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Stereoselective interaction of procyclidine, hexahydro-difenidol, hexbutinol and oxyphencyclimine, and of related antagonists, with four muscarinic receptors

par Waelbroeck, Magali ;Camus, Jean Claude ;Tastenoy, Michèle ;Mutschler, Ernst;Strohmann, C.;Tacke, Reinhold;Schjelderup, Lise;Aasen, A.;Lambrecht, Günter;Christophe, Jean
Référence European Journal of Pharmacology - Molecular Pharmacology Section, 227, 1, page (33-42)
Publication Publié, 1992

Article révisé par les pairs

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Résumé :

We investigated the binding properties of the (R)- and (S)-enantiomers of the muscarinic antagonists trihexyphenidyl, procyclidine, hexahydro-difenidol, p-fluoro-hexahydro-difenidol, hexbutinol, p-fluoro-hexbutinol, and their corresponding methiodides at muscarinic M1, M2, M3 and M4 receptor subtypes. In addition, binding properties of the (R)- and (S)-enantiomers of oxyphencyclimine were studied. The (R)-enantiomers (eutomers) of all the compounds had a greater affinity than the (S)-isomers for the four muscarinic receptor subtypes. The binding patterns of the (R)- and (S)-enantiomers were generally different. We did not observe any general correlation between the potency of the high-affinity enantiomer and the affinity ratio (eudismic ratio) of the two enantiomers. The results are discussed in terms of a 'four subsites' binding model.