A series of acetylenic imidazoles related to oxotremorine (la) were prepared and evaluated as cholinergic agents with in vitro binding assays and in vivo pharmacological teste in mice. 1-[4-(1H-Imidazol-1-yl)-2-butynyl]-2-pyrrolidinone (lb) was a cholinergic agonist with one- half the potency of oxotremorine. Analogues of lb with a 5-or 2-methyl substituent in the imidazole ring (compounds IC and lg) were cholinergic partial agonists. Analogues of lb ...
