Stereoselective interaction of procyclidine, hexahydro-difenidol, hexbutinol and oxyphencyclimine, and of related antagonists, with four muscarinic receptors.
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Waelbroeck M, Camus J, Tastenoy M, Mutschler E, Strohmann C, Tacke R, Schjelderup L, Aasen A, Lambrecht G, Christophe J
Stereoselective interaction of procyclidine, hexahydro-difenidol, hexbutinol and oxyphencyclimine, and of related antagonists, with four muscarinic receptors.
Eur J Pharmacol. 1992 Sep 1;227(1):33-42.
- PubMed ID
- 1426023 [ View in PubMed]
- Abstract
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.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Oxyphencyclimine Muscarinic acetylcholine receptor M1 Protein Humans YesAntagonistDetails Oxyphencyclimine Muscarinic acetylcholine receptor M2 Protein Humans YesAntagonistDetails Oxyphencyclimine Muscarinic acetylcholine receptor M3 Protein Humans YesAntagonistDetails Procyclidine Muscarinic acetylcholine receptor M1 Protein Humans YesAntagonistDetails Procyclidine Muscarinic acetylcholine receptor M2 Protein Humans YesAntagonistDetails Procyclidine Muscarinic acetylcholine receptor M3 Protein Humans YesAntagonistDetails Procyclidine Muscarinic acetylcholine receptor M4 Protein Humans YesAntagonistDetails