| Name | phosphodiesterase |
|---|---|
| Synonyms | CAMP specific phosphodiesterase variant PDE4A 10; CAMP specific phosphodiesterase variant TM3; CAMP specific phosphodiesterase; Cyclic AMP phosphodiesterase PDE4A11; Cyclic AMP specific phosphodiesterase HSPDE4A10; DPDE 2; DPDE2; PDE 4… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 11343689 | Asomoza-Espinosa R, Alonso-Lopez R, Mixcoatl-Zecuatl T, Aguirre-Banuelos P, Torres-Lopez JE, Granados-Soto V: increases diclofenac antinociception in the formalin test. Eur J Pharmacol. 2001 Apr 27;418(3):195-200. In contrast, 1-[4-ethoxy-3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo [3,4-d] pyrimidin-5-yl) phenylsulfonyl]-4-methyl piperazine an inhibitor of phosphodiesterase 5) produced significant antinociception, only during the second phase of the formalin test. |
83(1,1,1,3) | Details |
| 17640490 | Yoo HH, Kim NS, Im GJ, Kim DH: Pharmacokinetics and tissue distribution of a novel PDE5 inhibitor, SK-3530, in rats. Acta Pharmacol Sin. 2007 Aug;28(8):1247-53. AIM: To investigate the pharmacokinetic profile and tissue distribution of a novel phosphodiesterase type 5 inhibitor, 5-ethyl-2-{5-[4-(2--ethyl)-piperazine-1-sulfonyl]-2-propoxy-phenyl} -7-propyl-3,5-dihydro-pyrrolo (3,2-d) pyrimidin-4-one (SK-3530), in rats after administration of the (14) C-labeled compound. |
81(1,1,1,1) | Details |
| 17688073 | Schneider F, Mattern-Dogru E, Hillgenberg M, Alken RG: Changed phosphodiesterase selectivity and enhanced in vitro efficacy by selective deuteration of Arzneimittelforschung. 2007;57(6):293-8. In order to explore whether selective deuteration of affects selectivity and efficacy of the drug, the inhibitory activity of (1-[4-ethoxy-3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo [4,3-d] pyri midin-5-yl) phenyl-sulfonyl] -4-methylpiperazine CAS 139755-83-2) and three deuterated derivatives, D8-piperazine- (BDD-10402), D3-methyl-D8-piperazine- (BDD-10403) and D5-ethoxy- (BDD-10406) against phosphodiesterases 1-6 was compared. |
3(0,0,0,3) | Details |
| 17689219 | Shin BS, Hu SK, Kim J, Oh JG, Youn WN, Lee B, Um KA, Kim DK, Lee JY, Yoo SD: Development of LC/MS/MS assay for the determination of 5-ethyl-2-{5-[4-(2-hydroxyethyl) piperazine-1-sulfonyl]-2-propoxyphenyl}-7- propyl-3,5-dihydropyrrolo [3,2-d] pyrimidin-4-one (SK3530) in human plasma: application to a clinical pharmacokinetic study. J Pharm Biomed Anal. 2007 Sep 21;45(1):176-84. Epub 2007 Jun 30. 5-Ethyl-2-{5-[4-(2-hydroxyethyl) piperazine-1-sulfonyl]-2-propoxyphenyl}-7- propyl-3,5-dihydropyrrolo [3,2-d] pyrimidin-4-one (SK3530) is a new phosphodiesterase type-5 inhibitor currently undergoing a Phase III investigation for the treatment of male erectile dysfunction. |
31(0,1,1,1) | Details |
| 19635671 | Abdulkadir Coban T, Beydemir S, Gucin I, Ekinci D, Innocenti A, Vullo D, Supuran CT: Sildenafil is a strong activator of mammalian carbonic anhydrase isoforms I-XIV. Bioorg Med Chem. 2009 Aug 15;17(16):5791-5. Epub 2009 Jul 17. a phosphodiesterase-5 (PDE5) inhibitor widely used for the treatment of erectile dysfunction was investigated for its interaction with the zinc-enzyme carbonic anhydrase (CA, EC 4.2.1.1), as it has in its molecule a piperazine moiety also found in some CA activators (CAAs). |
31(0,1,1,1) | Details |
| 15452190 | Gardiner SM, March JE, Kemp PA, Ballard SA, Hawkeswood E, Hughes B, Bennett T: Hemodynamic effects of phosphodiesterase 5 and angiotensin-converting enzyme inhibition alone or in combination in conscious SHR. J Pharmacol Exp Ther. 2005 Jan;312(1):265-71. Epub 2004 Sep 27. |
2(0,0,0,2) | Details |
| 16759100 | Allerton CM, Barber CG, Beaumont KC, Brown DG, Cole SM, Ellis D, Lane CA, Maw GN, Mount NM, Rawson DJ, Robinson CM, Street SD, Summerhill NW: A novel series of potent and selective PDE5 inhibitors with potential for high and dose-independent oral bioavailability. J Med Chem. 2006 Jun 15;49(12):3581-94. (5-[2-ethoxy-5-(4-methyl-1-piperazinylsulfonyl) phenyl]-1-methyl-3-n-propyl -1,6-dihydro-7H-pyrazolo [4,3-d] pyrimidin-7-one), a potent and selective phosphodiesterase type 5 (PDE5) inhibitor, provided the first oral treatment for male erectile dysfunction. This goal was achieved through identification of a lower clearance series with a high absorption profile, by replacing the 5'-piperazine sulfonamide in the template with a 5'- |
1(0,0,0,1) | Details |
| 15312980 | Corbin JD, Beasley A, Blount MA, Francis SH: Vardenafil: structural basis for higher potency over in inhibiting -specific phosphodiesterase-5 (PDE5). Neurochem Int. 2004 Nov;45(6):859-63. They also differ in the substituent (ethyl/methyl) of a piperazine side chain. |
2(0,0,0,2) | Details |
| 19427155 | Gratz SR, Zeller M, Mincey DW, Flurer CL: Structural characterization of sulfoaildenafil, an analog of . J Pharm Biomed Anal. 2009 Sep 8;50(2):228-31. Epub 2009 Apr 10. Phosphodiesterase type 5 (PDE-5) inhibitors represent a class of drugs used primarily in the treatment of erectile dysfunction. When compared to sulfoaildenafil contains a substitution for the atom in the pyrazolopyrimidine portion of the molecule, and a 3,5-dimethyl substitution on the piperazine ring, rather than the 4-methyl moiety. |
1(0,0,0,1) | Details |
| 20013111 | Lipina T, Roder J: A new model of the disrupted latent inhibition in C57BL/6J mice after treatment. Psychopharmacology. 2010 Feb;208(3):487-98. Epub 2009 Dec 16. OBJECTIVES: The objectives of this study were as follows: to probe whether disrupts LI; to compare its efficacy to the effects of GBR12783 (specific DA uptake inhibitor) and to amphetamine (DA releaser); to test if antipsychotics would reverse LI deficits induced by GBR12783, and amphetamine; and to probe if rolipram (phosphodiesterase-4 inhibitor), which increases cyclic AMP (cAMP) similarly to antipsychotics, effectively corrects drug-induced LI deficits. |
1(0,0,0,1) | Details |
| 15680943 | Zsombok A, Schrofner S, Hermann A, Kerschbaum HH: A -dependent cascade enhances an L-type-like Ca2+ current in identified snail neurons. Brain Res. 2005 Jan 25;1032(1-2):70-6. Blockade of protein kinase activity with 1-[5-isoquinolinesulfonyl]-2 methyl piperazine (H 7), a nonselective protein kinase inhibitor, or Rp-8-pCPT- a selective protein kinase G (PKG) inhibitor, decreased, whereas Rp-cAMP, a selective protein kinase A (PKA) inhibitor, increased the Ba (2+) current upon application of analogues or SNP. When neurons were exposed to the nonselective phosphodiesterase (PDE) inhibitor 3-isobutyl-1-methylxanthine (IBMX), analogues induced a persistent increase of the Ba (2+) current, whereas SNP induced a biphasic response. |
1(0,0,0,1) | Details |