Abstract
Abstract The thiolactam analogue of oxotremorine (I) has been prepared and examined for muscarinic activity in mice and on guinea-pig ileal preparations. It is inactive in itself, but is transformed in vivo to oxotremorine (II), which has been identified in the urine of mice. The urine also contains 1-(2-oxopyrrolidino)-4-pyrrolidino-2-butanone (III) which is formed non-enzymatically from I under acidic conditions, but does not display any acetylcholine-like properties in vivo or in vitro. Oxotremorine is not formed from I in vitro.
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