158001-76-4
158001-76-4 结构式
基本信息
4H-Pyrazolo[3,4-d]pyrimidin-4-one, 1-cyclopentyl-1,5-dihydro-3-methyl-6-(4-pyridinyl)-
常见问题列表
Ki: 170 nM (PDE V)
Win 58237 is a competitive inhibitor of cGMP PDE V from canine aorta, with a K i value of 170 nM. Win 58237 is a potent inhibitor of PDE V isolated from vascular tissue with an IC 50 value of 240 nM. It is a relatively less potent inhibitor of calmodulin-sensitive PDE I and cGMP-inhibitable cyclic AMP PDE III; but does inhibit cyclic AMP PDE IV with an IC 50 value of approximately 300 nM. Win 58237 possesses vasorelaxant activity in the presence of an intact endothelium or nitric oxide.
Win 58237 (0.3-3.0 mg/kg i.v.) decreases mean arterial pressure in conscious spontaneously hypertensive rats with an associated increase in vascular (aortic) cGMP content in vivo. Win 58237 (10 mg/kg i.v.) increases plasma cGMP levels, from basal levels of 6.7 ± 1.0 to 31.4 ± 3.5 fmol/μL.