Elevation of ligand binding to muscarinic M2 acetylcholine receptors by bis(ammonio)alkane-type allosteric modulators
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.
Raasch, Alexandra,Scharfenstein, Olaf,Tr?nkle, Christian,Holzgrabe, Ulrike,Mohr, Klaus
Real time observation of microwave-enhanced reactions via fast FTIR spectroscopy
Microwave-enhanced reactions are very fast in comparison to thermal reactions. The determination of optimal end point often fails because conventional analytical methods are too slow. Therefore, we established a fast method using FTIR spectroscopy. The re