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Stereoselectivity of the interaction of muscarinic antagonists with their receptors

par Waelbroeck, Magali ;Tastenoy, Michèle ;Camus, Jean Claude ;Feifel, Roland;Mutschler, Ernst;Tacke, Reinhold;Lambrecht, Günter;Christophe, Jean ;Strohmann, Carsten
Référence Trends in pharmacological sciences, 10, SUPPL., page (65-69)
Publication Publié, 1989

Article révisé par les pairs

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Résumé :

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.