Stereoselective interaction of procyclidine, hexahydro-difenidol, hexbutinol and oxyphencyclimine, and of related antagonists, with four muscarinic receptors
| Autor: | Ernst Mutschler, Jean Claude Camus, Michèle Tastenoy, Jean Christophe, Carsten Strohmann, Günter Lambrecht, Lise Schjelderup, Arne J. Aasen, Magali Waelbroeck, Reinhold Tacke |
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| Rok vydání: | 1992 |
| Předmět: |
Male
Eudysmic ratio Stereochemistry Scopolamine Derivatives In Vitro Techniques Oxyphencyclimine Tritium chemistry.chemical_compound Neuroblastoma Piperidines Muscarinic acetylcholine receptor medicine Animals Humans Anorganische Chemie Pancreas Pharmacology Chemistry Procyclidine Muscarinic acetylcholine receptor M3 Parasympatholytics Muscarinic acetylcholine receptor M2 Heart Rats Inbred Strains Stereoisomerism Muscarinic acetylcholine receptor M1 N-Methylscopolamine Receptors Muscarinic Corpus Striatum Rats Pyrimidines Alkynes ddc:540 Enantiomer medicine.drug |
| Zdroj: | European journal of pharmacology. 227(1) |
| ISSN: | 0014-2999 |
| Popis: | Wc invcstigatcd thc binding properlies of thc (R)- and (Sl-cnantiomcrs of thc muscarinic antagonists trihcxyphcnidyl, procyclidinc, hcxahydro-difcnidol. p-fluoro-hcxahydro-difcnidol. hcxbutinol, p-fluoro-hcxbutinnl. and thcir corrcsponding methiodidcs at muscarinic M\(_1\), M\(_2\)• M\(_3\) and M\(_4\) receptor subtypes. In addition. binding properlies of thc (R)- and (S)-cnantiomcrs of oxyphcncycliminc wcrc studicd. The {R)- cnantiomcrs (cutomcrs} of all the compounds had a grcatcr affinity than the (S)-isomcrs for thc four muscarinic rcccptor subtypcs. Thc binding pattcrns of thc (R)- and (S)-enantiomers wcrc gcncrally different. We did not obscrvc any gcncral corrclation hctwccn thc potcncy of thc high-affinity enantiomer and Lhc affinity ratio (cudismic ratio) of the two cnantiomcrs. Thc rcsuhs arc discusscd in tcrms of a 'four suhsitcs' binding modcl. |
| Databáze: | OpenAIRE |
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