title: Stereoselectivity of the interaction of muscarinic antagonists with their receptors.
abstract: The stereoselectivity of the interaction with muscarinic receptors of enantiomers of a series of chiral antagonists is receptor subtype dependent. There is no overall relationship between stereoselectivity and receptor affinity. Depending on the antagonist studied, receptor stereoselectivity may indeed reflect: (1) the weakening or loss of a single interaction involving one of the four groups bound to the asymmetric carbon; (2) steric hindrance preventing optimum interaction of the low affinity steroisomer with the receptor; and/or (3) the inversion of the relative positions of two moieties of the ligand with similar structural and electronic properties i.e. comparable affinities for the two corresponding subsites in the receptor.
authors.forename: M
authors.initials: M
authors.lastname: Waelbroeck
authors.forename: M
authors.initials: M
authors.lastname: Tastenoy
authors.forename: J
authors.initials: J
authors.lastname: Camus
authors.forename: R
authors.initials: R
authors.lastname: Feifel
authors.forename: E
authors.initials: E
authors.lastname: Mutschler
authors.forename: C
authors.initials: C
authors.lastname: Strohmann
authors.forename: R
authors.initials: R
authors.lastname: Tacke
authors.forename: G
authors.initials: G
authors.lastname: Lambrecht
authors.forename: J
authors.initials: J
authors.lastname: Christophe
mesh_terms: D000818:Animals; D006801:Humans; D010276:Parasympatholytics / Q000494:pharmacology*; D011976:Receptors, Muscarinic / Q000187:drug effects*; D013237:Stereoisomerism
chemical_list: D010276:Parasympatholytics; D011976:Receptors, Muscarinic