| 苄基四氢巴马汀对α受体的作用 |
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| 引用本文： | 张树东 姚伟星. 苄基四氢巴马汀对α受体的作用[J]. 中国药理学通报, 1991, 7(3): 182-186 |
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| 作者姓名： | 张树东 姚伟星 |
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| 作者单位： | 同济医科大学药理教研室 汉口430030(张树东，姚伟星，曲玲，夏国瑾)，同济医科大学药理教研室 汉口430030(江明性) |
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| 基金项目： | 国家自然科学基金资助课题 |
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| 摘 要： | 本实验表明苄基四氢巴马汀(BTHP)具有阻断α-肾上腺素受体的作用。它能竞争性拮抗苯肾上腺素所致大鼠肛尾肌和兔主动脉条的收缩反应,其pA_2值分别为5.86和5.8;也能浓度依赖性地使可乐定和B-HT920的量效曲线平行右移,最大反应不变,其pA_2值分别为5.2和5.3。放射配基结合测定表明,BTHP对α_1和α_2受体均有亲和力,其竞争抑制常数(K_i)分别为3.52μmol/L和8.1μmol/L。
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| 关 键 词： | 小檗因类 节基四氢巴马汀 肾上腺素α受体 放射配基结合测定 |
THE ACTION OF BENZYLTETRAHYDROPALMATINE ON α ADRENOCEPTOR |
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| Zhang Shudong,Yao Weixing,Qu ling. THE ACTION OF BENZYLTETRAHYDROPALMATINE ON α ADRENOCEPTOR[J]. Chinese Pharmacological Bulletin, 1991, 7(3): 182-186 |
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| Authors: | Zhang Shudong Yao Weixing Qu ling |
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| Abstract: | The action of BTHP on a-adrenoceptor was studied in anococcy-geus muscles, vas deferens and cell membrane of cerebral cortex of rats and aortic strips, saphenous vein of rabbit. BTHP produced parallel shifts to the right of dose-response curves for phenylephrine in rat anococcygeus muscle and rabbit aortic strips without change in the maximal responses. Their pA2 values were 5.8 and 5.86 respectively. BTHP was also a competitive antagonist for presynaptic and postsynaptic α2-adrenoceptors on prostatic portion of rat vas deferens( pA2 against clonidine=5.2 ) and on rabbit saphenous vein ( pA2 against B-HT920=5.3 ) . BTHP decreased in dose-dependent manner 〔8H〕 prazosin and 〔3H〕 clonidine specific binding to α1- and α2- adrenoceptors on cell membrane of cerebral cortex in rats with IC50 of4 and 9.5 μmol/L and with Ki ( apparent dissociation constant ) of 3.5 and 8.1μmol/L respectively, suggeating that BTHP has affinity for both α1 and α2- adrenoceptors of rat cerebrance. |
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| Keywords: | Berbines Benzyltetrahydropalmatine α-adrenoceptor Radioligand binding assay |
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