Karrenbrock B, Heim J M, Gerzer R
Medizinische Klinik Innenstadt der Universität München.
Klin Wochenschr. 1990 Feb 15;68(4):213-7. doi: 10.1007/BF01662718.
To find out whether 3-morpholino-sydnonimine (SIN 1), the active metabolite of molsidomine, exerts its antiaggregatory effects not only in vitro but also in vivo, we tested ex vivo aggregation before and after intravenous application of molsidomine in healthy volunteers. We also measured plasma levels of guanosine 3':5'-cyclic monophosphate (cyclic GMP) as SIN 1, the bioactive metabolite of molsidomine, becomes effective via activation of soluble guanylate cyclase. In eight out of ten subjects molsidomine had an inhibitory effect on platelet aggregation and a higher threshold concentration of platelet-activating factor was required after molsidomine application to induce irreversible aggregation. Despite the effect on platelets, plasma cyclic GMP levels did not increase. These results suggest that the nitric oxide-containing SIN 1 inhibits platelet aggregation not only in vitro but also in vivo and that this property can be a beneficial effect in antianginal therapy.
为了弄清楚吗多明的活性代谢产物3-吗啉代西多明（SIN 1）是否不仅在体外而且在体内都发挥其抗聚集作用，我们在健康志愿者静脉注射吗多明前后测试了体外血小板聚集情况。我们还测量了血浆中鸟苷3':5'-环磷酸（环磷酸鸟苷）的水平，因为吗多明的生物活性代谢产物SIN 1通过激活可溶性鸟苷酸环化酶发挥作用。在十名受试者中有八名，吗多明对血小板聚集有抑制作用，应用吗多明后诱导不可逆聚集所需的血小板激活因子阈值浓度更高。尽管对血小板有影响，但血浆环磷酸鸟苷水平并未升高。这些结果表明，含一氧化氮的SIN 1不仅在体外而且在体内都能抑制血小板聚集，并且这种特性在抗心绞痛治疗中可能是一种有益的作用。
