Inverse agonists - what do they mean for psychiatry?

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Title: Inverse agonists - what do they mean for psychiatry?
Author(s): Nutt, D
Stahl, S
Blier, P
Drago, F
Zohar, J
Wilson, S
Item Type: Journal Article
Abstract: The nomenclature of drugs is a critical aspect of science, since it can direct research and optimize treatment choices. Traditionally drugs acting on CNS receptors have been classified as either agonists or antagonists. Recently a new class of ligand, the inverse agonist, has been identified in some receptor systems. Inverse agonists have opposite actions to those of agonists but the effects of both of these can be blocked by antagonists. Pimavanserin is a new 5-HT2A receptor acting drug that has been given market authorization for psychosis in Parkinson׳s disease. The FDA have termed it an inverse agonist, but this conclusion is based on in-vitro data. In this paper we discuss the evidence for such a claim being made for pimavanserin in the human brain and conclude that this is not currently sufficient. It is therefore premature to conclude that the actions of pimavanserin in humans are due to inverse agonism, and we are of the opinion that it should be called a 5-HT2A antagonist until better evidence emerges.
Publication Date: 7-Dec-2016
Date of Acceptance: 21-Nov-2016
URI: http://hdl.handle.net/10044/1/43624
DOI: https://dx.doi.org/10.1016/j.euroneuro.2016.11.013
ISSN: 1873-7862
Publisher: Elsevier
Start Page: 87
End Page: 90
Journal / Book Title: European Neuropsychopharmacology
Volume: 27
Issue: 1
Copyright Statement: © 2016 Published by Elsevier B.V. This manuscript is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International http://creativecommons.org/licenses/by-nc-nd/4.0/
Keywords: Science & Technology
Life Sciences & Biomedicine
Clinical Neurology
Neurosciences
Pharmacology & Pharmacy
Psychiatry
Neurosciences & Neurology
Inverse agonist
Antagonist
Serotonin
5-HT2A
5-HT2A RECEPTOR
PIMAVANSERIN
RISPERIDONE
EFFICACY
SLEEP
5-HT2A
Antagonist
Inverse agonist
Serotonin
Psychiatry
11 Medical And Health Sciences
17 Psychology And Cognitive Sciences
Publication Status: Published
Conference Place: Netherlands
Appears in Collections:Department of Medicine
Faculty of Medicine



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