Stereoselectivity of (R)- and (S)-hexahydro-difenidol binding to neuroblastoma M1, cardiac M2, pancreatic M3, and striatum M4 muscarinic receptors
| Autor: | Jean Claude Camus, Ernst Mutschler, Carsten Strohmann, Magali Waelbroeck, Michèle Tastenoy, Günter Lambrecht, Jean Christophe, Reinhold Tacke |
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| Rok vydání: | 1991 |
| Předmět: |
Male
Stereochemistry Binding Competitive Catalysis Analytical Chemistry Neuroblastoma Piperidines Drug Discovery Muscarinic acetylcholine receptor Animals Humans Anorganische Chemie Binding site Receptor Pancreas Spectroscopy Acetylcholine receptor Pharmacology Chemistry Myocardium Organic Chemistry Muscarinic acetylcholine receptor M3 Muscarinic acetylcholine receptor M2 Rats Inbred Strains Stereoisomerism Muscarinic acetylcholine receptor M1 Receptors Muscarinic Corpus Striatum Rats ddc:540 Stereoselectivity |
| Zdroj: | Chirality. 3(2) |
| ISSN: | 0899-0042 |
| Popis: | (R)-Hexahydro-difenidol has a higher affinity for M\(_1\) receptors in NB-OK 1 cells, pancreas M\(_3\) and striatum M\(_4\) receptors (pKi 7.9 to 8.3) than for cardiac M2 receptors (pKi 7 .0). (8)-Hexahydro-difenidol, by contrast, is nonselective (pKi 5.8 to 6.1). Our goal in the present study was to evaluate the importance ofthe hydrophobic phenyl, and cyclohexyl rings of hexahydro-difenidol for the stereoselectivity and reeeptor selectivity of hexahydro-difenidol binding to the four muscarinic receptors. Our results indieated that replacement of the phenyl ring of hexahydro-difenidol by a cyclohexyl group |
| Databáze: | OpenAIRE |
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