Title: Elevation of ligand binding to muscarinic M(2) acetylcholine receptors by bis(ammonio)alkane-type allosteric modulators Raasch A, Scharfenstein O, Trankle C, Holzgrabe U, Mohr K Ref: Journal of Medicinal Chemistry, 45:3809, 2002 : PubMed
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.
        
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Raasch A, Scharfenstein O, Trankle C, Holzgrabe U, Mohr K (2002) Elevation of ligand binding to muscarinic M(2) acetylcholine receptors by bis(ammonio)alkane-type allosteric modulators Journal of Medicinal Chemistry45: 3809-12
Raasch A, Scharfenstein O, Trankle C, Holzgrabe U, Mohr K (2002) Journal of Medicinal Chemistry45: 3809-12