21093-51-6Relevant articles and documents
Elevation of ligand binding to muscarinic M2 acetylcholine receptors by bis(ammonio)alkane-type allosteric modulators
Raasch, Alexandra,Scharfenstein, Olaf,Tr?nkle, Christian,Holzgrabe, Ulrike,Mohr, Klaus
, p. 3809 - 3812 (2002)
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 [3H]N-methylscopolamine ([3H]NMS) from porcine heart M2 receptors. [3H]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.
A fast and efficient track to allosteric modulators of muscarinic receptors: Microwave-assisted syntheses
Schmitz, Jens,Heller, Eberhard,Holzgrabe, Ulrike
, p. 171 - 174 (2008/02/01)
By using microwave irradiation bisammonium-and bispyridinium-type allosteric modulators of muscarinic receptors can be obtained fast and efficiently.
