| 4种异喹啉类衍生物对α-肾上腺素受体的阻断作用 |
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| 引用本文： | 姚伟星,夏国瑾,江明胜,黄文龙,黄枕亚,彭司勋.4种异喹啉类衍生物对α-肾上腺素受体的阻断作用[J].中国药理学通报,1989(6). |
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| 作者姓名： | 姚伟星 夏国瑾 江明胜 黄文龙 黄枕亚 彭司勋 |
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| 作者单位： | 同济医科大学药理教研组 汉口430030
(姚伟星，夏国瑾，江明胜)，中国药科大学药化研究室 南京210009
(黄文龙，黄枕亚)，中国药科大学药化研究室 南京210009(彭司勋) |
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| 摘 要： | 4种异喹啉类化合物(Isoquinoline derivative IQ_(85029),Q_(85030),IQ_(86034),IQ_(86035)的抗α_1及α_2肾上腺素受体的作用在大鼠肛尾肌及输精管标本上进行了比较,在肛尾肌标本上,IQ_(86034)抗α_1受体的作用最强(pA_2=6.5),IQ_(85030)最弱(pA_2=5.1),而IQ_(85020)及IQ_(86035)的效价强度相近(pA_2=6.0～6.1)。在输精管前列腺端,它们拮抗α_2受体的效价强度依次为IQ_(86035)(pA_2=6.75)>IQ_(85030)(6.69)>IQ_(85029)(6.34)>IQ_(86034)(5.3)。
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| 关 键 词： | 异喹啉类衍化物 肛尾肌 输精管前列腺端 苯福林 可乐定 量效曲线 |
COMPARISON BETWEEN BLOCKING ACTIONS OF ISOQUINOLINE DERIVATIVES ON α_1 AND α_2 ADRENOCEPTORS |
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| Yao Weixing,Xia Guojin,Jiang Mingxing.COMPARISON BETWEEN BLOCKING ACTIONS OF ISOQUINOLINE DERIVATIVES ON α_1 AND α_2 ADRENOCEPTORS[J].Chinese Pharmacological Bulletin,1989(6). |
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| Authors: | Yao Weixing Xia Guojin Jiang Mingxing |
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| Abstract: | The potencies of the α1 and α2 adrenoceptor antagonists of 4 isoquinoline derivatives ( IQ85029, IQ85030, IQ86034, IQ86035) were compared at pre - and postsynalptic a adrenoceptors in the isolated vas deferens and anococcygeus muscle of rats respectively.
The 4 compounds were shown to be competitive antagonists of phenylephrine on the rat anococcygeus muscle. Among the 4 compounds IQ86034 was most active (pA2 = 6.5), and IQ85030 least active ( pA2 = 5.1). Whereas IQ85029 and IQ86035 were of equal potency as α, recept6r antagonists ( pA2 = 6 .0~6.1).
The relative order of potency of the 4 compounds against clonidine in the vas deferens was IQ86035 ( pA2 = 6.75 ) >IQ85030(6.69)>IQ85020 (6.34)>IQ86034 (5.3).
In addition, the blocking action of 4 isoquinoline derivatives on α1 and α2 adrenoceptors was similar to that of benzoquinolizine derivatives. |
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| Keywords: | Isoquinoline derivatives Anococcygeus muscle Vas deferens Phenylephrine Clonidine Dose-response curve |
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