ALLOSTERIC SITES ON MUSCARINIC RECEPTORS

摘要

An allosteric site on muscarinic receptors is disclosed, together with its usefor screening for compounds capable of modulating the binding of a primaryligand such as acetylcholine to the receptor. The site is characterised hereina series of indolocarbazoles represented by formula (1) and a series ofrelated compounds represented by formula (2). These compounds are capable ofbinding to the allosteric site to modulate the binding of a primary ligand tothe receptors, showing positive, negative and neutral cooperativity andselectivity for muscarinic receptor subtypes.