CHAPTER 8: Muscarinic Receptors Allosteric Modulation Check Access

This chapter describes recent activity in the advancement of ligands and therapeutic lead compounds for the allosteric modulation of the muscarinic receptors and their potential utility as therapies for central nervous system (CNS) disorders. The chapter reviews the activity over the past five years of allosteric modulation of the muscarinic receptor subtypes M₁ and M₄, along with giving a brief overview of the M₅ subtype. Due to concerns about off-target effects and toxicity with orthosteric modulators, much attention has concentrated on positive and negative allosteric modulators of these receptors in order to identify more selective lead compounds. Recent efforts have afforded a variety of improvements in potency and selectivity and pharmacokinetic properties that warrant further investigation and optimization.