CHAPTER 8: Muscarinic Receptors Allosteric Modulation

Bruce J. Melancon, Corey R. Hopkins

Research output: Chapter in Book/Report/Conference proceedingChapter

Abstract

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.

Original languageEnglish (US)
Title of host publicationAllosterism in Drug Discovery
EditorsDario Doller
PublisherRoyal Society of Chemistry
Pages175-193
Number of pages19
Edition56
DOIs
StatePublished - 2017

Publication series

NameRSC Drug Discovery Series
Number56
Volume2017-January
ISSN (Print)2041-3203
ISSN (Electronic)2041-3211

ASJC Scopus subject areas

  • Drug Discovery

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  • Cite this

    Melancon, B. J., & Hopkins, C. R. (2017). CHAPTER 8: Muscarinic Receptors Allosteric Modulation. In D. Doller (Ed.), Allosterism in Drug Discovery (56 ed., pp. 175-193). (RSC Drug Discovery Series; Vol. 2017-January, No. 56). Royal Society of Chemistry. https://doi.org/10.1039/9781782629276-00175