Journal article
Current status of inverse agonism at serotonin(2A) (5-HT2A) and 5-HT2C receptors
Pharmacology & therapeutics (Oxford), v 121(2)
01 Feb 2009
PMID: 19109993
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
Contemporary receptor theory was developed to account for the existence of constitutive activity, as defined by the presence of receptor signaling in the absence of any ligand. Thus, ligands acting at a constitutively active receptor, can act as agonists, antagonists, and inverse agonists. In vitro studies have also revealed the complexity of ligand/receptor interactions including agonist-directed stimulus trafficking, a finding that has led to multi-active state models of receptor function. Studies with a variety of cell types have established that the serotonin 5-HT2A and 5-HT2C receptors also demonstrate constitutive activity and inverse agonism. However, until recently, there has been no evidence to suggest that these receptors also demonstrate constitutive activity and hence reveal inverse agonist properties of ligands in vivo. This paper describes our current knowledge of constitutive activity in vitro and then examines the evidence for constitutive activity in vivo. Both the seratonin 5-HT2A and 5-HT2C receptors are involved in a number of physiological and behavioral functions and are the targets for treatment of schizophrenia, anxiety, weight control, Parkinsonism, and other disorders. The existence of constitutive activity at these receptors in vivo, along with the possibility of inverse agonism, provides new avenues for drug development. (c) 2008 Elsevier Inc. All rights reserved.
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Details
- Title
- Current status of inverse agonism at serotonin(2A) (5-HT2A) and 5-HT2C receptors
- Creators
- V. J. Aloyo - Drexel UniversityK. A. Berg - The University of Texas Health Science Center at San AntonioU. Spampinato - Université Bordeaux SegalenW. P. Clarke - The University of Texas Health Science Center at San AntonioJ. A. Harvey - Drexel University
- Publication Details
- Pharmacology & therapeutics (Oxford), v 121(2)
- Publisher
- Elsevier
- Number of pages
- 14
- Grant note
- R01GM058652 / NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES; United States Department of Health & Human Services; National Institutes of Health (NIH) - USA; NIH National Institute of General Medical Sciences (NIGMS) R01MH016841 / NATIONAL INSTITUTE OF MENTAL HEALTH; United States Department of Health & Human Services; National Institutes of Health (NIH) - USA; NIH National Institute of Mental Health (NIMH) GM58652; MH16841-40 / National Institutes of Health; United States Department of Health & Human Services; National Institutes of Health (NIH) - USA Institut National de la Sante e de la Recherche Medicale (INSERM)Bordeaux 2 University; Institut National de la Sante et de la Recherche Medicale (Inserm)
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Pharmacology and Physiology
- Web of Science ID
- WOS:000264236100004
- Scopus ID
- 2-s2.0-59949102887
- Other Identifier
- 991019167579004721
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- Collaboration types
- Domestic collaboration
- International collaboration
- Web of Science research areas
- Pharmacology & Pharmacy