Is there a role for 5-HT1A agonists in the treatment of depression?

Biological Psychiatry
Pierre Blier, Nick M Ward


The role of serotonin (5-hydroxytryptamine; 5-HT) in the treatment of depressive and anxiety disorders is underscored by the therapeutic action of selective 5-HT reuptake inhibitors acting to enhance the degree of activation of various 5-HT receptor subtypes. The 5-HT1A receptors are particularly relevant to the antidepressant and anxiolytic responses in human beings. They are located presynaptically in the raphe nuclei, where they act as cell body autoreceptors to inhibit the firing rate of 5-HT neurons, and are located postsynaptically in limbic and cortical regions, where they also attenuate firing activity. The azapirones are full agonists at 5-HT1A autoreceptors and are generally, but not exclusively, partial agonists at postsynaptic 5-HT1A receptors. Some of these drugs, including gepirone and other 5-HT1A agonists such as buspirone, have been reported to exert anxiolytic and antidepressive activity in double-blind, placebo-controlled, and comparative trials. Their delayed therapeutic activity is believed to result from increased activation of postsynaptic 5-HT1A receptors occurring only after 5-HT neurons regain their normal firing activity. The recovery of this parameter, which is attributable to 5-HT1A autoreceptor des...Continue Reading


Sep 2, 2006·Naunyn-Schmiedeberg's Archives of Pharmacology·Marie-Bernadette AssiéAdrian Newman-Tancredi
Mar 11, 2010·Psychopharmacology·Gregory V CarrIrwin Lucki
Nov 26, 2010·Psychopharmacology·Gregory V Carr, Irwin Lucki
Jun 11, 2005·Cell and Tissue Research·Monika Palchaudhuri, Gabriele Flügge
Nov 30, 2010·Bulletin of Experimental Biology and Medicine·D F AvgustinovichL A Koryakina
Aug 30, 2012·Journal of Molecular Neuroscience : MN·Dongjuan LiuYuxiu Shi
Aug 11, 2012·Acta neurologica Belgica·Saida HaiderDarakhshan Jabeen Haleem
Sep 1, 2003·Current Therapeutic Research, Clinical and Experimental·Louis F Fabre, Cees J Timmer
Mar 9, 2004·Journal of Psychiatric Research·Jay D AmsterdamMichael Gibertini
May 17, 2005·Neuroscience and Biobehavioral Reviews·Alasdair M Barr, Athina Markou
Apr 20, 2004·Progress in Neuro-psychopharmacology & Biological Psychiatry·Abdalla Salem Elhwuegi
Oct 28, 2011·Journal of Medicinal Chemistry·Isabel MarcoMaría L López-Rodríguez
Dec 4, 2013·Journal of Medicinal Chemistry·Ferdinando FiorinoElisa Perissutti
Sep 21, 2013·Journal of Medicinal Chemistry·Margarita ValhondoMaría L López-Rodríguez
Dec 17, 2009·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Jens BenninghoffAngelo Luigi Vescovi
Jun 26, 2009·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Joshua GreeneRonald S Duman
Sep 9, 2011·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Xiaohua LiRichard C Shelton
Jul 14, 2005·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Erika Estrada-CamarenaCarolina López-Rubalcava
Oct 21, 2005·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Laurent BardinAdrian Newman-Tancredi
Mar 14, 2007·Behavioural Pharmacology·Darakhshan Jabeen HaleemMuhammad Abdul Haleem
Apr 22, 2011·Exercise and Sport Sciences Reviews·Benjamin N Greenwood, Monika Fleshner
Nov 20, 2013·International Clinical Psychopharmacology·Arif KhanDonald S Robinson
Jul 25, 2012·Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences·Paul R Albert
Dec 23, 2006·Clinical and Experimental Pharmacology & Physiology·Eugene Nalivaiko
Apr 19, 2007·Clinical and Experimental Pharmacology & Physiology·L Sanjay NandamPerry Bartlett
Apr 19, 2008·American Journal of Alzheimer's Disease and Other Dementias·Lauren Massimo, Murray Grossman
May 31, 2011·Molecular Brain·Paul R AlbertAnne M Millar
Jun 24, 2008·Neuropsychiatric Disease and Treatment·Francis E Lotrich, Bruce G Pollock


May 1, 1992·Progress in Neuro-psychopharmacology & Biological Psychiatry·Jay D Amsterdam
Jun 1, 1990·Journal of Clinical Psychopharmacology·Pierre Blier, C de Montigny
Jun 11, 1990·Journal of Clinical Psychopharmacology·S W JenkinsL A Reich
Jan 1, 1990·European Journal of Clinical Pharmacology·G S RuigtH A Kamphuisen
Mar 15, 1988·European Journal of Pharmacology·F GilbertS M Stahl
Oct 1, 1994·Journal of Clinical Psychopharmacology·P J McGrathD S Robinson
Oct 1, 1993·Naunyn-Schmiedeberg's Archives of Pharmacology·T SharpS Hjorth
Jul 1, 1994·Trends in Pharmacological Sciences·Pierre Blier, C de Montigny
Jul 1, 1993·Journal of Clinical Pharmacology·L K TayK A Pittman
Oct 1, 1995·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·B SelettiC de Montigny
May 1, 1997·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Pierre BlierC de Montigny
Apr 1, 1997·Reviews in the Neurosciences·L E RueterB L Jacobs
Dec 31, 1997·Journal of Clinical Psychopharmacology·R ZanardiJ Perez
Aug 1, 1997·The Journal of Clinical Psychiatry·S M Stahl
Oct 2, 1998·Archives of Family Medicine·E H LinE Ludman
Aug 5, 1999·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·E Gould
Mar 4, 2000·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·M UhrF Holsboer
Aug 16, 2000·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·E A RabinerP M Grasby

Related Concepts

Involutional Paraphrenia
Serotonin Measurement
Anti-Anxiety Effect
Receptors, Tryptamine
Receptor, Serotonin,5-HT1A

Trending Feeds


Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Synapse Loss as Therapeutic Target in MS

As we age, the number of synapses present in the human brain starts to decline, but in neurodegenerative diseases this occurs at an accelerated rate. In MS, it has been shown that there is a reduction in synaptic density, which presents a potential target for treatment. Here is the latest research on synapse loss as a therapeutic target in MS.

Artificial Intelligence in Cardiac Imaging

Artificial intelligence (ai) techniques are increasingly applied to cardiovascular (cv) medicine in cardiac imaging analysis. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

Social Learning

Social learning involves learning new behaviors through observation, imitation and modeling. Follow this feed to stay up to date on the latest research.

Cell Atlas of the Human Eye

Constructing a cell atlas of the human eye will require transcriptomic and histologic analysis over the lifespan. This understanding will aid in the study of development and disease. Find the latest research pertaining to the Cell Atlas of the Human Eye here.

Single Cell Chromatin Profiling

Techniques like ATAC-seq and CUT&Tag have the potential to allow single cell profiling of chromatin accessibility, histones, and TFs. This will provide novel insight into cellular heterogeneity and cell states. Discover the latest research on single cell chromatin profiling here.

Genetic Screens in iPSC-derived Brain Cells

Genetic screening is a critical tool that can be employed to define and understand gene function and interaction. This feed focuses on genetic screens conducted using induced pluripotent stem cell (iPSC)-derived brain cells.