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Targeting the 5-HT 2C Receptor in Biological Context and the Current State of 5-HT 2C Receptor Ligand Development

Authors
  • Wold, Eric A.1
  • Wild, Christopher T.1
  • Cunningham, Kathryn A.1
  • Zhou, Jia1
  • 1 Center for Addiction Research and Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, Texas 77555, USA
Type
Published Article
Journal
Current topics in medicinal chemistry
Publication Date
Jan 01, 2019
Volume
19
Issue
16
Pages
1381–1398
Identifiers
DOI: 10.2174/1568026619666190709101449
PMID: 31288724
PMCID: PMC6761005
Source
PubMed Central
Keywords
License
Unknown

Abstract

Serotonin (5-HT) 5-HT2C receptor (5-HT2CR) is recognized as a critical mediator of disease-related pathways and behaviors based upon actions in the central nervous system (CNS). Since 5-HT2CR is a class A G protein-coupled receptor (GPCR), drug discovery efforts have traditionally pursued the activation of the receptor through synthetic ligands with agonists proposed for the treatment of obesity, substance use disorders and impulse control disorders while antagonists may add value for the treatment of anxiety, depression and schizophrenia. The most significant agonist discovery to date is the FDA-approved anti-obesity medication lorcaserin. In recent years, efforts towards developing other mechanisms to enhance receptor function have resulted in the discovery of Positive Allosteric Modulators (PAMs) for the 5-HT2CR, with several molecule series now reported. The biological significance and context for signaling and function of the 5-HT2CR, and the current status of 5-HT2CR agonists and PAMs are discussed in this review.

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