ALLOSTERIC SITES ON MUSCARINIC RECEPTORS

摘要

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