InterPro : IPR000610

Name  5-Hydroxytryptamine 1A receptor Short Name  5HT1A_rcpt
Type  Family Description  5-hydroxytryptamine (5-HT) or serotonin, is a neurotransmitter that it is primarily found in the gastrointestinal (GI) tract, platelets, and in the central nervous system (CNS). It is implicated in a vast array of physiological and pathophysiological pathways. Receptors for 5-HT mediate both excitatory and inhibitory neurotransmission, and modulate the release of many neurotransmitters including glutamate, GABA, dopamine, epinephrine/norepinephrine, and acetylcholine, as well as many hormones, including oxytocin, prolactin, vasopressin and cortisol. In the CNS, 5-HT receptors can influence various neurological processes, such as aggression, anxiety and appetite and, as a, result are the target of a variety of pharmaceutical drugs, including many antidepressants, antipsychotics and anorectics []. The 5-HT receptors are grouped into a number of distinct subtypes, classified according to their antagonist susceptibilities and their affinities for 5-HT. With the exception of the 5-HT3 receptor, which is a ligand-gated ion channel [], all 5-HT receptors are members of the rhodopsin-like G protein-coupled receptor family [], and they activate an intracellular second messenger cascade to produce their responses. The 5-HT1 receptors are a subfamily of 5-HT receptors that were originally classified according to their inhibition of adenylyl cyclase, degree of sequence similarity and their overlapping pharmacological specificities. The subfamily is comprised of five different receptors 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT1F, and they can couple to Gi/Go and mediate inhibitory neurotransmission, although signalling via other transduction systems are known. One of the 5-HT1 receptors, the 5-HT1E receptor, is yet to achieve receptor status from the International Union of Basic and Clinical Pharmacology (IUPHAR), since a robust response mediated via the protein has not been reported in the literature.5-HT1A receptors are the most widespread of all the 5-HT receptors. They are found pre- and post-synaptically [, , , ]: in the raphe nuclei they are somatodendritic and act as autoreceptors to inhibit cell firing; whereas postsynaptic 5-HT1A receptors are present in a number of limbic structures, particularly the hippocampus [, , ]. 5-HT1A receptors are involved in many neuromodulative processes, and are potential anxiolytic and hypertensive targets [, , , ]. Receptor antagonists like buspirone []and flesinoxan []have been shown to relieve anxiety [, ]and depression [, ]. Other 5-HT1A receptor agonists decrease blood pressure and heart rate via a central mechanism, by inducing peripheral vasodilation []. This also increases heat dissipation from the organism, causing a decrease in body temperature [, ]. 5-HT1A receptors have been implicated in the neuroendocrine regulation of adrenocorticotrophic hormone (ACTH) []. In the CNS, 5-HT1A receptors exist in the cerebral cortex, hippocampus, septum, amygdala, and in the raphe nucleus in high densities, whilst lower amounts also exist in the basal ganglia and thalamus [, ].
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Id Name Short Name Type
IPR002231 5-hydroxytryptamine receptor family 5HT_rcpt Family

23 Publications

First Author Title Year Journal Volume Pages
Nichols DE Serotonin receptors. 2008 Chem Rev 108 1614-41
Reeves DC The molecular basis of the structure and function of the 5-HT3 receptor: a model ligand-gated ion channel (review). 2002 Mol Membr Biol 19 11-26
Burnet PW The distribution of 5-HT1A and 5-HT2A receptor mRNA in human brain. 1995 Brain Res 676 157-68
Ito H Localization of 5-HT1A receptors in the living human brain using [carbonyl-11C]WAY-100635: PET with anatomic standardization technique. 1999 J Nucl Med 40 102-9
de Almeida J Serotonin 1A receptors in human and monkey prefrontal cortex are mainly expressed in pyramidal neurons and in a GABAergic interneuron subpopulation: implications for schizophrenia and its treatment. 2008 J Neurochem 107 488-96
Raymond JR Immunohistochemical mapping of cellular and subcellular distribution of 5-HT1A receptors in rat and human kidneys. 1993 Am J Physiol 264 F9-19
Aznar S The 5-HT1A serotonin receptor is located on calbindin- and parvalbumin-containing neurons in the rat brain. 2003 Brain Res 959 58-67
Laporte AM Autoradiographic mapping of serotonin 5-HT1A, 5-HT1D, 5-HT2A and 5-HT3 receptors in the aged human spinal cord. 1996 J Chem Neuroanat 11 67-75
Albert PR Cloning, functional expression, and mRNA tissue distribution of the rat 5-hydroxytryptamine1A receptor gene. 1990 J Biol Chem 265 5825-32
Pompeiano M Distribution and cellular localization of mRNA coding for 5-HT1A receptor in the rat brain: correlation with receptor binding. 1992 J Neurosci 12 440-53
Schreiber R 5-HT1A receptor ligands in animal models of anxiety, impulsivity and depression: multiple mechanisms of action? 1993 Prog Neuropsychopharmacol Biol Psychiatry 17 87-104
Cohn JB A pooled, double-blind comparison of the effects of buspirone, diazepam and placebo in women with chronic anxiety. 1989 Curr Med Res Opin 11 304-20
Cryan JF The effects of the 5-HT1A agonist flesinoxan, in three paradigms for assessing antidepressant potential in the rat. 1997 Eur Neuropsychopharmacol 7 109-14
Parks CL Increased anxiety of mice lacking the serotonin1A receptor. 1998 Proc Natl Acad Sci U S A 95 10734-9
Tunnicliff G Molecular basis of buspirone's anxiolytic action. 1991 Pharmacol Toxicol 69 149-56
Kennett GA Antidepressant-like action of 5-HT1A agonists and conventional antidepressants in an animal model of depression. 1987 Eur J Pharmacol 134 265-74
Den Boer JA Serotonergic drugs in the treatment of depressive and anxiety disorders. 2000 Hum Psychopharmacol 15 315-336
Heisler LK Elevated anxiety and antidepressant-like responses in serotonin 5-HT1A receptor mutant mice. 1998 Proc Natl Acad Sci U S A 95 15049-54
Li Q Medial hypothalamic 5-hydroxytryptamine (5-HT)1A receptors regulate neuroendocrine responses to stress and exploratory locomotor activity: application of recombinant adenovirus containing 5-HT1A sequences. 2004 J Neurosci 24 10868-77
Osei-Owusu P 5-Hydroxytryptamine 1A receptors in the paraventricular nucleus of the hypothalamus mediate oxytocin and adrenocorticotropin hormone release and some behavioral components of the serotonin syndrome. 2005 J Pharmacol Exp Ther 313 1324-30
Dabiré H Central 5-hydroxytryptamine (5-HT) receptors in blood pressure regulation. 1991 Therapie 46 421-9
Ootsuka Y Activation of 5-HT1A receptors in rostral medullary raphé inhibits cutaneous vasoconstriction elicited by cold exposure in rabbits. 2006 Brain Res 1073-1074 252-61
Rusyniak DE 3,4-Methylenedioxymethamphetamine- and 8-hydroxy-2-di-n-propylamino-tetralin-induced hypothermia: role and location of 5-hydroxytryptamine 1A receptors. 2007 J Pharmacol Exp Ther 323 477-87



To cite PlanMine, please refer to the following publication:

Rozanski, A., Moon, H., Brandl, H., Martín-Durán, J. M., Grohme, M., Hüttner, K., Bartscherer, K., Henry, I., & Rink, J. C.
PlanMine 3.0—improvements to a mineable resource of flatworm biology and biodiversity
Nucleic Acids Research, gky1070. doi:10.1093/nar/gky1070 (2018)