[3H]Rauwolscine and [3H]yohimbine binding to rat cerebral and human platelet membranes: possible heterogeneity of alpha 2-adrenoceptors.
[3H]Rauwolscine and [3H]yohimbine binding to rat cerebral and human platelet membranes: possible heterogeneity of alpha 2-adrenoceptors.
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[3H]Rauwolscine 和 [3H]yohimbine 与大鼠脑和人血小板膜结合：α2-肾上腺素受体可能存在异质性。
DOI：
10.1016/0014-2999(82)90159-5
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发表时间：
1982
影响因子：
5
通讯作者：
S. Nahorski
中科院分区：
文献类型：
--
作者：
Y. Cheung;D. Barnett;S. Nahorski
α2-肾上腺素受体拮抗剂[3H]育亨宾和[3H]萝芙素与大鼠大脑皮层和人血小板制备的膜的特异性结合是快速、可逆、可饱和且具有高亲和力。两种配体都标记了大脑或血小板膜中相同的位点群，尽管两种药物在大脑中的亲和力明显较低。两种组织中[3H]育亨宾和[3H]rauwolscine的特异性结合被各种肾上腺素能药物取代，其方式表明标记位点可能代表α2-肾上腺素受体。然而，大脑和血小板制剂之间某些α-拮抗剂的亲和力存在显着差异，尽管这些药物在两种组织中产生斜率接近一致的位移曲线。因此，虽然育亨宾、萝芙素、WB4101和Corynanthin在大脑皮质中的作用均较弱，但哌唑嗪在皮质中的作用明显强于在血小板膜中的作用。讨论了 α2-肾上腺素受体可能的异质性。
The specific binding of the α2-adrenoceptor antagonists [3H]yohimbine and [3H]rauwolscine to membranes prepared from rat cerebral cortex and human platelets was rapid, reversible, saturable and of high affinity. Both ligands labelled an identical population of sites in cerebral or platelet membranes though the affinities of both agents were significantly lower in brain. The specific binding of [3H]yohimbine and [3H]rauwolscine in both tissues was displaced by various adrenergic agents in a manner that suggests that the labelled sites probably represent the α2-adrenoceptor. There were, however, significant differences in the affinities of certain α-antagonists between cerebral and platelet preparations, even though these agents generated displacement curves with slopes close to unity in both tissues. Thus, whereas yohimbine, rauwolscine, WB4101 and corynanthine were all weaker in cerebral cortex, prazosin was significantly more potent at cortical than in platelet membranes. A possible heterogeneity of α2-adrenoceptors is discussed.
与α-肾上腺素能受体结合的激动剂与拮抗剂。
DOI：
10.1073/pnas.77.8.4569
发表时间：
1980
影响因子：
11.1
作者：
Hoffman,BB;Michel,T;Kilpatrick,DM;Lefkowitz,RJ;Tolbert,ME;Gilman,H;Fain,JN
通讯作者：
Fain,JN