McCarthy B G, Peroutka S J
Department of Neurology, Stanford University Medical Center, CA 94305.
Aviat Space Environ Med. 1988 Jan;59(1):63-6.
Radioligand binding studies were used to analyze muscarinic cholinergic receptor subtypes in human cortex and pons. Muscarinic cholinergic receptors were labeled by 3H-quinuclidinyl benzilate (3H-QNB). Scopolamine was equipotent in both brain regions and did not discriminate subtypes of 3H-QNB binding. By contrast, the M1 selective antagonist pirenzepine was approximately 33-fold more potent in human cortex than pons. Carbachol, a putative M2 selective agonist, was more than 100-fold more potent in human pons than cortex. These results demonstrate that the human pons contains a relatively large proportion of carbachol sensitive muscarinic cholinergic receptors. Drugs targeted to this subpopulation of muscarinic cholinergic receptors may prove to be effective anti-motion sickness agents with less side effects than scopolamine.
放射性配体结合研究用于分析人类大脑皮层和脑桥中的毒蕈碱型胆碱能受体亚型。毒蕈碱型胆碱能受体用3H-喹核醇基苯甲酸酯（3H-QNB）标记。东莨菪碱在两个脑区的效力相同，无法区分3H-QNB结合的亚型。相比之下，M1选择性拮抗剂哌仑西平在人类大脑皮层中的效力比脑桥大约强33倍。卡巴胆碱，一种假定的M2选择性激动剂，在人类脑桥中的效力比大脑皮层强100倍以上。这些结果表明，人类脑桥中含有相对较大比例的对卡巴胆碱敏感的毒蕈碱型胆碱能受体。针对这一毒蕈碱型胆碱能受体亚群的药物可能被证明是有效的抗晕动病药物，且副作用比东莨菪碱小。
