Stereoselectivity of muscarinic receptors in vivo and in vitro for oxotremorine analogs. N-[4-tert-amino-2-butynyl]-5-methyl-2-pyrrolidones

R Amstutz, B Ringdahl, B Karlen, M Roch…

文献索引：Amstutz; Ringdahl; Karlen; Roch; Jenden Journal of Medicinal Chemistry, 1985 , vol. 28, # 12 p. 1760 - 1765

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被引用次数: 27

摘要

The enantiomers of three 5-methyl-2-pyrrolidone dogues of the muscarinic agent oxotremorine (1) were synthesized. The pyrrolidine derivative (R)-13 was an antagonist to carbachol in the guinea pig ileum and also showed central and peripheral antimuscarinic activity in vivo. It was more potent and more selective than atropine in antagonizing the central effects of 1. The dimethylamino analogue (R)-14 and the trimethylammonium salt ( ...