Zembowicz A, Dudek R D, Radziszewski W, Swierkosz T A, Trybulec M, Gryglewski R J
Department of Pharmacology, N. Copernicus Academy of Medicine, Cracow, Poland.
Pol J Pharmacol Pharm. 1990 May-Jun;42(3):275-81.
Rabbit aortic strips were arranged in a Vane's cascade and superfused with Krebs buffer which contained phenylephrine hydrochloride (100 nM) and indomethacin (5 microM). EC50 (nM) for vasorelaxant action of NO-donors on rabbit aortic strips were as follows: glyceryl trinitrate--64.0, sodium nitroprusside--124.5, S-nitroso-N-acetylpenicillamine--305.7, SIN-1 (metabolite of molsidomine)--510.0. On the other hand IC50 (microM) for antiaggregatory action of NO-donors in human platelet rich plasma aggregated with threshold concentrations of collagen (0.5-1 micrograms/ml) were as follows: S-nitroso-N-acetylpenicillamine--7,1, SIN-1--13.6, sodium nitroprusside--28.0. Glyceryl trinitrate did not inhibit platelet aggregation at concentrations up to 1 mM. Sodium nitroprusside was more specific (EC50/IC50 = 0.0043) than SNAP and SIN-1 (EC50/IC50 = 0.043 and 0.037, respectively) as a vasorelaxant than as a platelet suppressant. Thus relative potencies of four c-GMP stimulants as vasorelaxants and platelet-suppressants differed considerably and several possible explanations for these differences were put forward.
将兔主动脉条按Vane氏串联法排列，并用人造脑脊液进行灌流，该人造脑脊液含有盐酸去氧肾上腺素（100 nM）和消炎痛（5 μM）。一氧化氮供体对兔主动脉条的血管舒张作用的半数有效浓度（EC50，nM）如下：硝酸甘油——64.0，硝普钠——124.5，S-亚硝基-N-乙酰青霉胺——305.7，SIN-1（吗多明的代谢产物）——510.0。另一方面，在富含人血小板的血浆中，一氧化氮供体对与阈值浓度的胶原蛋白（0.5 - 1微克/毫升）聚集的血小板的抗聚集作用的半数抑制浓度（IC50，μM）如下：S-亚硝基-N-乙酰青霉胺——7.1，SIN-1——13.6，硝普钠——28.0。硝酸甘油在浓度高达1 mM时不抑制血小板聚集。作为血管舒张剂，硝普钠比SNAP和SIN-1（EC50/IC50分别为0.043和0.037）更具特异性（EC50/IC50 = 0.0043），作为血小板抑制剂的作用较弱。因此，四种c-GMP刺激剂作为血管舒张剂和血小板抑制剂的相对效力有很大差异，并针对这些差异提出了几种可能的解释。
