ALLOSTERIC MODULATORS OF LIGAND-BINDING TO MUSCARINIC ACETYLCHOLINE-RECEPTORS

Allosteric modulators of muscarinic receptors act at a site apart from the common ligand binding site of the receptor protein. These compoun ds affect both of the molecular events that determine the level of equ ilibrium binding, namely ligand association and dissociation. As a con sequence, ligand binding can be elevated, reduced or remain unchanged, depending on the receptor subtype, the type of ligand and the type of allosteric modulator. Thus, allosterically acting drugs represent a n ovel approach for affecting muscarinic receptors, Notably, they may ac t as subtype-selective enhancers of acetylcholine binding. This might be exploited therapeutically, to improve cognition or to promote antin ociception, for example.