Christopoulos A, El-Fakahany E E
Division of Neuroscience Research in Psychiatry, University of Minnesota Medical School, Minneapolis 55455, USA.
Eur J Pharmacol. 1997 Sep 3;334(1):R3-4. doi: 10.1016/s0014-2999(97)01162-x.
The muscarinic agonists, xanomeline and carbachol, displayed similar intrinsic activities in stimulating neuronal nitric oxide synthase at muscarinic M1 receptors in Chinese hamster ovary (CHO) cells, with xanomeline being more potent. Pre-incubation (1 h) with 1 microM xanomeline, followed by extensive washing, resulted in a significantly elevated basal response, which was absent on co-incubation with atropine. This phenomenon was not observed with carbachol. This is the first report of a persistent, receptor-activating effect of a muscarinic agonist.
毒蕈碱激动剂西那美宁和卡巴胆碱，在中国仓鼠卵巢（CHO）细胞的毒蕈碱M1受体上刺激神经元型一氧化氮合酶时表现出相似的内在活性，其中西那美宁的效力更强。用1微摩尔西那美宁预孵育（1小时），随后进行充分洗涤，导致基础反应显著升高，而与阿托品共同孵育时则无此现象。卡巴胆碱未观察到这种现象。这是关于毒蕈碱激动剂持续的受体激活作用的首次报道。
