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千金藤碱等异喹啉类生物碱对5—羟色胺受体的阻断作用
引用本文:刘国卿,陈曙光,马志清. 千金藤碱等异喹啉类生物碱对5—羟色胺受体的阻断作用[J]. 中国药理学通报, 1988, 0(2)
作者姓名:刘国卿  陈曙光  马志清
作者单位:中国药科大学药理教研室 南京(刘国卿,陈曙光),中国药科大学药理教研室 南京(马志清)
摘    要:用大鼠离体胃底条标本研究表明,1-STP在低浓度(16,25μM)时竞争性阻断5-HT受体,使5-HT对胃底条标本的量效曲线平行右移,其pA_2值为5.8,在较高浓度时(50μM)则与1-REM相似,表现为非竞争性拮抗作用,两者的pD’_2值分别为4.2和4.5。1—SPD,1-THP和THB亦能阻断5-HT受休,pA_2值分别为6.2,5.2和5.0。实验结果表明,1-STP等异喹啉生物碱对大鼠胃底条 5-HT受体具有阻断作用。

关 键 词:左旋千金藤碱  异喹啉生物碱  大鼠胃底条  5-羟色胺受体  阻断作用

5-HT RECEPTOR BLOCKADE PROPERTIES OF STEPHANINE AND OTHER TETRAHYDROQUINOLINE ALKALOIDS
Liu Guoqing,Chen Shuguang and Ma Zhiqin. 5-HT RECEPTOR BLOCKADE PROPERTIES OF STEPHANINE AND OTHER TETRAHYDROQUINOLINE ALKALOIDS[J]. Chinese Pharmacological Bulletin, 1988, 0(2)
Authors:Liu Guoqing  Chen Shuguang  Ma Zhiqin
Abstract:Studies using isolated rat fundus strip preparation demonstrated that l-stephanine ( l-STP ) , l-roemerine ( 1-REM ), l-stepholidine (l-SPD), 1-tetrahydropalmatine ( l-THP ) and dl-tetrahydrode-berine ( THB ) possessed 5-HT blockade properties. 1-STP ( 16, 25 μM ) produced competitve antagonism against 5-HT receptor on rat fundus, while higher concentration ( 50 μM ) suggested a non-competi tive inhibition, with pA2' and2' values equal to 5.8 and 4.2 respectively. 1-REM was found to be a non-competitive antagonIst ( pD' 2 = 4.5). 1-SPD, 1-THP and THB cuased a parallel shift to the right of 5-HT concentration response curve without any significant changes in their maximum response, indicating that they were competitive antagonists of 5-HT receptor. The antagonistic potencies of 1-SPD, l-THP and THB were expressed as pA2 values: 6.2,5.2 and 5.0.
Keywords:Stephanine  Tetrahydroquinoline alkaloids  5-HT receptor  Rat fnndus  Antagonist
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