过刊浏览

M-胆碱药物对大鼠皮层、腮腺和豚鼠小肠纵肌中 M-乙酰胆碱受体的作用比较

俞霭瑶, 金国章, 许建, 俞蕾平, 李建华

上海第二医学院. 上海；中国科学院上海药物研究所. 上海

摘要

该文应用[~(3)H]-QNB 为放射性配基,研究 M-胆碱激动剂或阻滞剂对大鼠脑皮层、腮腺和豚鼠小肠纵肌中 M-乙酰胆碱受体竞争结合的影响。经量-效比式计算后,证明它们的作用斜率(b)约为1,表明它们作用在相同的 M-乙酰胆碱受体。阻滞剂对皮层中 M-胆碱受体的抑制结合强度次序为:QNB>阿托品,东莨菪碱>苯海索>M-8218>B-7601>M-8225>7911;而它们对腮腺中 M-乙酰胆碱受体的抑制作用次序有明显不同,即 M-8218>QNB>7911>M-8225>B-7601>苯海索>阿托品>东莨菪碱,其中阿托品和东莨菪碱的抑制结合强度分别为皮层的1/111和1/315。这提示不同靶细胞中的 M-乙酰胆碱受体与相同配基结合时有不同的专一性。

关键词： 东莨菪碱; 二苯羟乙酸喹宁酯; M-8218; 包公藤甲素; 大鼠腮腺; M-乙酰胆碱受体; 大鼠皮层 M-乙酰胆碱受体; 豚鼠小肠纵肌 M-乙酰胆碱受体

Comparison of effects of M-cholinergic compounds on m-acetylcholine receptors in rat cortex parotid gland and longitudinal muscle from small intestine of guinea pig

Yu Aiyao, Jin Guozhang, K C Kin, Xu Jian, Yu Leiping

Shanghai Institute of Materia Medica, Chinese Academy of Sciences. Shanghai, China

Abstract

[~(3)H]-QNB was used as a radioligand for M-acetylcholine receptors (M-AChR) binding in the experiments of competitive inhibition by M-cholinergic agonists and antagonists with the homogenate preparations of rat cortex, parotid gland, and longitudinal muscle from small intestine of guinea pig. With the regression computation (dose-response equation), the slopes of these compounds were all approximate to 1. Thus it was indicated that they acted in the same way on M-AChR (or receptor sites). The rank order of potency of receptor binding assay (IC_(50)) in rat cortex was QNB>atropine, scopolamine>benzhexal>M-8218>B-7601>M-8225>7911, but that in the rat parotid gland was signifcantly different, i.e. M-8218>QNB>7911>M-8225>B-7601>benzhexal>atropine>scopolamine. In particular, the potencies of atropine and scopolamine in the rat cortex were 111 and 316.6 times as active respectively as those in the rat parotid gland. It is ,therefore, suggested that M-AChR in the different target organs have some specific characteristics to be found by various M-antagonists.

Key words: Scopolamin;QNB;M-8218;Alpha, #beta#-hydroxy-g #beta#-acetoxynortropane;M-acetylcholine receptors in rat parotid gland;M-acetyloholine receptor in rat cortex;M-acetylcholine receptors in longitudinal muscle of guinea pig;

收稿日期：　　录用日期：

通讯作者：　　E-mail:

引用本文：

俞霭瑶, 金国章, 许建, 俞蕾平, 李建华. M-胆碱药物对大鼠皮层、腮腺和豚鼠小肠纵肌中 M-乙酰胆碱受体的作用比较[J]. 生理学报 1985; 37 (3): .

Yu Aiyao, Jin Guozhang, K C Kin, Xu Jian, Yu Leiping. Comparison of effects of M-cholinergic compounds on m-acetylcholine receptors in rat cortex parotid gland and longitudinal muscle from small intestine of guinea pig . Acta Physiol Sin 1985; 37 (3): (in Chinese with English abstract).