腺苷5'-O-(2-硫代二磷酸)对人血小板的部分激动剂行为。
Partial agonist behaviour of adenosine 5'-O-(2-thiodiphosphate) on human platelets.
作者信息
Cusack N J, Hourani S M
出版信息
Br J Pharmacol. 1981 Jun;73(2):405-8. doi: 10.1111/j.1476-5381.1981.tb10436.x.
Abstract
1 The effects of an adenosine diphosphate (ADP) analogue, adenosine 5'-O-(2-thiodiphosphate) (ADP-beta-S), in which a terminal phosphate oxygen has been replaced by sulphur, were studied on human platelets. 2 ADP-beta-S induced platelet aggregation and inhibited prostaglandin E1 (PGE1)-stimulated adenylate cyclase but in both cases was less potent than ADP and did not achieve the same maximal effects. 3 Both actions of ADP could be inhibited by the simultaneous addition of ADP-beta-S (50 microM). 4 Aggregation induced by 11 alpha, 9 alpha-epoxymethano prostaglandin H2 (a stable endoperoxide analogue) was not inhibited by simultaneous addition of ADP-beta-S (50 microM). 5 The behaviour of ADP-beta-S towards human platelets was consistent with it being a partial agonist.
摘要
- 研究了一种二磷酸腺苷（ADP）类似物，即腺苷5'-O-（2-硫代二磷酸）（ADP-β-S）对人血小板的作用，其中一个末端磷酸氧被硫取代。2. ADP-β-S诱导血小板聚集并抑制前列腺素E1（PGE1）刺激的腺苷酸环化酶，但在这两种情况下其效力均低于ADP，且未达到相同的最大效应。3. ADP的两种作用均可被同时添加的ADP-β-S（50微摩尔）抑制。4. 同时添加ADP-β-S（50微摩尔）不会抑制由11α，9α-环氧甲撑前列腺素H2（一种稳定的内过氧化物类似物）诱导的聚集。5. ADP-β-S对人血小板的作用表明它是一种部分激动剂。
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