Kharkevich D A, Skoldinov A P, Samăilov D N, Shorr V A
Farmakol Toksikol. 1980 Nov-Dec;43(6):645-52.
Effects of a number of agents on the muscarine-sensitive acetylcholine receptors (muscarinic receptors) of different localization were investigated. Experiments on anesthetized cats revealed the following effects of acetylcholine: hypotension, bradycardia, bronchospasm, contractions of the ileum and urinary bladder, hypersalivation. It was shown that the highest sensitivity to bisquaternary ammonium derivatives of diphenyl cyclobutanedicarboxylic (truxillic) acid is exhibited by the muscarinic receptors of the heart. The sensitivity of bronchial muscarinic receptors is slightly lower. The prevailing action on the muscarinic receptors of the heart was also shown by some N-adamantyl bisquaternary ammonium compounds. Procaine and the antihistaminics mebhydroline and diphenhydramine eliminated bradycardia induced by acetylcholine without affecting the latter's hypotensive effect. The evidence obtained indicates the heterogeneity of the muscarinic receptors of different localization.
研究了多种药物对不同定位的毒蕈碱敏感型乙酰胆碱受体(毒蕈碱受体)的影响。在麻醉猫身上进行的实验揭示了乙酰胆碱的以下作用:低血压、心动过缓、支气管痉挛、回肠和膀胱收缩、唾液分泌过多。结果表明,二苯基环丁烷二羧酸(吐昔酸)的双季铵衍生物对心脏的毒蕈碱受体表现出最高的敏感性。支气管毒蕈碱受体的敏感性略低。一些N-金刚烷基双季铵化合物对心脏的毒蕈碱受体也有主要作用。普鲁卡因以及抗组胺药甲苄二胺和苯海拉明消除了乙酰胆碱引起的心动过缓,而不影响后者的降压作用。所获得的证据表明不同定位的毒蕈碱受体具有异质性。