New analogues of oxotremorine and oxotremorine-M - Estimation of their in vitro affinity and efficacy at muscarinic receptor subtypes

Two subsets of tertiary amines (1a-6a) and methiodides (1b-6b) with a struc tural resemblance to oxotremorine and oxotremorine-M were tested at rabbit vas deferens (M-1), guinea pig left atrium (M-2), guinea pig ileum and urin ary bladder (M-3) muscarinic receptor subtypes, The pharmacological profile of the derivatives under study has been discussed by evaluating their pote ncy, affinity and efficacy as well as the regional differences in muscarini c receptor occupancy. (C) 2000 Elsevier Science Inc. All rights reserved.