Pharmacological Characterisation of the Enantiomers of BM‐5, a Muscarinic Partial Agonist with Opposed Enantioselectivity between Affinity and Efficacy*
Abstract:The interaction of (R) and (S) enantiomers of the chiral oxotremorine analogue BM-5 with muscarinic acetylcholine receptors was studied in vitro using radioligand binding and isolated tissue preparations. The in vivo effects of (R)-BM-5 were also studied in anaesthetised cat. No receptor or tissue selectivity was found for either enantiomer in radioligand binding studies in cells expressing human muscarinic receptors (M 1 -M 5 ) or in guinea pig tissues. The affinity of (R)-BM-5 was about 40 times, or 15-60 ti… Show more
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.