5-HT1A-рецептор: различия между версиями

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{{DISPLAYTITLE:5-HT<sub>1A</sub>-рецептор}}
#REDIRECT [[5-HT1 рецепторы]]
{{редактирую|1=[[Служебная:Contributions/Роман Беккер|Роман Беккер]]|2=16 февраля 2015|details=}}

The '''5-HT<sub>1A</sub> receptor''' is a subtype of [[5-HT receptor]] that binds the [[endogenous]] [[neurotransmitter]] [[serotonin]] (5-hydroxytryptamine, 5-HT). It is a [[G protein-coupled receptor]] (GPCR) that is coupled to [[Gi alpha subunit|G<sub>i</sub>/G<sub>o</sub>]] and mediates [[IPSP|inhibitory]] [[neurotransmission]]. ''HTR1A'' denotes the [[human]] [[gene]] encoding for the [[Receptor (biochemistry)|receptor]].<ref name="pmid2591972">{{cite journal | authors = Gilliam TC, Freimer NB, Kaufmann CA, Powchik PP, Bassett AS, Bengtsson U, Wasmuth JJ | title = Deletion mapping of DNA markers to a region of chromosome 5 that cosegregates with schizophrenia | journal = Genomics | volume = 5 | issue = 4 | pages = 940-4 | year = 1989 | date = November 1989 | pmid = 2591972 | pmc = 3154173 | doi = 10.1016/0888-7543(89)90138-9 }}</ref><ref name="entrez">{{cite web | title = Entrez Gene: HTR1A 5-hydroxytryptamine (serotonin) receptor 1A | url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=3350 }}</ref>

== Распределение в организме ==

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The 5-HT<sub>1A</sub> receptor is the most widespread of all the 5-HT receptors. In the [[central nervous system]], 5-HT<sub>1A</sub> receptors exist in the [[cerebral cortex]], [[hippocampus]], [[Septum pellucidum|septum]], [[amygdala]], and [[Raphe nuclei|raphe nucleus]] in high densities, while low amounts also exist in the [[basal ganglia]] and [[thalamus]].<ref name="pmid9935065">{{cite journal | authors = Ito H, Halldin C, Farde L | title = Localization of 5-HT1A receptors in the living human brain using [carbonyl-11C]WAY-100635: PET with anatomic standardization technique | journal = J. Nucl. Med. | volume = 40 | issue = 1 | pages = 102-9 | year = 1999 | pmid = 9935065 }}</ref><ref name="urlSerotonin Receptor Subtypes and Ligands">{{cite web | url = http://www.acnp.org/g4/GN401000039/Ch039.html | title = Serotonin Receptor Subtypes and Ligands | accessdate = 2008-04-11 | author = Glennon RA, Dukat M, Westkaemper RB | date = 2000-01-01 | publisher = American College of Neurophyscopharmacology | archiveurl= http://web.archive.org/web/20080421160353/http://www.acnp.org/g4/GN401000039/Ch039.html| archivedate= 21 April 2008 | deadurl= no}}</ref><ref name="pmid18761712">{{cite journal | authors = de Almeida J, Mengod G | title = 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 | journal = J. Neurochem. | volume = 107 | issue = 2 | pages = 488-96 | year = 2008 | pmid = 18761712 | doi = 10.1111/j.1471-4159.2008.05649.x }}</ref> The 5-HT<sub>1A</sub> receptors in the raphe nucleus are largely [[somatodendritic]] [[autoreceptor]]s, whereas those in other areas such as the hippocampus are [[postsynaptic]] receptors.<ref name="urlSerotonin Receptor Subtypes and Ligands"/>

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== Физиологическая роль ==

=== Нейромодуляция ===

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5-HT<sub>1A</sub> [[Receptor (biochemistry)|receptor]] [[agonist]]s are involved in [[Neuromodulation (medicine)|neuromodulation]]. They decrease [[blood pressure]] and [[heart rate]] via a central mechanism, by inducing [[peripheral]] [[vasodilation]], and by stimulating the [[vagus nerve]].<ref name="pmid1819150">{{cite journal | authors = Dabiré H | title = Central 5-hydroxytryptamine (5-HT) receptors in blood pressure regulation | journal = Therapie | volume = 46 | issue = 6 | pages = 421-9 | year = 1991 | pmid = 1819150 }}</ref> These effects are the result of activation of 5-HT<sub>1A</sub> receptors within the [[rostral ventrolateral medulla]].<ref name="pmid1819150"/> The [[sympatholytic]] [[antihypertensive]] [[drug]] [[urapidil]] is an [[α1-adrenergic receptor|α<sub>1</sub>-adrenergic receptor]] [[receptor antagonist|antagonist]] and [[α2-adrenergic receptor|α<sub>2</sub>-adrenergic receptor]] agonist, as well as 5-HT<sub>1A</sub> receptor agonist, and it has been demonstrated that the latter property contributes to its overall therapeutic effects.<ref name="pmid1855130">{{cite journal | authors = Ramage AG | title = The mechanism of the sympathoinhibitory action of urapidil: role of 5-HT1A receptors | journal = Br. J. Pharmacol. | volume = 102 | issue = 4 | pages = 998-1002 | year = 1991 | date = April 1991 | pmid = 1855130 | pmc = 1917978 | doi = 10.1111/j.1476-5381.1991.tb12290.x }}</ref><ref name="pmid2569265">{{cite journal | authors = Kolassa N, Beller KD, Sanders KH | title = Involvement of brain 5-HT1A receptors in the hypotensive response to urapidil | journal = Am. J. Cardiol. | volume = 64 | issue = 7 | pages = 7D-10D | year = 1989 | pmid = 2569265 | doi = 10.1016/0002-9149(89)90688-7 }}</ref> Vasodilation of the [[blood vessel]]s in the [[skin]] via central 5-HT<sub>1A</sub> activation increases [[heat]] [[heat transfer|dissipation]] from the organism out into the environment, causing a decrease in [[body temperature]].<ref name="pmid16455061">{{cite journal | authors = Ootsuka Y, Blessing WW | title = Activation of 5-HT1A receptors in rostral medullary raphé inhibits cutaneous vasoconstriction elicited by cold exposure in rabbits | journal = Brain Res. | volume = 1073-1074 | pages = 252-61 | year = 2006 | pmid = 16455061 | doi = 10.1016/j.brainres.2005.12.031 }}</ref><ref name="pmid17702902">{{cite journal | authors = Rusyniak DE, Zaretskaia MV, Zaretsky DV, DiMicco JA | title = 3,4-Methylenedioxymethamphetamine- and 8-hydroxy-2-di-n-propylamino-tetralin-induced hypothermia: role and location of 5-hydroxytryptamine 1A receptors | journal = J. Pharmacol. Exp. Ther. | volume = 323 | issue = 2 | pages = 477-87 | year = 2007 | pmid = 17702902 | doi = 10.1124/jpet.107.126169 }}</ref>

Activation of central 5-HT<sub>1A</sub> receptors triggers the release or inhibition of [[norepinephrine]] depending on species, presumably from the [[locus coeruleus]], which then reduces or increases neuronal tone to the [[iris sphincter muscle]] by modulation of [[postsynaptic]] [[α2-adrenergic receptor|α<sub>2</sub>-adrenergic receptor]]s within the [[Edinger-Westphal nucleus]], resulting in [[mydriasis|pupil dilation]] in [[rodent]]s, and [[miosis|pupil constriction]] in [[primate]]s including [[human]]s.<ref name="pmid15087245">{{cite journal | authors = Yu Y, Ramage AG, Koss MC | title = Pharmacological studies of 8-OH-DPAT-induced pupillary dilation in anesthetized rats | journal = Eur. J. Pharmacol. | volume = 489 | issue = 3 | pages = 207-13 | year = 2004 | pmid = 15087245 | doi = 10.1016/j.ejphar.2004.03.007 }}</ref><ref name="pmid8982715">{{cite journal | authors = Prow MR, Martin KF, Heal DJ | title = 8-OH-DPAT-induced mydriasis in mice: a pharmacological characterisation | journal = Eur. J. Pharmacol. | volume = 317 | issue = 1 | pages = 21-8 | year = 1996 | pmid = 8982715 | doi = 10.1016/S0014-2999(96)00693-0 }}</ref><ref name="pmid7697953">{{cite journal | authors = Fanciullacci M, Sicuteri R, Alessandri M, Geppetti P | title = Buspirone, but not sumatriptan, induces miosis in humans: relevance for a serotoninergic pupil control | journal = Clin. Pharmacol. Ther. | volume = 57 | issue = 3 | pages = 349-55 | year = 1995 | date = March 1995 | pmid = 7697953 | doi = 10.1016/0009-9236(95)90161-2 }}</ref>

5-HT<sub>1A</sub> receptor agonists like [[buspirone]]<ref>{{cite journal | authors = Cohn JB, Rickels K | title = A pooled, double-blind comparison of the effects of buspirone, diazepam and placebo in women with chronic anxiety | journal = Curr Med Res Opin | volume = 11 | issue = 5 | pages = 304-20 | year = 1989 | pmid = 2649317 | doi = 10.1185/03007998909115213 }}</ref> and [[flesinoxan]]<ref name="pmid9169298">{{cite journal | authors = Cryan JF, Redmond AM, Kelly JP, Leonard BE | title = The effects of the 5-HT1A agonist flesinoxan, in three paradigms for assessing antidepressant potential in the rat | journal = Eur Neuropsychopharmacol | volume = 7 | issue = 2 | pages = 109-14 | year = 1997 | pmid = 9169298 | doi = 10.1016/S0924-977X(96)00391-4 }}</ref> show efficacy in relieving [[anxiety]]<ref name="pmid9724773">{{cite journal | authors = Parks CL, Robinson PS, Sibille E, Shenk T, Toth M | title = Increased anxiety of mice lacking the serotonin1A receptor | journal = Proc. Natl. Acad. Sci. U.S.A. | volume = 95 | issue = 18 | pages = 10734-9 | year = 1998 | pmid = 9724773 | pmc = 27964 | doi = 10.1073/pnas.95.18.10734 }}</ref> and [[Depression (mood)|depression]],<ref name="pmid2883013">{{cite journal | authors = Kennett GA, Dourish CT, Curzon G | title = Antidepressant-like action of 5-HT1A agonists and conventional antidepressants in an animal model of depression | journal = Eur. J. Pharmacol. | volume = 134 | issue = 3 | pages = 265-74 | year = 1987 | pmid = 2883013 | doi = 10.1016/0014-2999(87)90357-8 }}</ref> and [[buspirone]] and [[tandospirone]] are currently approved for these indications in various parts of the world. Others such as [[gepirone]],<ref name="pmid15643103">{{cite journal | authors = Keller MB, Ruwe FJ, Janssens CJ, Sitsen JM, Jokinen R, Janczewski J | title = Relapse prevention with gepirone ER in outpatients with major depression | journal = J Clin Psychopharmacol | volume = 25 | issue = 1 | pages = 79-84 | year = 2005 | date = February 2005 | pmid = 15643103 | doi = 10.1097/01.jcp.0000150221.53877.d9 | url = http://meta.wkhealth.com/pt/pt-core/template-journal/lwwgateway/media/landingpage.htm?issn=0271-0749&volume=25&issue=1&spage=79 }}</ref> [[flesinoxan]],<ref name="pmid9169298">{{cite journal | authors = Cryan JF, Redmond AM, Kelly JP, Leonard BE | title = The effects of the 5-HT1A agonist flesinoxan, in three paradigms for assessing antidepressant potential in the rat | journal = Eur Neuropsychopharmacol | volume = 7 | issue = 2 | pages = 109-14 | year = 1997 | date = May 1997 | pmid = 9169298 | doi = 10.1016/S0924-977X(96)00391-4 | url = http://linkinghub.elsevier.com/retrieve/pii/S0924-977X(96)00391-4 }}</ref> [[flibanserin]],<ref>{{cite journal | authors = Invernizzi RW, Sacchetti G, Parini S, Acconcia S, Samanin R | title = Flibanserin, a potential antidepressant drug, lowers 5-HT and raises dopamine and noradrenaline in the rat prefrontal cortex dialysate: role of 5-HT(1A) receptors | journal = Br. J. Pharmacol. | volume = 139 | issue = 7 | pages = 1281-8 | year = 2003 | date = August 2003 | pmid = 12890707 | pmc = 1573953 | doi = 10.1038/sj.bjp.0705341 | url = http://www.nature.com/bjp/journal/v139/n7/full/0705341a.html }}</ref> and [[naluzotan]]<ref name="pmid17263189">{{cite journal | authors = de Paulis T | title = Drug evaluation: PRX-00023, a selective 5-HT1A receptor agonist for depression | journal = Curr Opin Investig Drugs | volume = 8 | issue = 1 | pages = 78-86 | year = 2007 | pmid = 17263189 }}</ref> have also been investigated, though none have been fully developed and approved yet. Some of the [[atypical antipsychotic]]s like [[aripiprazole]]<ref name="pmid17242925">{{cite journal | authors = Stark AD, Jordan S, Allers KA, Bertekap RL, Chen R, Mistry Kannan T, Molski TF, Yocca FD, Sharp T, Kikuchi T, Burris KD | title = Interaction of the novel antipsychotic aripiprazole with 5-HT1A and 5-HT2A receptors: functional receptor-binding and in vivo electrophysiological studies | journal = Psychopharmacology (Berl.) | volume = 190 | issue = 3 | pages = 373-82 | year = 2007 | pmid = 17242925 | doi = 10.1007/s00213-006-0621-y }}</ref> are also [[partial agonist]]s at the 5-HT<sub>1A</sub> receptor and are sometimes used in low doses as augmentations to standard [[antidepressant]]s like the [[selective serotonin reuptake inhibitor]]s (SSRIs).<ref>{{cite journal | authors = Wheeler Vega JA, Mortimer AM, Tyson PJ | title = Conventional antipsychotic prescription in unipolar depression, I: an audit and recommendations for practice | journal = J Clin Psychiatry | volume = 64 | issue = 5 | pages = 568-74 | year = 2003 | date = May 2003 | pmid = 12755661 | doi = 10.4088/JCP.v64n0512 | url = http://www.psychiatrist.com/abstracts/abstracts.asp?abstract=200305/050311.htm | publisher = Physicians Postgraduate Press | archiveurl = http://web.archive.org/web/20090620064725/http://www.psychiatrist.com/abstracts/abstracts.asp?abstract=200305/050311.htm | deadurl = no | archivedate = 20 June 2009 }}</ref>

5-HT<sub>1A</sub> autoreceptor desensitization and increased 5-HT<sub>1A</sub> receptor postsynaptic activation via general increases in serotonin levels by serotonin [[Precursor (chemistry)|precursor]] [[Dietary supplement|supplementation]], [[serotonin reuptake inhibitor|serotonin reuptake inhibition]], or [[monoamine oxidase]] [[enzyme inhibition|inhibition]] has been shown to be a major mediator in the therapeutic benefits of most mainstream [[antidepressant]] [[Dietary supplement|supplements]] and [[pharmaceutical]]s, including serotonin precursors like [[L-tryptophan]] and [[5-hydroxytryptophan|5-HTP]], [[selective serotonin reuptake inhibitor]]s (SSRIs), [[serotonin-norepinephrine reuptake inhibitor]]s (SNRIs), [[tricyclic antidepressant]]s (TCAs), [[tetracyclic antidepressant]]s (TeCAs), and [[monoamine oxidase inhibitor]]s (MAOIs).<ref name="pmid11212592">{{cite journal | authors = Blier P, Abbott FV | title = Putative mechanisms of action of antidepressant drugs in affective and anxiety disorders and pain | journal = J Psychiatry Neurosci | volume = 26 | issue = 1 | pages = 37-43 | year = 2001 | date = January 2001 | pmid = 11212592 | pmc = 1408043 | url = http://www.cma.ca/multimedia/staticContent/HTML/N0/l2/jpn/vol-26/issue-1/pdf/pg37.pdf }}</ref> 5-HT<sub>1A</sub> receptor activation likely plays a significant role in the positive effects of serotonin [[releasing agent]]s (SRAs) like [[MDMA]] («[[Ecstasy (drug)|Ecstasy]]») as well.<ref name="pmid15908091">{{cite journal | authors = Morley KC, Arnold JC, McGregor IS | title = Serotonin (1A) receptor involvement in acute 3,4-methylenedioxymethamphetamine (MDMA) facilitation of social interaction in the rat | journal = Prog. Neuropsychopharmacol. Biol. Psychiatry | volume = 29 | issue = 5 | pages = 648-57 | year = 2005 | date = June 2005 | pmid = 15908091 | doi = 10.1016/j.pnpbp.2005.04.009 }}</ref><ref name="pmid17383105">{{vcite2 journal | vauthors = Thompson MR, Callaghan PD, Hunt GE, Cornish JL, McGregor IS | title = A role for oxytocin and 5-HT(1A) receptors in the prosocial effects of 3,4 methylenedioxymethamphetamine ("ecstasy") | journal = Neuroscience | volume = 146 | issue = 2 | pages = 509-14 | year = 2007 | date = May 2007 | pmid = 17383105 | doi = 10.1016/j.neuroscience.2007.02.032 }}</ref>

5-HT<sub>1A</sub> receptors in the [[dorsal raphe nucleus]] are co-localized with [[Tachykinin receptor 1|neurokinin 1]] (NK<sub>1</sub>) receptors and have been shown to inhibit the release of [[substance P]], their [[endogenous]] [[ligand]].<ref name="pmid16950604">{{cite journal | authors = Gobbi G, Cassano T, Radja F, Morgese MG, Cuomo V, Santarelli L, Hen R, Blier P | title = Neurokinin 1 receptor antagonism requires norepinephrine to increase serotonin function | journal = Eur Neuropsychopharmacol | volume = 17 | issue = 5 | pages = 328-38 | year = 2007 | date = April 2007 | pmid = 16950604 | doi = 10.1016/j.euroneuro.2006.07.004 }}</ref><ref>{{cite journal | authors = Baker KG, Halliday GM, Hornung JP, Geffen LB, Cotton RG, Törk I | title = Distribution, morphology and number of monoamine-synthesizing and substance P-containing neurons in the human dorsal raphe nucleus | journal = Neuroscience | volume = 42 | issue = 3 | pages = 757-75 | year = 1991 | pmid = 1720227 | doi = 10.1016/0306-4522(91)90043-N | url = http://linkinghub.elsevier.com/retrieve/pii/0306-4522(91)90043-N }}</ref> In addition to being [[antidepressant]] and [[anxiolytic]] in effect, 5-HT<sub>1A</sub> receptor activation has also been demonstrated to be [[antiemetic]]<ref name="pmid8013549">{{cite journal | authors = Lucot JB | title = Antiemetic effects of flesinoxan in cats: comparisons with 8-hydroxy-2-(di-n-propylamino)tetralin | journal = Eur. J. Pharmacol. | volume = 253 | issue = 1-2 | pages = 53-60 | year = 1994 | date = February 1994 | pmid = 8013549 | doi = 10.1016/0014-2999(94)90756-0 }}</ref><ref name="pmid12401641">{{cite journal | authors = Oshima T, Kasuya Y, Okumura Y, Terazawa E, Dohi S | title = Prevention of nausea and vomiting with tandospirone in adults after tympanoplasty | journal = Anesth. Analg. | volume = 95 | issue = 5 | pages = 1442-5, table of contents | year = 2002 | date = November 2002 | pmid = 12401641 | doi = 10.1097/00000539-200211000-00063 | url = http://www.anesthesia-analgesia.org/cgi/pmidlookup?view=long&pmid=12401641 }}</ref> and [[analgesic]],<ref name="pmid12595749">{{vcite2 journal | vauthors = Bardin L, Tarayre JP, Malfetes N, Koek W, Colpaert FC | title = Profound, non-opioid analgesia produced by the high-efficacy 5-HT(1A) agonist F 13640 in the formalin model of tonic nociceptive pain | journal = Pharmacology | volume = 67 | issue = 4 | pages = 182-94 | year = 2003 | date = April 2003 | pmid = 12595749 | doi = 10.1159/000068404 }}</ref><ref name="pmid16425670">{{cite journal | authors = Colpaert FC | title = 5-HT(1A) receptor activation: new molecular and neuroadaptive mechanisms of pain relief | journal = Curr Opin Investig Drugs | volume = 7 | issue = 1 | pages = 40-7 | year = 2006 | date = January 2006 | pmid = 16425670 }}</ref> and all of these properties may be mediated in part or full, depending on the property in question, by NK<sub>1</sub> receptor inhibition. Consequently, novel [[NK1 receptor antagonist|NK<sub>1</sub> receptor antagonists]] are now in use for the treatment of [[nausea]] and [[emesis]], and are also being investigated for the treatment of [[anxiety]] and [[Depression (mood)|depression]].<ref name="pmid15173897">{{cite journal | authors = Blier P, Gobbi G, Haddjeri N, Santarelli L, Mathew G, Hen R | title = Impact of substance P receptor antagonism on the serotonin and norepinephrine systems: relevance to the antidepressant/anxiolytic response | journal = J Psychiatry Neurosci | volume = 29 | issue = 3 | pages = 208-18 | year = 2004 | pmid = 15173897 | pmc = 400690 }}</ref>

5-HT<sub>1A</sub> receptor activation has been shown to increase [[dopamine]] release in the [[medial prefrontal cortex]], [[striatum]], and [[hippocampus]], and may be useful for improving the symptoms of [[schizophrenia]] and [[Parkinson's disease]].<ref name="pmid15189766">{{cite journal | authors = Li Z, Ichikawa J, Dai J, Meltzer HY | title = Aripiprazole, a novel antipsychotic drug, preferentially increases dopamine release in the prefrontal cortex and hippocampus in rat brain | journal = Eur. J. Pharmacol. | volume = 493 | issue = 1-3 | pages = 75-83 | year = 2004 | pmid = 15189766 | doi = 10.1016/j.ejphar.2004.04.028 }}</ref><ref name="pmid15906386">{{cite journal | authors = Bantick RA, De Vries MH, Grasby PM | title = The effect of a 5-HT1A receptor agonist on striatal dopamine release | journal = Synapse | volume = 57 | issue = 2 | pages = 67-75 | year = 2005 | pmid = 15906386 | doi = 10.1002/syn.20156 }}</ref> As mentioned above, some of the atypical antipsychotics are 5-HT<sub>1A</sub> receptor partial agonists, and this property has been shown to enhance their clinical efficacy.<ref name="pmid15189766"/><ref name="pmid10924666">{{cite journal | authors = Rollema H, Lu Y, Schmidt AW, Sprouse JS, Zorn SH | title = 5-HT(1A) receptor activation contributes to ziprasidone-induced dopamine release in the rat prefrontal cortex | journal = Biol. Psychiatry | volume = 48 | issue = 3 | pages = 229-37 | year = 2000 | pmid = 10924666 | doi = 10.1016/S0006-3223(00)00850-7 }}</ref><ref name="pmid9456005">{{cite journal | authors = Rollema H, Lu Y, Schmidt AW, Zorn SH | title = Clozapine increases dopamine release in prefrontal cortex by 5-HT1A receptor activation | journal = Eur. J. Pharmacol. | volume = 338 | issue = 2 | pages = R3-5 | year = 1997 | pmid = 9456005 | doi = 10.1016/S0014-2999(97)81951-6 }}</ref> Enhancement of dopamine release in these areas may also play a major role in the antidepressant and anxiolytic effects seen upon postsynaptic activation of the 5-HT<sub>1A</sub> receptor.<ref name="pmid11792466">{{cite journal | authors = Yoshino T, Nisijima K, Katoh S, Yui K, Nakamura M | title = Tandospirone potentiates the fluoxetine-induced increases in extracellular dopamine via 5-HT(1A) receptors in the rat medial frontal cortex | journal = Neurochem. Int. | volume = 40 | issue = 4 | pages = 355-60 | year = 2002 | date = April 2002 | pmid = 11792466 | doi = 10.1016/S0197-0186(01)00079-1 | url = http://linkinghub.elsevier.com/retrieve/pii/S0197018601000791 }}</ref><ref name="pmid1681449">{{cite journal | vauthors = Chojnacka-Wójcik E, Tatarczyńska E, Gołembiowska K, Przegaliński E | title = Involvement of 5-HT1A receptors in the antidepressant-like activity of gepirone in the forced swimming test in rats | journal = Neuropharmacology | volume = 30 | issue = 7 | pages = 711-7 | year = 1991 | date = July 1991 | pmid = 1681449 | doi = 10.1016/0028-3908(91)90178-E }}</ref>

Activation of 5-HT<sub>1A</sub> receptors has been demonstrated to impair certain aspects of [[memory]] (affecting declarative and non-declarative memory functions) and [[learning]] (due to interference with memory-encoding mechanisms), by inhibiting the release of [[glutamate]] and [[acetylcholine]] in various areas of the [[brain]].<ref name="pmid18394726">{{cite journal | authors = Ogren SO, Eriksson TM, Elvander-Tottie E, D'Addario C, Ekström JC, Svenningsson P, Meister B, Kehr J, Stiedl O | title = The role of 5-HT(1A) receptors in learning and memory | journal = Behav. Brain Res. | volume = 195 | issue = 1 | pages = 54-77 | year = 2008 | pmid = 18394726 | doi = 10.1016/j.bbr.2008.02.023 }}</ref> 5-HT<sub>1A</sub> activation are known to improve cognitive functions associated with the prefrontal cortex, possibly via inducing prefrontal cortex dopamine and acetylcholine release.<ref>{{cite journal | authors = Meltzer HY, Sumiyoshi T | title = Does stimulation of 5-HT(1A) receptors improve cognition in schizophrenia? | journal = Behav. Brain Res. | volume = 195 | issue = 1 | pages = 98-102 | year = 2008 | date = December 2008 | pmid = 18707769 | doi = 10.1016/j.bbr.2008.05.016 }}</ref> Conversely, 5-HT<sub>1A</sub> receptor [[antagonist]]s such as [[lecozotan]] have been shown to facilitate certain types of learning and memory in rodents, and as a result, are being developed as novel treatments for [[Alzheimer's disease]].<ref>{{cite journal | authors = Spreitzer H | date = August 13, 2008 | title = Neue Wirkstoffe - Lecozotan | journal = Österreichische Apothekerzeitung | issue = 17/2007 | pages = 805 | language = German }}</ref>

Other effects of 5-HT<sub>1A</sub> activation that have been observed in scientific research include:

* Decreased [[aggression]]<ref name="pmid16310183">{{cite2 journal | authors = de Boer SF, Koolhaas JM | title = 5-HT1A and 5-HT1B receptor agonists and aggression: a pharmacological challenge of the serotonin deficiency hypothesis | journal = Eur. J. Pharmacol. | volume = 526 | issue = 1-3 | pages = 125-39 | year = 2005 | pmid = 16310183 | doi = 10.1016/j.ejphar.2005.09.065 }}</ref><ref name="pmid2091890">{{cite journal | authors = Olivier B, Mos J, Rasmussen D | title = Behavioural pharmacology of the serenic, eltoprazine | journal = Drug Metabol Drug Interact | volume = 8 | issue = 1-2 | pages = 31-83 | year = 1990 | pmid = 2091890 | doi = 10.1515/DMDI.1990.8.1-2.31 }}</ref>
* Increased [[social relation|sociability]]<ref name="pmid17383105">{{cite journal | authors = Thompson MR, Callaghan PD, Hunt GE, Cornish JL, McGregor IS | title = A role for oxytocin and 5-HT(1A) receptors in the prosocial effects of 3,4 methylenedioxymethamphetamine ("ecstasy") | journal = Neuroscience | volume = 146 | issue = 2 | pages = 509-14 | year = 2007 | pmid = 17383105 | doi = 10.1016/j.neuroscience.2007.02.032 }}</ref>
* Decreased [[impulsivity]]<ref name="pmid15688093">{{cite journal | authors = Winstanley CA, Theobald DE, Dalley JW, Robbins TW | title = Interactions between serotonin and dopamine in the control of impulsive choice in rats: therapeutic implications for impulse control disorders | journal = Neuropsychopharmacology | volume = 30 | issue = 4 | pages = 669-82 | year = 2005 | pmid = 15688093 | doi = 10.1038/sj.npp.1300610 }}</ref>
* Inhibition of [[Behavioral addiction|drug-seeking behavior]]<ref name="pmid7862892">{{cite journal | authors = Tomkins DM, Higgins GA, Sellers EM | title = Low doses of the 5-HT1A agonist 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH DPAT) increase ethanol intake | journal = Psychopharmacology (Berl.) | volume = 115 | issue = 1-2 | pages = 173-9 | year = 1994 | pmid = 7862892 | doi = 10.1007/BF02244769 }}</ref><ref name="pmid17316955">{{vcite2 journal | vauthors = Müller CP, Carey RJ, Huston JP, De Souza Silva MA | title = Serotonin and psychostimulant addiction: focus on 5-HT1A-receptors | journal = Prog. Neurobiol. | volume = 81 | issue = 3 | pages = 133-78 | year = 2007 | pmid = 17316955 | doi = 10.1016/j.pneurobio.2007.01.001 }}</ref><ref name="pmid15713268">{{cite journal | authors = Carey RJ, DePalma G, Damianopoulos E, Shanahan A, Müller CP, Huston JP | title = Evidence that the 5-HT1A autoreceptor is an important pharmacological target for the modulation of cocaine behavioral stimulant effects | journal = Brain Res. | volume = 1034 | issue = 1-2 | pages = 162-71 | year = 2005 | pmid = 15713268 | doi = 10.1016/j.brainres.2004.12.012 }}</ref>
* Facilitation of [[Human sexual activity|sex drive]] and [[sexual arousal|arousal]]<ref name="pmid8981617">{{cite journal | authors = Fernández-Guasti A, Rodríguez-Manzo G | title = 8-OH-DPAT and male rat sexual behavior: partial blockade by noradrenergic lesion and sexual exhaustion | journal = Pharmacol. Biochem. Behav. | volume = 56 | issue = 1 | pages = 111-6 | year = 1997 | date = January 1997 | pmid = 8981617 | doi = 10.1016/S0091-3057(96)00165-7 }}</ref><ref name="pmid9228408">{{cite journal | authors = Haensel SM, Slob AK | title = Flesinoxan: a prosexual drug for male rats | journal = Eur. J. Pharmacol. | volume = 330 | issue = 1 | pages = 1-9 | year = 1997 | date = July 1997 | pmid = 9228408 | doi = 10.1016/S0014-2999(97)00170-2 | url = http://linkinghub.elsevier.com/retrieve/pii/S0014-2999(97)00170-2 }}</ref>
* Inhibition of [[penile erection]]<ref name="pmid1357709">{{cite journal | authors = Simon P, Guardiola B, Bizot-Espiard J, Schiavi P, Costentin J | title = 5-HT1A receptor agonists prevent in rats the yawning and penile erections induced by direct dopamine agonists | journal = Psychopharmacology (Berl.) | volume = 108 | issue = 1-2 | pages = 47-50 | year = 1992 | pmid = 1357709 | doi = 10.1007/BF02245284 }}</ref><ref name="pmid9085055">{{cite journal | authors = Millan MJ, Perrin-Monneyron S | title = Potentiation of fluoxetine-induced penile erections by combined blockade of 5-HT1A and 5-HT1B receptors | journal = Eur. J. Pharmacol. | volume = 321 | issue = 3 | pages = R11-3 | year = 1997 | pmid = 9085055 | doi = 10.1016/S0014-2999(97)00050-2 }}</ref>
* [[Anorexia (symptom)|Diminished food intake]]<ref name="pmid17609739">{{cite journal | authors = Ebenezer IS, Arkle MJ, Tite RM | title = 8-Hydroxy-2-(di-n-propylamino)-tetralin inhibits food intake in fasted rats by an action at 5-HT1A receptors | journal = Methods Find Exp Clin Pharmacol | volume = 29 | issue = 4 | pages = 269-72 | year = 2007 | pmid = 17609739 | doi = 10.1358/mf.2007.29.4.1075362 }}</ref>
* Prolongation of [[Rapid eye movement sleep|REM]] [[sleep]] latency<ref name="pmid10607047">{{cite journal | authors = Monti JM, Jantos H | title = Dose-dependent effects of the 5-HT1A receptor agonist 8-OH-DPAT on sleep and wakefulness in the rat | journal = J Sleep Res | volume = 1 | issue = 3 | pages = 169-175 | year = 1992 | pmid = 10607047 | doi = 10.1111/j.1365-2869.1992.tb00033.x }}</ref><ref>{{cite journal | authors = Marc Ansseau, William Pitchot, Antonio Gonzalez Moreno, Jacques Wauthy, Patrick Papart | title = Pilot study of flesinoxan, a 5-HT1A agonist, in major depression: Effects on sleep REM latency and body temperature | journal = Human Psychopharmacology: Clinical and Experimental | volume = 8 | issue = 4 | pages = 279–283 | year = 2004 | url = http://www3.interscience.wiley.com/journal/109710934/abstract | doi = 10.1002/hup.470080407 }}</ref>
* Reversal of [[opioid]]-induced [[respiratory depression]].<ref name="pmid16166206">{{cite journal | authors = Meyer LC, Fuller A, Mitchell D | title = Zacopride and 8-OH-DPAT reverse opioid-induced respiratory depression and hypoxia but not catatonic immobilization in goats | journal = Am. J. Physiol. Regul. Integr. Comp. Physiol. | volume = 290 | issue = 2 | pages = R405-13 | year = 2006 | date = February 2006 | pmid = 16166206 | doi = 10.1152/ajpregu.00440.2005 }}</ref>

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=== Эндокринные эффекты ===

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5-HT<sub>1A</sub> receptor activation induces the [[secretion]] of various [[hormone]]s including [[cortisol]], [[corticosterone]], [[adrenocorticotropic hormone]] (ACTH), [[oxytocin]], [[prolactin]], [[growth hormone]], and [[β-endorphin]].<ref name="pmid9678651">{{vcite2 journal | vauthors = Van de Kar LD, Levy AD, Li Q, Brownfield MS | title = A comparison of the oxytocin and vasopressin responses to the 5-HT1A agonist and potential anxiolytic drug alnespirone (S-20499) | journal = Pharmacol. Biochem. Behav. | volume = 60 | issue = 3 | pages = 677-83 | year = 1998 | pmid = 9678651 | doi = 10.1016/S0091-3057(98)00025-2 }}</ref><ref name="pmid2952898">{{vcite2 journal | vauthors = Lorens SA, Van de Kar LD | title = Differential effects of serotonin (5-HT1A and 5-HT2) agonists and antagonists on renin and corticosterone secretion | journal = Neuroendocrinology | volume = 45 | issue = 4 | pages = 305-10 | year = 1987 | pmid = 2952898 | doi = 10.1159/000124754 }}</ref><ref name="pmid2956114">{{vcite2 journal | vauthors = Koenig JI, Gudelsky GA, Meltzer HY | title = Stimulation of corticosterone and beta-endorphin secretion in the rat by selective 5-HT receptor subtype activation | journal = Eur. J. Pharmacol. | volume = 137 | issue = 1 | pages = 1-8 | year = 1987 | pmid = 2956114 | doi = 10.1016/0014-2999(87)90175-0 }}</ref><ref name="pmid15013031">{{vcite2 journal | vauthors = Pitchot W, Wauthy J, Legros JJ, Ansseau M | title = Hormonal and temperature responses to flesinoxan in normal volunteers: an antagonist study | journal = Eur Neuropsychopharmacol | volume = 14 | issue = 2 | pages = 151-5 | year = 2004 | date = March 2004 | pmid = 15013031 | doi = 10.1016/S0924-977X(03)00108-1 }}</ref> The receptor does not affect [[vasopressin]] or [[renin]] secretion, unlike the [[5-HT2 receptor|5-HT<sub>2</sub> receptors]].<ref name="pmid9678651"/><ref name="pmid2952898"/> It has been suggested that oxytocin release may contribute to the prosocial, [[serenic|antiaggressive]], and anxiolytic properties observed upon activation of the receptor.<ref name="pmid17383105"/> β-Endorphin secretion may contribute to antidepressant, anxiolytic, and analgesic effects.<ref name="pmid18725263">{{vcite2 journal | vauthors = Navinés R, Martín-Santos R, Gómez-Gil E, Martínez de Osaba MJ, Gastó C | title = Interaction between serotonin 5-HT1A receptors and beta-endorphins modulates antidepressant response | journal = Prog. Neuropsychopharmacol. Biol. Psychiatry | volume = 32 | issue = 8 | pages = 1804-9 | year = 2008 | date = December 2008 | pmid = 18725263 | doi = 10.1016/j.pnpbp.2008.07.021 | url = http://linkinghub.elsevier.com/retrieve/pii/S0278-5846(08)00237-6 }}</ref>

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=== Ауторецепторы ===

<!---

5-HT<sub>1A</sub> receptors can be located on the [[cell body]], [[dendrite]]s, [[axon]]s, and both [[presynaptic]]ally and [[postsynaptic]]ally in [[nerve terminal]]s or [[synapse]]s. Those located on the soma and dendrites are referred to as [[somatodendritic]], and those located presynaptically in the synapse are simply referred to as presynaptic. As a group, receptors that are sensitive to the neurotransmitter that is released by the neuron on which the receptors are located are known as [[autoreceptor]]s; they typically constitute the key component of an ultra-short negative feedback loop whereby the neuron’s release of neurotransmitter inhibits its further release of neurotransmitter. Stimulation of 5-HT<sub>1A</sub> autoreceptors inhibits the release of serotonin in nerve terminals. For this reason, 5-HT<sub>1A</sub> receptor agonists tend to exert a biphasic mode of action; they decrease serotonin release and postsynaptic 5-HT<sub>1A</sub> receptor activity in low doses, and further decrease serotonin release but increase postsynaptic 5-HT<sub>1A</sub> receptor activity at higher doses by directly stimulating the receptors in place of serotonin.

This autoreceptor-mediated inhibition of serotonin release has been theorized to be a major factor in the therapeutic lag that is seen with serotonergic antidepressants such as the SSRIs.<ref name="pmid10890313">{{vcite2 journal | vauthors = Hjorth S, Bengtsson HJ, Kullberg A, Carlzon D, Peilot H, Auerbach SB | title = Serotonin autoreceptor function and antidepressant drug action | journal = J. Psychopharmacol. (Oxford) | volume = 14 | issue = 2 | pages = 177-85 | year = 2000 | pmid = 10890313 | doi = 10.1177/026988110001400208 }}</ref> The autoreceptors must first [[downregulation|densensitize]] before the concentration of extracellular serotonin in the synapse can become elevated appreciably.<ref name="pmid10890313"/><ref name="pmid8221701">{{vcite2 journal | vauthors = Briley M, Moret C | title = Neurobiological mechanisms involved in antidepressant therapies | journal = Clin Neuropharmacol | volume = 16 | issue = 5 | pages = 387-400 | year = 1993 | pmid = 8221701 | doi = 10.1097/00002826-199310000-00002 }}</ref> Though the responsiveness of the autoreceptors is somewhat reduced with chronic treatment, they still remain effective at constraining large increases in extracellular serotonin concentrations.<ref name="pmid10890313"/> For this reason, [[serotonin reuptake inhibitor]]s that also have 5-HT<sub>1A</sub> receptor antagonistic or partial agonistic properties, such as [[vilazodone]] and [[SB-649,915]], are being investigated and introduced as novel antidepressants with the potential for a faster onset of action and improved effectiveness compared to those currently available.<ref name="pmid17356576">{{vcite2 journal | vauthors = Starr KR, Price GW, Watson JM, Atkinson PJ, Arban R, Melotto S, Dawson LA, Hagan JJ, Upton N, Duxon MS | title = SB-649915-B, a novel 5-HT1A/B autoreceptor antagonist and serotonin reuptake inhibitor, is anxiolytic and displays fast onset activity in the rat high light social interaction test | journal = Neuropsychopharmacology | volume = 32 | issue = 10 | pages = 2163-72 | year = 2007 | pmid = 17356576 | doi = 10.1038/sj.npp.1301341 }}</ref>

Unlike most drugs that elevate extracellular serotonin levels like the SSRIs and MAOIs, SRAs such as [[fenfluramine]] and [[MDMA]] bypass serotonin autoreceptors such as 5-HT<sub>1A</sub>. They do this by directly acting on the release mechanisms of serotonin neurons and forcing release to occur regardless of autorecepter-mediated inhibition.<ref name="pmid17017961">{{vcite2 journal | vauthors = Rothman RB, Baumann MH | title = Therapeutic potential of monoamine transporter substrates | journal = Curr Top Med Chem | volume = 6 | issue = 17 | pages = 1845-59 | year = 2006 | pmid = 17017961 | doi = 10.2174/156802606778249766 | url = http://www.bentham-direct.org/pages/content.php?CTMC/2006/00000006/00000017/0004R.SGM }}</ref> As such, SRAs induce immediate and much greater increases in extracellular serotonin concentrations compared to other serotonin-elevating agents such as the SSRIs. In contrast to SRAs, SSRIs actually ''decrease'' serotonin levels initially and require several weeks of chronic dosing before serotonin concentrations reach their maximal elevation and full clinical benefits for conditions such as depression and anxiety are seen.<ref name="pmid10428424">{{vcite2 journal | vauthors = Scorza C, Silveira R, Nichols DE, Reyes-Parada M | title = Effects of 5-HT-releasing agents on the extracellullar hippocampal 5-HT of rats. Implications for the development of novel antidepressants with a short onset of action | journal = Neuropharmacology | volume = 38 | issue = 7 | pages = 1055-61 | year = 1999 | date = July 1999 | pmid = 10428424 | doi = 10.1016/S0028-3908(99)00023-4 | url = http://linkinghub.elsevier.com/retrieve/pii/S0028390899000234 }}</ref><ref name="pmid9694528">{{vcite2 journal | vauthors = Marona-Lewicka D, Nichols DE | title = Drug discrimination studies of the interoceptive cues produced by selective serotonin uptake inhibitors and selective serotonin releasing agents | journal = Psychopharmacology (Berl.) | volume = 138 | issue = 1 | pages = 67-75 | year = 1998 | date = July 1998 | pmid = 9694528 | doi = 10.1007/s002130050646 | url = http://link.springer.de/link/service/journals/00213/bibs/8138001/81380067.htm }}</ref> For these reasons, [[selective serotonin releasing agent]]s (SSRAs) such as [[MDAI]] and [[MMAI]] have been proposed as novel antidepressants with a putatively faster onset of action and improved effectiveness compared to current treatments.<ref name="pmid10428424"/>

Similarly to SRAs, sufficiently high doses of 5-HT<sub>1A</sub> receptor agonists also bypass the 5-HT<sub>1A</sub> autoreceptor-mediated inhibition of serotonin release and therefore increase 5-HT<sub>1A</sub> postsynaptic receptor activation by directly agonizing the postsynaptic receptors [[in lieu]] of serotonin. However, in contrast to SRAs, 5-HT<sub>1A</sub> receptor agonists do not bypass the inhibitory effect of 5-HT<sub>1A</sub> autoreceptors located as [[heteroreceptor]]s in non-[[serotonergic]] [[synapse]]s where 5-HT<sub>1A</sub> postsynaptic receptors are not present, which, instead of serotonin, modulate the release of other [[neurotransmitter]]s such as [[dopamine]] or [[glutamate]]. The therapeutic consequences of this difference, if any, are unknown.

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== Лиганды ==

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The distribution of 5-HT<sub>1A</sub> receptors in the [[human brain]] may be imaged with the [[positron emission tomography]] using the [[radioligand]] [<sup>11</sup>C][[WAY-100,635]].<ref name="pmid7498295">{{vcite2 journal | vauthors = Pike VW, McCarron JA, Lammerstma AA, Hume SP, Poole K, Grasby PM, Malizia A, Cliffe IA, Fletcher A, Bench CJ | title = First delineation of 5-HT1A receptors in human brain with PET and [11C]WAY-100635 | journal = Eur. J. Pharmacol. | volume = 283 | issue = 1-3 | pages = R1-3 | year = 1995 | pmid = 7498295 | doi = 10.1016/0014-2999(95)00438-Q }}</ref>
For example, one study has found increased 5-HT<sub>1A</sub> binding in type 2 [[diabetes]].<ref name="pmid11814436">{{vcite2 journal | vauthors = Price JC, Kelley DE, Ryan CM, Meltzer CC, Drevets WC, Mathis CA, Mazumdar S, Reynolds CF | title = Evidence of increased serotonin-1A receptor binding in type 2 diabetes: a positron emission tomography study | journal = Brain Res. | volume = 927 | issue = 1 | pages = 97-103 | year = 2002 | pmid = 11814436 | doi = 10.1016/S0006-8993(01)03297-8 }}</ref> Another PET study found a negative correlation between the amount of 5-HT<sub>1A</sub> binding in the [[raphe nuclei]], [[hippocampus]] and [[neocortex]] and a self-reported tendency to have [[spiritual experience]]s.<ref name="pmid14594742">{{vcite2 journal | vauthors = Borg J, Andrée B, Soderstrom H, Farde L | title = The serotonin system and spiritual experiences | journal = Am J Psychiatry | volume = 160 | issue = 11 | pages = 1965-9 | year = 2003 | date = November 2003 | pmid = 14594742 | doi = 10.1176/appi.ajp.160.11.1965 }}</ref> Labeled with [[tritium]], WAY-100,635 may also be used in [[autoradiography]].<ref name="pmid9152998">{{vcite2 journal | vauthors = Burnet PW, Eastwood SL, Harrison PJ | title = [3H]WAY-100635 for 5-HT1A receptor autoradiography in human brain: a comparison with [3H]8-OH-DPAT and demonstration of increased binding in the frontal cortex in schizophrenia | journal = Neurochem. Int. | volume = 30 | issue = 6 | pages = 565-74 | year = 1997 | pmid = 9152998 | doi = 10.1016/S0197-0186(96)00124-6 }}</ref>

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=== Агонисты ===

* 8-OH-DPAT<ref>{{cite journal | authors = Winsauer PJ, Rodriguez FH, Cha AE, Moerschbaecher JM | title = Full and partial 5-HT1A receptor agonists disrupt learning and performance in rats | journal = J. Pharmacol. Exp. Ther. | volume = 288 | issue = 1 | pages = 335-47 | year = 1999 | date = January 1999 | pmid = 9862788 | url = http://jpet.aspetjournals.org/content/288/1/335.full.pdf }}</ref>
* Alnespirone
* Befiradol
* Eptapirone
* F-15,599
* Lesopitron
* MKC-242
* LY-293,284
* Osemozotan (partial at postsynaptic receptors)
* Repinotan
* U-92,016-A

=== Парциальные агонисты ===

* 5-Carboxamidotryptamine (5-CT)
* 5-Methoxytryptamine (5-MT)
* 5-MeO-DMT
* Adatanserin
* alpha-Ethyltryptamine (αET)
* alpha-Methyltryptamine (αMT)
* Aripiprazole
* Asenapine
* Bay R 1531
* Befiradol
* Binospirone
* Bufotenin
* Buspirone
* Cannabidiol
* Clozapine
* Dihydroergotamine
* Ebalzotan
* Eltoprazine
* Ergotamine
* Etoperidone
* F-11,461
* F-12,826
* F-13,714
* F-14,679
* Flesinoxan
* Flibanserin
* Ginkgo Biloba<ref>{{cite journal | authors = Winter JC, Timineri D | title = The discriminative stimulus properties of EGb 761, an extract of Ginkgo biloba | journal = Pharmacol. Biochem. Behav. | volume = 62 | issue = 3 | pages = 543-7 | year = 1999 | date = March 1999 | pmid = 10080249 | doi = 10.1016/S0091-3057(98)00190-7 }}</ref>
* Gepirone
* Haloperidol
* Ipsapirone
* Lisuride
* Lurasidone
* LY-301,317
* LSD
* MDMA
* Naluzotan
* NBUMP
* Nefazodone
* Olanzapine
* Perospirone
* Piclozotan
* Psilocin
* Psilocybin
* Quetiapine
* Rauwolscine
* RU-24,969
* S-15,535
* Sarizotan
* SSR-181,507
* Sunepitron
* Tandospirone
* Tiospirone
* Trazodone
* Trifluoromethylphenylpiperazine
* Urapidil
* Vortioxetine
* Vilazodone
* Xaliproden
* Yohimbine
* Zalospirone
* Ziprasidone

=== Антагонисты ===

* Alprenolol
* AV-965
* BMY-7,378
* Cyanopindolol
* Dotarizine
* Flopropione
* GR-46,611
* Iodocyanopindolol
* Isamoltane]
* Lecozotan
* Methiothepin
* Methysergide
* MPPF
* NAN-190
* Oxprenolol
* Pindobind
* Pindolol
* Propranolol
* Risperidone
* Robalzotan
* SB-649,915
* SDZ-216,525
* Spiperone
* Spiramide
* Spiroxatrine
* UH-301
* WAY-100,135
* WAY-100,635
* Xylamidine
* Mefway

== Генетика ==

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The 5-HT<sub>1A</sub> receptor is coded by the ''HTR1A'' [[gene]]. There are several human [[Polymorphism (biology)|polymorphisms]] associated with this gene. A 2007 review listed 27 [[single nucleotide polymorphism]]s (SNP).<ref name="pmid18047755">{{vcite2 journal | vauthors = Drago A, Ronchi DD, Serretti A | title = 5-HT1A gene variants and psychiatric disorders: a review of current literature and selection of SNPs for future studies | journal = Int. J. Neuropsychopharmacol. | volume = 11 | issue = 5 | pages = 701-21 | year = 2008 | date = August 2008 | pmid = 18047755 | doi = 10.1017/S1461145707008218 }}</ref> The most investigated SNPs are C-1019G ([[rs6295]]), C-1018G,<ref name="pmid10412191">{{vcite2 journal | vauthors = Wu S, Comings DE | title = A common C-1018G polymorphism in the human 5-HT1A receptor gene | journal = Psychiatr. Genet. | volume = 9 | issue = 2 | pages = 105-6 | year = 1999 | date = June 1999 | pmid = 10412191 | doi = 10.1097/00041444-199906000-00010 }}</ref> Ile28Val ([[rs1799921]]), Arg219Leu ([[rs1800044]]), and Gly22Ser ([[rs1799920]]).<ref name="pmid18047755"/> Some of the other SNPs are Pro16Leu, Gly272Asp, and the [[synonymous polymorphism]] G294A ([[rs6294]]). These gene variants have been studied in relation to [[psychiatric disorder]]s with no definitive results.<ref name="pmid18047755"/>

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== Взаимодействия рецептора с другими белками ==

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The 5-HT<sub>1A</sub> receptor has been shown to [[protein-protein interaction|interact]] with [[brain-derived neurotrophic factor]] (BDNF), which may play a major role in its regulation of mood and anxiety.<ref name="pmid17401528">{{vcite2 journal | vauthors = Anttila S, Huuhka K, Huuhka M, Rontu R, Hurme M, Leinonen E, Lehtimäki T | title = Interaction between 5-HT1A and BDNF genotypes increases the risk of treatment-resistant depression | journal = J Neural Transm | volume = 114 | issue = 8 | pages = 1065-8 | year = 2007 | pmid = 17401528 | doi = 10.1007/s00702-007-0705-9 }}</ref><ref name="pmid17559709">{{vcite2 journal | vauthors = Guiard BP, David DJ, Deltheil T, Chenu F, Le Maître E, Renoir T, Leroux-Nicollet I, Sokoloff P, Lanfumey L, Hamon M, Andrews AM, Hen R, Gardier AM | title = Brain-derived neurotrophic factor-deficient mice exhibit a hippocampal hyperserotonergic phenotype | journal = Int. J. Neuropsychopharmacol. | volume = 11 | issue = 1 | pages = 79-92 | year = 2008 | pmid = 17559709 | doi = 10.1017/S1461145707007857 }}</ref>

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=== Олигомеры рецептора ===

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The 5-HT<sub>1A</sub> receptor forms [[GPCR oligomer|heterodimers]] with the following receptors: [[5-HT7|5-HT<sub>7</sub>]],<ref>{{vcite2 journal | vauthors = Renner U, Zeug A, Woehler A, Niebert M, Dityatev A, Dityateva G, Gorinski N, Guseva D, Abdel-Galil D, Fröhlich M, Döring F, Wischmeyer E, Richter DW, Neher E, Ponimaskin EG | title = Heterodimerization of serotonin receptors 5-HT1A and 5-HT7 differentially regulates receptor signalling and trafficking | journal = J. Cell. Sci. | volume = 125 | issue = Pt 10 | pages = 2486-99 | year = 2012 | pmid = 22357950 | doi = 10.1242/jcs.101337 }}</ref> [[5-HT1B|5-HT<sub>1B</sub>]], [[5-HT1D|5-HT<sub>1D</sub>]], [[GABBR2|GABA<sub>B2</sub>]], GPCR26, [[LPAR1|LPA<sub>1</sub>]], [[LPAR3|LPA<sub>3</sub>]], [[S1PR1|S1P<sub>1</sub>]], [[S1PR3|S1P<sub>3</sub>]].<ref name=pmid11854302>{{vcite2 journal | vauthors = Salim K, Fenton T, Bacha J, Urien-Rodriguez H, Bonnert T, Skynner HA, Watts E, Kerby J, Heald A, Beer M, McAllister G, Guest PC | title = Oligomerization of G-protein-coupled receptors shown by selective co-immunoprecipitation | journal = J. Biol. Chem. | volume = 277 | issue = 18 | pages = 15482-5 | year = 2002 | date = May 2002 | pmid = 11854302 | doi = 10.1074/jbc.M201539200 }}</ref>

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== См. также ==

* [[Серотониновые рецепторы]]
* [[5-HT1|5-HT₁-рецептор]]
* [[5-HT2|5-HT₂-рецептор]]
* [[5-HT3|5-HT₃-рецептор]]
* [[5-HT5|5-HT₅-рецептор]]
* [[5-HT6|5-HT₆-рецептор]]
* [[5-HT7|5-HT₇-рецептор]]

== Примечания ==

{{примечания}}

== Для дополнительного чтения ==

* {{cite journal | authors = el Mestikawy S, Fargin A, Raymond JR, Gozlan H, Hnatowich M | title = The 5-HT1A receptor: an overview of recent advances | journal = Neurochem. Res. | volume = 16 | issue = 1 | pages = 1-10 | year = 1991 | pmid = 2052135 | doi = 10.1007/BF00965820 }}
* {{cite journal | authors = Hensler JG | title = Regulation of 5-HT1A receptor function in brain following agonist or antidepressant administration | journal = Life Sci. | volume = 72 | issue = 15 | pages = 1665-82 | year = 2003 | pmid = 12559389 | doi = 10.1016/S0024-3205(02)02482-7 }}
* {{cite journal | vauthors = Van Oekelen D, Luyten WH, Leysen JE | title = 5-HT2A and 5-HT2C receptors and their atypical regulation properties | journal = Life Sci. | volume = 72 | issue = 22 | pages = 2429-49 | year = 2003 | pmid = 12650852 | doi = 10.1016/S0024-3205(03)00141-3 }}
* {{cite journal | vauthors = Lesch KP, Gutknecht L | title = Focus on The 5-HT1A receptor: emerging role of a gene regulatory variant in psychopathology and pharmacogenetics | journal = Int. J. Neuropsychopharmacol. | volume = 7 | issue = 4 | pages = 381-5 | year = 2004 | pmid = 15683551 | doi = 10.1017/S1461145704004845 }}
* {{cite journal | vauthors = Kalipatnapu S, Chattopadhyay A | title = Membrane protein solubilization: recent advances and challenges in solubilization of serotonin1A receptors | journal = IUBMB Life | volume = 57 | issue = 7 | pages = 505-12 | year = 2005 | pmid = 16081372 | doi = 10.1080/15216540500167237 }}
* {{cite journal | vauthors = Varrault A, Bockaert J, Waeber C | title = Activation of 5-HT1A receptors expressed in NIH-3T3 cells induces focus formation and potentiates EGF effect on DNA synthesis | journal = Mol. Biol. Cell | volume = 3 | issue = 9 | pages = 961-9 | year = 1992 | pmid = 1330092 | pmc = 275657 | doi = 10.1091/mbc.3.9.961 }}
* {{cite journal | vauthors = Levy FO, Gudermann T, Perez-Reyes E, Birnbaumer M, Kaumann AJ, Birnbaumer L | title = Molecular cloning of a human serotonin receptor (S12) with a pharmacological profile resembling that of the 5-HT1D subtype | journal = J. Biol. Chem. | volume = 267 | issue = 11 | pages = 7553-62 | year = 1992 | pmid = 1559993 }}
* {{cite journal | vauthors = Melmer G, Sherrington R, Mankoo B, Kalsi G, Curtis D, Gurling HM | title = A cosmid clone for the 5HT1A receptor (HTR1A) reveals a TaqI RFLP that shows tight linkage to dna loci D5S6, D5S39, and D5S76 | journal = Genomics | volume = 11 | issue = 3 | pages = 767-9 | year = 1991 | pmid = 1685484 | doi = 10.1016/0888-7543(91)90088-V }}
* {{cite journal | vauthors = Parks CL, Chang LS, Shenk T | title = A polymerase chain reaction mediated by a single primer: cloning of genomic sequences adjacent to a serotonin receptor protein coding region | journal = Nucleic Acids Res. | volume = 19 | issue = 25 | pages = 7155-60 | year = 1991 | pmid = 1766875 | pmc = 332551 | doi = 10.1093/nar/19.25.7155 }}
* {{cite journal | vauthors = Gilliam TC, Freimer NB, Kaufmann CA, Powchik PP, Bassett AS, Bengtsson U, Wasmuth JJ | title = Deletion mapping of DNA markers to a region of chromosome 5 that cosegregates with schizophrenia | journal = Genomics | volume = 5 | issue = 4 | pages = 940-4 | year = 1989 | pmid = 2591972 | pmc = 3154173 | doi = 10.1016/0888-7543(89)90138-9 }}
* {{cite journal | vauthors = Kobilka BK, Frielle T, Collins S, Yang-Feng T, Kobilka TS, Francke U, Lefkowitz RJ, Caron MG | title = An intronless gene encoding a potential member of the family of receptors coupled to guanine nucleotide regulatory proteins | journal = Nature | volume = 329 | issue = 6134 | pages = 75-9 | year = 1987 | pmid = 3041227 | doi = 10.1038/329075a0 }}
* {{cite journal | vauthors = Fargin A, Raymond JR, Lohse MJ, Kobilka BK, Caron MG, Lefkowitz RJ | title = The genomic clone G-21 which resembles a beta-adrenergic receptor sequence encodes the 5-HT1A receptor | journal = Nature | volume = 335 | issue = 6188 | pages = 358-60 | year = 1988 | pmid = 3138543 | doi = 10.1038/335358a0 }}
* {{cite journal | vauthors = Nakhai B, Nielsen DA, Linnoila M, Goldman D | title = Two naturally occurring amino acid substitutions in the human 5-HT1A receptor: glycine 22 to serine 22 and isoleucine 28 to valine 28 | journal = Biochem. Biophys. Res. Commun. | volume = 210 | issue = 2 | pages = 530-6 | year = 1995 | pmid = 7755630 | doi = 10.1006/bbrc.1995.1692 }}
* {{cite journal | vauthors = Aune TM, McGrath KM, Sarr T, Bombara MP, Kelley KA | title = Expression of 5HT1a receptors on activated human T cells. Regulation of cyclic AMP levels and T cell proliferation by 5-hydroxytryptamine | journal = J. Immunol. | volume = 151 | issue = 3 | pages = 1175-83 | year = 1993 | pmid = 8393041 }}
* {{cite journal | vauthors = Parks CL, Shenk T | title = The serotonin 1a receptor gene contains a TATA-less promoter that responds to MAZ and Sp1 | journal = J. Biol. Chem. | volume = 271 | issue = 8 | pages = 4417-30 | year = 1996 | pmid = 8626793 | doi = 10.1074/jbc.271.8.4417 }}
* {{cite journal | vauthors = Stockmeier CA, Shapiro LA, Dilley GE, Kolli TN, Friedman L, Rajkowska G | title = Increase in serotonin-1A autoreceptors in the midbrain of suicide victims with major depression-postmortem evidence for decreased serotonin activity | journal = J. Neurosci. | volume = 18 | issue = 18 | pages = 7394-401 | year = 1998 | pmid = 9736659 }}
* {{cite journal | vauthors = Kawanishi Y, Harada S, Tachikawa H, Okubo T, Shiraishi H | title = Novel mutations in the promoter and coding region of the human 5-HT1A receptor gene and association analysis in schizophrenia | journal = Am. J. Med. Genet. | volume = 81 | issue = 5 | pages = 434-9 | year = 1998 | pmid = 9754630 | doi = 10.1002/(SICI)1096-8628(19980907)81:5<434::AID-AJMG13>3.0.CO;2-D }}
* {{cite journal | vauthors = Salim K, Fenton T, Bacha J, Urien-Rodriguez H, Bonnert T, Skynner HA, Watts E, Kerby J, Heald A, Beer M, McAllister G, Guest PC | title = Oligomerization of G-protein-coupled receptors shown by selective co-immunoprecipitation | journal = J. Biol. Chem. | volume = 277 | issue = 18 | pages = 15482-5 | year = 2002 | pmid = 11854302 | doi = 10.1074/jbc.M201539200 }}
* {{cite web|last=Panesar|first=Kiran|title=5-HT1A Receptors in Psychopharmacology|url=http://psychopharmacologyinstitute.com/cns-receptors/5-ht1a-receptors/|work=Web Article|publisher=Psychopharmacology Institute|accessdate=11 April 2013}}

== Ссылки ==

* {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2310 | title = 5-HT<sub>1A</sub> | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology }}

[[Категория:Серотониновые рецепторы]]
[[Категория:Белки человека]]

Версия от 10:27, 16 февраля 2015

The 5-HT1A receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). It is a G protein-coupled receptor (GPCR) that is coupled to Gi/Go and mediates inhibitory neurotransmission. HTR1A denotes the human gene encoding for the receptor.[1][2]

Распределение в организме

Физиологическая роль

Нейромодуляция

Эндокринные эффекты

Ауторецепторы

Лиганды

Агонисты

  • 8-OH-DPAT[3]
  • Alnespirone
  • Befiradol
  • Eptapirone
  • F-15,599
  • Lesopitron
  • MKC-242
  • LY-293,284
  • Osemozotan (partial at postsynaptic receptors)
  • Repinotan
  • U-92,016-A

Парциальные агонисты

  • 5-Carboxamidotryptamine (5-CT)
  • 5-Methoxytryptamine (5-MT)
  • 5-MeO-DMT
  • Adatanserin
  • alpha-Ethyltryptamine (αET)
  • alpha-Methyltryptamine (αMT)
  • Aripiprazole
  • Asenapine
  • Bay R 1531
  • Befiradol
  • Binospirone
  • Bufotenin
  • Buspirone
  • Cannabidiol
  • Clozapine
  • Dihydroergotamine
  • Ebalzotan
  • Eltoprazine
  • Ergotamine
  • Etoperidone
  • F-11,461
  • F-12,826
  • F-13,714
  • F-14,679
  • Flesinoxan
  • Flibanserin
  • Ginkgo Biloba[4]
  • Gepirone
  • Haloperidol
  • Ipsapirone
  • Lisuride
  • Lurasidone
  • LY-301,317
  • LSD
  • MDMA
  • Naluzotan
  • NBUMP
  • Nefazodone
  • Olanzapine
  • Perospirone
  • Piclozotan
  • Psilocin
  • Psilocybin
  • Quetiapine
  • Rauwolscine
  • RU-24,969
  • S-15,535
  • Sarizotan
  • SSR-181,507
  • Sunepitron
  • Tandospirone
  • Tiospirone
  • Trazodone
  • Trifluoromethylphenylpiperazine
  • Urapidil
  • Vortioxetine
  • Vilazodone
  • Xaliproden
  • Yohimbine
  • Zalospirone
  • Ziprasidone

Антагонисты

  • Alprenolol
  • AV-965
  • BMY-7,378
  • Cyanopindolol
  • Dotarizine
  • Flopropione
  • GR-46,611
  • Iodocyanopindolol
  • Isamoltane]
  • Lecozotan
  • Methiothepin
  • Methysergide
  • MPPF
  • NAN-190
  • Oxprenolol
  • Pindobind
  • Pindolol
  • Propranolol
  • Risperidone
  • Robalzotan
  • SB-649,915
  • SDZ-216,525
  • Spiperone
  • Spiramide
  • Spiroxatrine
  • UH-301
  • WAY-100,135
  • WAY-100,635
  • Xylamidine
  • Mefway

Генетика

Взаимодействия рецептора с другими белками

Олигомеры рецептора

См. также

Примечания

  1. ↑ "Deletion mapping of DNA markers to a region of chromosome 5 that cosegregates with schizophrenia". Genomics. 5 (4): 940–4. November 1989. doi:10.1016/0888-7543(89)90138-9. PMC 3154173. PMID 2591972. {{cite journal}}: Источник использует устаревший параметр |authors= (справка)Википедия:Обслуживание CS1 (дата и год) (ссылка)
  2. ↑ Entrez Gene: HTR1A 5-hydroxytryptamine (serotonin) receptor 1A.
  3. ↑ "Full and partial 5-HT1A receptor agonists disrupt learning and performance in rats" (PDF). J. Pharmacol. Exp. Ther. 288 (1): 335–47. January 1999. PMID 9862788. {{cite journal}}: Источник использует устаревший параметр |authors= (справка)Википедия:Обслуживание CS1 (дата и год) (ссылка)
  4. ↑ "The discriminative stimulus properties of EGb 761, an extract of Ginkgo biloba". Pharmacol. Biochem. Behav. 62 (3): 543–7. March 1999. doi:10.1016/S0091-3057(98)00190-7. PMID 10080249. {{cite journal}}: Источник использует устаревший параметр |authors= (справка)Википедия:Обслуживание CS1 (дата и год) (ссылка)

Для дополнительного чтения

Ссылки

  • 5-HT1A. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
Источник — https://ru.wikipedia.org/w/index.php?title=5-HT1A-рецептор&oldid=68626569