP hydrolysis. Paper-2197900.
CONCLUSION AND IMPLICATIONS: LPS caused a selective hypocontractility of rat aorta to ET-1 mediated mainly through NO-independent sGC activation, whereas in the pulmonary artery, the effect of sGC activation was reduced by a decreased protein expression of sGC(beta1) together with increased PDE5 activity. Paper-13484085.
Therefore, inhibition of type 5 phosphodiesterase ( PDE5), the principle enzyme responsible for cyclic guanosine monophosphate catabolism in the lungs and skeletal muscle, has been targeted in an effort to counteract vasoconstriction that contributes to increased right and LV afterload in HF. Paper-12180965.
The structure-activity analysis suggests that a small hydrophobic pocket and the H-loop of PDE5 are important for the inhibitor affinity, in addition to two common elements for binding of almost all the PDE inhibitors: the stack against the phenylalanine and the hydrogen bond with the invariant glutamine. Paper-12784897.
The availability of selective inhibitors of the cyclic guanosine monophosphate (cGMP)-specific type 5 phosphodiesterase ( PDE5) has created increasing interest in unlocking the therapeutic potential of PDE5 inhibition in cardiovascular diseases that are marked by dysfunction of nitric oxide (NO)-cGMP signaling. Paper-10646313.
L-arginine (L-arg), the precursor of NO, and selective phosphodiesterase type 5 ( PDE-5) inhibitors that increase levels of intracellular cGMP may complementarily enhance VEGF synthesis in corpus cavernosal smooth muscle cells (CCSMCs), and may consequently restore impaired endothelial function. Paper-13083315.
Vardenafil ( Levitra) is a potent and highly selective oral phosphodiesterase type 5 ( PDE5) inhibitor.Vardenafil improved erectile function in men with mild to severe erectile dysfunction (ED) of varying aetiology in two randomised, double-blind, multicentre, fixed-dose studies of 12 or 26 weeks' duration. Paper-10240334.
Overexpression of dominant-negative Rac(1) or addition of iloprost, DETA-NONOate or Y27632 completely blocked both superoxide release and PDE5 protein expression and activity.Conclusions and implications:These data demonstrate that superoxide derived from NOX upregulates the expression of PDE5 in human VSMCs. Paper-13087781.
From this result, we noticed that PDE5 activity is required for IL-1?- induced NO synthesis and iNOS expressions in human synovial sarcoma cells, and sildenafil citrate may be able to suppress an inflammatory reaction of synovium through inhibition of NO synthesis and iNOS expression by cytokines. Paper-12858455.
This study aimed to use a cell extraction procedure compatible with routine forensic sampling methods, and to investigate the expression of cytokeratin ( CK), estrogen receptor-alpha (ERalpha), and phosphodiesterase 5 ( PDE5) in order to distinguish between skin, buccal, vaginal, and external penile epithelial cells. Paper-12254881.
The effects of iloprost, DETA-NONOate and the Rho-kinase inhibitor, Y27632, on PDE5 and NOX-1 expression were also studied.Key results:Following 16 h incubation, U46619 and X-XO promoted the expression of PDE5 and NOX-1, an effect blocked by SOD or apocynin when co-incubated over the same time course. Paper-13087781.
We observed a negative correlation of TPSA with activity data for anticancer alkaloids, MT1 and MT2 agonists, MAO-B and tumor necrosis factor-alpha inhibitors and a positive correlation with inhibitory activity data for telomerase, PDE-5, GSK-3, DNA-PK, aromatase, malaria, trypanosomatids and CB2 agonists. Paper-13579007.
Contraction was induced on isolated strips of corporal smooth muscle by norepinephrine; then relaxation was assessed with the administration of two agents: selective phosphodiesterase type 5 ( PDE5) inhibitor ( sildenafil citrate) and S-nitroso-N-acetylpenicillamine (SNAP), an NO-donor, and combination of both agents. Paper-8757219.
In this paper, we report the case of a young man with homozygote genotype mutated with 5- methylenetetrahydrofolate reductase ( MTHFR) thermolabile variant who, in the absence of relational stress, developed an erectile dysfunction (ED) refractory to the vasoactive type-V phosphodiesterase ( PDE5) inhibitor therapy. Paper-10952065.
To examine whether endogenous PDE5 activity suppresses endothelial cell angiogenic potential, small interfering RNA (siRNA) constructs were stably expressed in pulmonary artery endothelial cells. siRNA selectively decreased PDE5 expression and increased basal and ANP-stimulated cGMP concentrations in these conduit cells. Paper-13589981.
The results indicate that the substrate-binding site of PDE5 contains positive elements for accommodating cGMP, as well as negative elements that discriminate against binding of cAMP, and that the cGMP/cAMP selectivity of PDE5 can be shifted 106-fold by substituting four residues of PDE5 with the residues in the corresponding positions of PDE4. Paper-1388460.
2. PDE3A/B gene transcript levels were increased in the main, first, intrapulmonary and resistance pulmonary arteries by chronic hypoxia. mRNA transcript and protein levels of PDE5A2 in the main and first branch pulmonary arteries were also increased by chronic hypoxia, with no effect on PDE5A1/A2 in the intra-pulmonary and resistance vessels. Paper-9650726.
These synonyms are used for gene PDE5A (phosphodiesterase 5A, cGMP-specific): PDE5A1, PDE5, CN5A, cGMP-specific 3',5'-cyclic phosphodiesterase, cGMP-binding cGMP-specific phosphodiesterase, CGB-PDE.
These accession numbers are used for gene PDE5A: O75887 (UNIPROT__AC), BAA28945 (NCBI_GENBANK__AC), AAI26234 (NCBI_GENBANK__AC), A8K2C4 (UNIPROT__AC).
PDE5A is a homologue of PDE5A (phosphodiesterase 5A, cGMP-specific) from Bos taurus.
PDE5A is a homologue of PDE5A (phosphodiesterase 5A, cGMP-specific) from Pan troglodytes.
PDE5A is a homologue of PDE5A (phosphodiesterase 5A, cGMP-specific) from Gallus gallus.
PDE5A is a homologue of PDE5A (phosphodiesterase 5A, cGMP-specific) from Canis lupus familiaris.
PDE5A is a homologue of Pde5a (phosphodiesterase 5A, cGMP-specific) from Mus musculus.
PDE5A is a homologue of Pde5a (phosphodiesterase 5A, cGMP-specific) from Rattus norvegicus.
PDE5A is a homologue of pde5a (phosphodiesterase 5A, cGMP-specific) from Danio rerio.
PDE5A is a homologue of Pde11 (Phosphodiesterase 11) from Drosophila melanogaster.
PDE5A is a homologue of AgaP_AGAP008646 (AGAP008646-PA) from Anopheles gambiae str. PEST.
Important links !
iHOP - Information Hyperlinked over Proteins .
Concept & Implementation by Robert Hoffmann.