一种新型血小板5-羟色胺受体拮抗剂。
A new antagonist of the 5-hydroxytryptamine receptor of blood platelets.
作者信息
Laubscher A, Pletscher A, Mester L, Mester M
出版信息
Arzneimittelforschung. 1982;32(6):686-8.
The newly synthesized 1-desoxyfructo-alpha,beta-dehydro-4, 5-dioxotryptamine (M4) inhibited the 5-hydroxytryptamine (5-HT)-induced shape-change reaction of human and rabbit platelets and to a lesser extent the adenosine-3',5'-diphosphate-induced shape-change reaction of rabbit platelets. The 5-HT-antagonism was shown to be of the competitive type in human platelets. In the latter M4 also counteracted the 5-HT-uptake, but was virtually ineffective in releasing 5-HT. Another new derivative of desoxyfructo-5-HT (M5) was a 5-HT-agonist. It is concluded that M4 represents a new class of antagonists of 5-HT-receptors in platelets.
新合成的1-脱氧果糖-α,β-脱氢-4,5-二氧代色胺（M4）抑制了5-羟色胺（5-HT）诱导的人及兔血小板的形态变化反应，对兔血小板的腺苷-3',5'-二磷酸诱导的形态变化反应的抑制作用较小。在人血小板中，5-HT拮抗作用显示为竞争性类型。在人血小板中，M4还可对抗5-HT的摄取，但在释放5-HT方面几乎无效。脱氧果糖-5-HT的另一种新衍生物（M5）是一种5-HT激动剂。得出的结论是，M4代表血小板中5-HT受体的一类新型拮抗剂。
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