Elevation of ligand binding to muscarinic M(2) acetylcholine receptors by bis(ammonio)alkane-type allosteric modulators |
| |
Authors: | Raasch Alexandra Scharfenstein Olaf Tränkle Christian Holzgrabe Ulrike Mohr Klaus |
| |
Institution: | Pharmacology and Toxicology, Institute of Pharmacy, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany. |
| |
Abstract: | Bis(ammonio)alkane-type compounds are archetypal muscarinic allosteric modulators. Phthalimido-substituted hexane-bis-ammonium agents were methylated in the phthalimide moieties and the lateral propyl side chains. All compounds retarded allosterically the dissociation of the orthosteric ligand (3)H]N-methylscopolamine ((3)H]NMS) from porcine heart M(2) receptors. (3)H]NMS equilibrium binding was reduced, left unaltered, or elevated, depending on the degree and position of methylation. This is the first time that an allosteric elevation of ligand binding is demonstrated for bis(ammonio)alkane-type compounds. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|