| 美西律衍生物对α1肾上腺素受体的作用 |
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| 引用本文： | 宋武,张义军.美西律衍生物对α1肾上腺素受体的作用[J].药学学报,1998,33(2):102-105. |
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| 作者姓名： | 宋武 张义军 |
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| 作者单位： | 中国药科大学药理教研室，山东潍坊医学院药理教研室 |
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| 摘 要： | 为寻找新的α1受体阻断剂,用3H]-WB4101配体测定法测定了18种美西律衍生物。结果表明,其中6种化合物对大鼠脑皮层α1受体有不同程度的亲和力。凡具有手性碳结构的化合物亲和力都较高。化合物M-85001的亲和力较妥拉唑林(tolazoline)高一个数量级并能抑制苯肾上腺素引起的大鼠肛尾肌收缩,其pA2(6.86)与pKi(6.51)相近。结果提示,美西律衍生物对α1-受体的亲和力可能与手性碳结构有关,从美西律衍生物中研制新的α1-受体阻断剂是有前途的。
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| 关 键 词： | α1-受体阻断剂 美西律衍生物 放射配体结合法 |
| 收稿时间： | 1997-03-24 |
Effects of some mexiletine derivatives on alpha 1-adrenoceptors] |
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| W Song,Y Zhang,L Xia,G Liu.Effects of some mexiletine derivatives on alpha 1-adrenoceptors][J].Acta Pharmaceutica Sinica,1998,33(2):102-105. |
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| Authors: | W Song Y Zhang L Xia G Liu |
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| Institution: | Department of Pharmacology, China Pharmaceutical University, Nanjing 210009. |
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| Abstract: | Using 3H]-WB 4101 binding assay in rat cerebral cortex membranes, effects of 18 mexiletine derivatives on alpha 1-adrenoceptors were studied in order to find new antihypertensive alpha 1 receptor blocking agents. The results showed that 6 of them showed significant affinities to alpha 1-adrenoceptors in rat cerebral cortex membranes. Some structure-activity relationship were found, among them only the compounds with chiral carbon showed high affinity to alpha 1-adrenoceptor. The affinity of compound M-85001 (pKi = 6.51) was shown to be higher than that of tolazoline. In the rat anococcygeal muscle, compound M-85001 competitively antagonized phenylephrine-induced contraction with pA2 value of 6.86 which is similar to its pKi value in the binding assay. These findings may be of significance in the search for novel class of alpha 1 receptor antagonists. |
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