Lorcaserin and pimavanserin: Emerging selectivity of serotonin receptor subtype-targeted drugs

Herbert Y Meltzer, Bryan L. Roth*

*Corresponding author for this work

Research output: Contribution to journalReview article

55 Citations (Scopus)

Abstract

Serotonin (5-hydroxytryptamine, or 5-HT) receptors mediate a plethora of physiological phenomena in the brain and the periphery. Additionally, serotonergic dysfunction has been implicated in nearly every neuropsychiatric disorder. The effects of serotonin are mediated by fourteen GPCRs. Both the therapeutic actions and side effects of commonly prescribed drugs are frequently due to nonspecific actions on various 5-HT receptor subtypes. For more than 20 years, the search for clinically efficacious drugs that selectively target 5-HT receptor subtypes has been only occasionally successful. This review provides an overview of 5-HT receptor pharmacology and discusses two recent 5-HT receptor subtype-selective drugs, lorcaserin and pimavanserin, which target the 5HT2C and 5HT2A receptors and provide new treatments for obesity and Parkinson's disease psychosis, respectively.

Original languageEnglish (US)
Pages (from-to)4986-4991
Number of pages6
JournalJournal of Clinical Investigation
Volume123
Issue number12
DOIs
StatePublished - Dec 2 2013

Fingerprint

Serotonin Receptors
Serotonin
Pharmaceutical Preparations
Physiological Phenomena
Psychotic Disorders
Parkinson Disease
Obesity
lorcaserin
Pimavanserin
Pharmacology
Brain

ASJC Scopus subject areas

  • Medicine(all)

Cite this

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abstract = "Serotonin (5-hydroxytryptamine, or 5-HT) receptors mediate a plethora of physiological phenomena in the brain and the periphery. Additionally, serotonergic dysfunction has been implicated in nearly every neuropsychiatric disorder. The effects of serotonin are mediated by fourteen GPCRs. Both the therapeutic actions and side effects of commonly prescribed drugs are frequently due to nonspecific actions on various 5-HT receptor subtypes. For more than 20 years, the search for clinically efficacious drugs that selectively target 5-HT receptor subtypes has been only occasionally successful. This review provides an overview of 5-HT receptor pharmacology and discusses two recent 5-HT receptor subtype-selective drugs, lorcaserin and pimavanserin, which target the 5HT2C and 5HT2A receptors and provide new treatments for obesity and Parkinson's disease psychosis, respectively.",
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Lorcaserin and pimavanserin : Emerging selectivity of serotonin receptor subtype-targeted drugs. / Meltzer, Herbert Y; Roth, Bryan L.

In: Journal of Clinical Investigation, Vol. 123, No. 12, 02.12.2013, p. 4986-4991.

Research output: Contribution to journalReview article

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