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Additional abstract from: Abstracts of the 3rd joint meeting of the Societa Italiana di Farmacologia and the French Association des Pharmacologistes, Capri, 23–26 May 1996

To develop ligands which may be useful in exploring muscarinic receptor heterogeneity, we synthesized a series of analogues of 2,2 diphenyl [ 1,3 ] dioxolan 4 ylmethyldimethylamine oxalate and methiodide bearing a modified cationic head. These compounds, when tested on tissues containing the three subtypes M,, M, and M,, behaved as muscarinic antagonists; the results show that different substituents on the quaternary and tertiary nitrogen affect aftinlty and selectivity in different ways (1). Dose-response curves were constructed by cumulative addition of agonist. The concentration of agonist in the organ bath was increased approximately 3-fold at each step, each addition being made only after the response to the previous addition had attained a maximal level and remained steady. In all cases, parallel experiments in which tissues did not receive any antagonist were run in order to check any variation in sensitivity. Preliminary results show that some of these compounds seem to discriminate (5 -10 fold) between the M, subtypes of guinea pig ileum and bladder.