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腺苷5-二磷酸拮抗剂与人类血小板:无证据表明聚集和刺激型腺苷酸环化酶的抑制作用由不同受体介导。

Adenosine 5-diphosphate antagonists and human platelets: no evidence that aggregation and inhibition of stimulated adenylate cyclase are mediated by different receptors.

作者信息

Cusack N J, Hourani S M

出版信息

Br J Pharmacol. 1982 May;76(1):221-7. doi: 10.1111/j.1476-5381.1982.tb09210.x.

Abstract

1 Adenosine 5'-diphosphate (ADP) induces human platelet aggregation and noncompetitively inhibits stimulated human platelet adenylate cyclase; it has been suggested that these two effects are mediated by separate ADP receptors on the platelet surface. 2 Adenosine 5'-triphosphate and seven adenine nucleotide analogues were tested as inhibitors of both effects of ADP on human platelets, and were found to be competitive. 3 pA2 values were calculated for each antagonist for inhibition of both effects of ADP, and a good correlation (correlation coefficient 0.87; p less than 0.01) was found between the pA2 values for inhibition of ADP-induced aggregation and the pA2 values for inhibition of the effect of ADP on stimulated adenylate cyclase. 4 Such a correlation does not support the suggestion that ADP-induced aggregation and the inhibition by ADP of stimulated adenylate cyclase are mediated by two separate receptors.

摘要
  1. 腺苷5'-二磷酸(ADP)可诱导人血小板聚集,并对受刺激的人血小板腺苷酸环化酶产生非竞争性抑制作用;有人提出这两种作用是由血小板表面不同的ADP受体介导的。2. 对腺苷5'-三磷酸和七种腺嘌呤核苷酸类似物作为ADP对人血小板两种作用的抑制剂进行了测试,发现它们具有竞争性。3. 计算了每种拮抗剂抑制ADP两种作用的pA2值,发现抑制ADP诱导聚集的pA2值与抑制ADP对受刺激腺苷酸环化酶作用的pA2值之间存在良好的相关性(相关系数0.87;p小于0.01)。4. 这种相关性不支持ADP诱导聚集和ADP对受刺激腺苷酸环化酶的抑制作用是由两种不同受体介导的这一观点。

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