吕志珍, 魏璇, 金国章, 韩启德. 四氢原小檗碱同类物对α1肾上腺素受体的拮抗作用J. 药学学报, 1996, 31(9): 652-656.
引用本文: 吕志珍, 魏璇, 金国章, 韩启德. 四氢原小檗碱同类物对α1肾上腺素受体的拮抗作用J. 药学学报, 1996, 31(9): 652-656.
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ZZ Lu, X Wei, GZ Jin, QD Han. ANTAGONISTIC EFFECT OF TETKAHYDKOPROBERBEKINE HOMOLOGUES ON α1-ADRENOCEPTORJ. Acta Pharmaceutica Sinica, 1996, 31(9): 652-656.
Citation: ZZ Lu, X Wei, GZ Jin, QD Han. ANTAGONISTIC EFFECT OF TETKAHYDKOPROBERBEKINE HOMOLOGUES ON α1-ADRENOCEPTORJ. Acta Pharmaceutica Sinica, 1996, 31(9): 652-656.
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四氢原小檗碱同类物对α1肾上腺素受体的拮抗作用

ANTAGONISTIC EFFECT OF TETKAHYDKOPROBERBEKINE HOMOLOGUES ON α1-ADRENOCEPTOR

    摘要
  • 摘要: 用放射配体结合实验与离体血管收缩功能实验相结合的方法,研究了4种四氢原小檗碱(tetrahydroproberberine,THPB)同类物对α1-肾上腺素受体(α1-AR)的作用。结果显示左旋四氢巴马汀(l-THP),左旋千金藤立陡碱(l-SPD),四氢原小檗碱-18(THPB-18)和四氢小檗碱(THB)125IBE2254125I-2-β(4-hydroxyphenyl)-ethyaminomethyl-tetralone,125IBE)与大鼠脑皮质α1-AR的结合呈竞争性拮抗作用,pKI值分别为5.54±0.36,5.56±0.47,5.75±0.56和6.01±0.60,Hill系数接近于1.0。并拮抗苯肾上腺素(phenylephrine,PE)介导大鼠主动脉的收缩,pA2值分别为5.48±0.58,5.66±0.54,5.64±0.34和5.45±0.76,斜率与1.0无显著性差别。结果提示,4种四氢原小檗碱同类物对α1-AR均有非亚型选择性拮抗效应,且亲和性相同。

     

    Abstract: The antagonistic effect of tetrahydroproberberine(THP)homologues on α1-adrenoceptor was studied by combination of radioligand binding assays and measurements ofvasoconstriction responses.The results showed that l-tetrahydropalmatine(l-THP),l- stepholidine(l-SPD),THPB-18 and tetrahydroberberine(THB)competitively inhibited the 125 I-BE2254 specificbinding in rat cerebral cortex with pKI values of 5.54±0.36,5.56±0.47,5.75±0.56 and 6.01 ±0.60,respectively,and the Hill efficiency was not significantly different from unity.They inhibitedphenylephrine-induced constrictions with pA2 values of 5.48 ± 0.58,5.66 ± 0.54,5.64 ± 0.34 and5.45 ± 0.76,respectively,and the slopes of Schild plot were not significantly different from unity。The results indicate that the 4 THP homologues are nonsubtype selective competitive antagonists forα1 

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