Targeting the 5-HT2C Receptor in Biological Context and the Current State of 5-HT2C Receptor Ligand Development.
5-HT2C receptor
Agonists
Allosteric modulation
Central nervous system disorders
Drug discovery
Ligand development
Neurotherapeutics
Pharmacological probes
Positive allosteric modulators
Signaling bias
Target selectivity.
Journal
Current topics in medicinal chemistry
ISSN: 1873-4294
Titre abrégé: Curr Top Med Chem
Pays: United Arab Emirates
ID NLM: 101119673
Informations de publication
Date de publication:
2019
2019
Historique:
received:
28
03
2019
revised:
14
05
2019
accepted:
16
05
2019
pubmed:
11
7
2019
medline:
29
10
2019
entrez:
11
7
2019
Statut:
ppublish
Résumé
Serotonin (5-HT) 5-HT2C receptor (5-HT2CR) is recognized as a critical mediator of diseaserelated 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 FDAapproved 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.
Identifiants
pubmed: 31288724
pii: CTMC-EPUB-99490
doi: 10.2174/1568026619666190709101449
pmc: PMC6761005
mid: NIHMS1050909
doi:
Substances chimiques
Ligands
0
Receptor, Serotonin, 5-HT2C
0
Serotonin 5-HT2 Receptor Agonists
0
Serotonin 5-HT2 Receptor Antagonists
0
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
1381-1398Subventions
Organisme : NIDA NIH HHS
ID : F31 DA038922
Pays : United States
Organisme : NIDA NIH HHS
ID : F31 DA045511
Pays : United States
Organisme : NIDA NIH HHS
ID : R01 DA038446
Pays : United States
Organisme : NIDA NIH HHS
ID : T32 DA007287
Pays : United States
Informations de copyright
Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.
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