| Name | PDE5 |
|---|---|
| Synonyms | CGB PDE; CGMP specific phosphodiesterase PDE5A1; CGMP specific phosphodiesterase PDE5A2; CGMP specific phosphodiesterase type 5A; CN5A; PDE 5; PDE5; PDE5A… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 11569531 | Walker DK, Beaumont KC, Comby P, Evans KM, Gedge JI, Halliday RC, Roffey SJ, Wright PA: Pharmacokinetics and metabolism of a selective PDE5 inhibitor (UK-343,664) in rat and dog. Xenobiotica. 2001 Aug-Sep;31(8-9):651-64. The major primary pathways in dog involved piperazine N-deethylation and loss of a two carbon fragment from the piperazine ring (N,N'-de-ethylation). |
2(0,0,0,2) | 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. |
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. It is concluded that the methyl/ethyl appended group on the piperazine moiety plays very little role in the difference in potency between and vardenafil for inhibiting PDE5, whereas the differences in the ring systems play a critical role in higher potency of vardenafil over |
87(1,1,1,7) | 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 |
| 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. 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'- |
3(0,0,0,3) | 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. The regional hemodynamic responses to continuous 4-day infusion of UK-357,903 [1-ethyl-4-{3-[3-ethyl-6,7-dihydro-7-oxo-2-(2-pyridylmethyl)-2H-pyrazolo [4 ,3-d] pyrimidin-5-yl]-2-(2-methoxyethoxy)-5-pyridylsulphonyl}piperazine] (266 microg kg (-1) h (-1)) alone and in combination with a low dose of enalapril (10 microg kg (-1) h (-1)) were measured in conscious spontaneously hypertensive rats to test the hypothesis that the renin-angiotensin system may influence the cardiovascular consequences of inhibition of phosphodiesterase 5 (PDE5) by UK-357,903 or vice versa. |
2(0,0,0,2) | Details |