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大鼠脑中[3H]哌唑嗪标记的α1受体结合位点亚型的鉴定。

Identification of subtypes of [3H]prazosin-labelled alpha 1 receptor binding sites in rat brain.

作者信息

Morrow A L, Battaglia G, Norman A B, Creese I

出版信息

Eur J Pharmacol. 1985 Feb 26;109(2):285-7. doi: 10.1016/0014-2999(85)90432-7.

Abstract

Detailed antagonist competition curves for [3H]prazosin-labelled binding sites in rat cerebral cortex membranes reveal anomalous binding characteristics. Dihydroergocryptine and indoramine compete in a steep, monophasic manner while WB4101 and phentolamine exhibit shallow competition curves. Computer-assisted analysis of binding data indicate that both WB4101 and phentolamine discriminate identical subpopulations of [3H]prazosin binding sites, which each comprise approximately 50% of specific [3H]prazosin binding. These data suggest the presence of subtypes of [3H]prazosin-labelled alpha 1 adrenergic receptors in rat cerebral cortex.

摘要

大鼠大脑皮层膜中[3H]哌唑嗪标记结合位点的详细拮抗剂竞争曲线显示出异常的结合特性。双氢麦角隐亭和吲哚胺以陡峭的单相方式竞争,而WB4101和酚妥拉明则呈现出浅竞争曲线。结合数据的计算机辅助分析表明,WB4101和酚妥拉明都能区分相同的[3H]哌唑嗪结合位点亚群,每个亚群约占特异性[3H]哌唑嗪结合的50%。这些数据表明大鼠大脑皮层中存在[3H]哌唑嗪标记的α1肾上腺素能受体亚型。

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