肝素使人类血小板膜中的α2 -肾上腺素能受体与Gi蛋白解偶联。
Heparin uncouples alpha 2-adrenoceptors from the Gi-protein in membranes of human platelets.
作者信息
Willuweit B, Aktories K
机构信息
Rudolf-Buchheim-Institut für Pharmakologie, Giessen, Federal Republic of Germany.
出版信息
Biochem J. 1988 Feb 1;249(3):857-63. doi: 10.1042/bj2490857.
Abstract
The influence of heparin was studied on the inhibitory regulation of adenylate cyclase in human platelet membranes. Heparin blocked the adrenaline-induced inhibition of adenylate cyclase and the stimulation of GTP hydrolysis with half-maximal and maximal efficiency at 0.3 and 1-3 micrograms/ml, respectively. The effect of heparin was reversed by washing the membranes. Heparin did not change the number of alpha-adrenoceptors. In contrast, the affinity of the alpha-adrenoceptor for adrenaline was decreased in the presence of heparin. The pertussis toxin-catalysed ADP-ribosylation of the inhibitory guanine nucleotide-binding Gi-protein was not altered by heparin. Heparin also abolished the inhibition of adenylate cyclase caused by GTP itself. The data indicate that heparin can impair the hormone-induced inhibition of adenylate cyclase and the stimulation of GTP hydrolysis and suggest that the effects of heparin are caused by an action at the Gi-protein of the adenylate cyclase system.
摘要
研究了肝素对人血小板膜中腺苷酸环化酶抑制调节的影响。肝素可阻断肾上腺素诱导的腺苷酸环化酶抑制作用以及GTP水解的刺激作用，其半数最大效应浓度和最大效应浓度分别为0.3微克/毫升和1 - 3微克/毫升。通过洗涤膜可逆转肝素的作用。肝素不改变α-肾上腺素能受体的数量。相反，在肝素存在的情况下，α-肾上腺素能受体对肾上腺素的亲和力降低。肝素不改变百日咳毒素催化的抑制性鸟嘌呤核苷酸结合蛋白Gi的ADP核糖基化。肝素还消除了GTP本身引起的腺苷酸环化酶抑制作用。这些数据表明，肝素可损害激素诱导的腺苷酸环化酶抑制作用以及GTP水解的刺激作用，并提示肝素的作用是由其对腺苷酸环化酶系统中Gi蛋白的作用引起的。
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本文引用的文献
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Effects of heparin on platelet aggregation and release and thromboxane A2 production.肝素对血小板聚集、释放及血栓素A2生成的影响。
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Ni-mediated inhibition of human platelet adenylate cyclase by thrombin.镍介导凝血酶对人血小板腺苷酸环化酶的抑制作用。
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