セロトニン受容体、セロトニンレセプター、5-HT受容体、5-HTレセプター

関: serotonin receptor

WordNet

the 8th letter of the Roman alphabet (同)h
a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response

PrepTutorEJDIC

hydrogenの化学記号
鉛筆の硬度 / 《俗》heroin
=sense organ / 受信装置

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/12/15 08:05:59」(JST)

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The 5-HT_1B receptor as an example of a metabotropic serotonin receptor. Its crystallographic structure in ribbon representation

The serotonin receptors, also known as 5-hydroxytryptamine receptors or 5-HT receptors, are a group of G protein-coupled receptors (GPCRs) and ligand-gated ion channels (LGICs) found in the central and peripheral nervous systems.^[1]^[2] They mediate both excitatory and inhibitory neurotransmission. The serotonin receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand.

The serotonin receptors modulate the release of many neurotransmitters, including glutamate, GABA, dopamine, epinephrine / norepinephrine, and acetylcholine, as well as many hormones, including oxytocin, prolactin, vasopressin, cortisol, corticotropin, and substance P, among others. The serotonin receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, and thermoregulation. The serotonin receptors are the target of a variety of pharmaceutical drugs, including many antidepressants, antipsychotics, anorectics, antiemetics, gastroprokinetic agents, antimigraine agents, hallucinogens, and entactogens.^[3]

Serotonin receptors are found in almost all animals and humans and are even known to regulate longevity and behavioral aging in the primitive nematode, Caenorhabditis elegans.^[4]^[5]

Classification

With the exception of the 5-HT₃ receptor, a ligand-gated ion channel, all other serotonin receptors are G protein-coupled receptors that activate an intracellular second messenger cascade to produce an excitatory or inhibitory response. In 2014 a novel 5-HT receptor was described that was isolated from the small white butterfly, Pieris rapae, and named pr5-HT₈. It shares relatively low similarity to the known 5-HT receptor classes and does not occur in mammals.^[6]

Families

Family	Type	Mechanism	Potential
5-HT₁	G_i/G_o-protein coupled.	Decreasing cellular levels of cAMP.	Inhibitory
5-HT₂	G_q/G₁₁-protein coupled.	Increasing cellular levels of IP₃ and DAG.	Excitatory
5-HT₃	Ligand-gated Na⁺ and K⁺ cation channel.	Depolarizing plasma membrane.	Excitatory
5-HT₄	G_s-protein coupled.	Increasing cellular levels of cAMP.	Excitatory
5-HT₅	G_i/G_o-protein coupled.^[7]	Decreasing cellular levels of cAMP.	Inhibitory
5-HT₆	G_s-protein coupled.	Increasing cellular levels of cAMP.	Excitatory
5-HT₇	G_s-protein coupled.	Increasing cellular levels of cAMP.	Excitatory

Subtypes

The 7 general serotonin receptor classes include a total of 14 known serotonin receptors.^[8] The specific types have been characterized as follows:^[9]^[10]^[11]

Overview of Serotonin Receptors


Receptor (first cloned)	Gene(s)	Distribution	Function	Agonists	Antagonists	Uses of drugs that act on this receptor
5-HT_1A (1987)	HTR1A	Blood Vessels CNS	Addiction ^[12]^[13]^[14] Aggression^[15] Anxiety^[16] Appetite^[17] Autoreceptor Blood Pressure^[18]^[19] Cardiovascular Function^[20] Emesis^[21] Heart Rate^[18]^[19] Impulsivity^[22] Memory^[23]^[24] Mood^[25] Nausea^[21] Nociception^[26] Penile Erection^[27] Pupil Dilation^[28] Respiration^[29] Sexual Behavior^[30] Sleep^[31] Sociability^[32] Thermoregulation^[33] Vasoconstriction^[34]	Selective (for 5-HT_1A over other 5-HT receptors) F-15,599 (research compound, highly potent and selective for 5-HT_1A) Flesinoxan (potent, EC₅₀ = 24 nM) Gepirone (partial agonist, K_i = 70 nM) Haloperidol Ipsapirone (partial agonist, K_i = 12.1 nM) Quetiapine Trazodone (SARI, selective in the sense that on all other 5-HT receptors it acts as either an antagonist or has no action. K_d = 78nM) Yohimbine (unselective partial agonist) Tandospirone (potent and selective partial agonist) Nonselective 5-CT (potent - K_i = 250±50 pM) 8-OH-DPAT (potent) Aripiprazole (atypical antipsychotic) Asenapine (atypical antipsychotic) Buspirone^[35] (partial agonist) Vortioxetine (high-efficacy partial agonist)^[36] Ziprasidone (Partial agonist, K_i = 3.4 nM)	BMY 7378 Cyanopindolol Iodocyanopindolol Lecozotan Methiothepin Methysergide^[37] NAN-190 Nebivolol Nefazodone WAY-100,135 WAY-100,635 Mefway	Analgesics (agonists) Antidepressants (post-synaptic receptor agonists and pre-synaptic autoreceptor antagonists serve as antidepressants) Anxiolytics^[38] (antagonist)
5-HT_1B (1992)	HTR1B	Blood Vessels CNS	Addiction ^[39] Aggression^[15] Anxiety^[40]^[41]^[42] Autoreceptor Learning^[43] Locomotion^[44] Memory^[43] Mood^[42] Penile Erection^[27] Sexual Behavior^[30] Vasoconstriction	5-CT CGS-12066A CP-93,129 CP-94,253 Dihydroergotamine Eltoprazine Ergotamine Methysergide RU 24969 TFMPP Triptans^[35] (antimigraine^[35]) Zolmitriptan Eletriptan Sumatriptan Vortioxetine (partial agonist, K_i = 33 nM)^[36]	Alprenolol AR-A000002 Asenapine Cyanopindolol GR-127,935 Iodocyanopindolol Isamoltane Metergoline Methiothepin Oxprenolol Pindolol Propranolol SB-216,641 Yohimbine	Migraines (e.g. triptans)
5-HT_1D (1991)	HTR1D	Blood Vessels CNS	Anxiety^[45]^[46] Autoreceptor Locomotion^[44] Vasoconstriction	5-CT CP-135,807 Dihydroergotamine Ergotamine Methysergide Triptans^[35] (antimigraine^[35]) Almotriptan Eletriptan Frovatriptan Naratriptan Rizatriptan Sumatriptan Zolmitriptan Yohimbine	BRL-15572 GR-127,935 Ketanserin Metergoline Methiothepin Rauwolscine Ritanserin Vortioxetine (K_i = 54 nM)^[36] Ziprasidone	Migraines (e.g. triptans)
5-HT_1E (1992)	HTR1E	Blood Vessels CNS		BRL-54443		None known
5-HT_1F (1993)	HTR1F	CNS	Migraine	BRL-54443 Lasmiditan LY-334,370 Naratriptan		None known
5-HT_2A (1988)	HTR2A	Blood Vessels CNS GI Tract Platelets PNS Smooth Muscle	Addiction (potentially modulating) ^[47] Anxiety^[48] Appetite Cognition Imagination Learning Memory Mood Perception Sexual Behavior^[49] Sleep^[50] Thermoregulation^[51] Vasoconstriction^[52]	25I-NBOMe (Full agonist) 2C-B 5-MeO-DMT BZP Bufotenin DMT DOM Ergonovine Lisuride LSD Mescaline Myristicin PNU-22394 (Partial agonist)^[53]^[54]^[55] Psilocin Psilocybin TFMPP (partial agonist or antagonist)	Atypical antipsychotics Clozapine^[35] Olanzapine Quetiapine Risperidone Ziprasidone Aripiprazole Asenapine Amitriptyline Clomipramine Cyproheptadine Eplivanserin Etoperidone Haloperidol Hydroxyzine Iloperidone Ketanserin^[35] (antihypertensive^[35]) Methysergide Mianserin Mirtazapine Nefazodone Pimavanserin Pizotifen Ritanserin Trazodone Yohimbine	Atypical antipsychotics (antagonist) Psychedelics (partial agonists) NaSSAs (antidepressants and anxiolytics; they serve as antagonists at this site) Treating serotonin syndrome (antagonists; e.g. cyproheptadine) Sleeping aid (antagonists; e.g. trazodone)
5-HT_2B (1992)	HTR2B	Blood Vessels CNS GI Tract Platelets PNS Smooth Muscle	Anxiety^[56]^[57]^[58] Appetite^[59] Cardiovascular Function GI Motility^[60] Sleep^[50] Vasoconstriction	BW-723C86 Fenfluramine MDMA Norfenfluramine PNU-22394 (Partial agonist)^[53]^[54]^[55] Ro60-0175	Agomelatine Asenapine BZP Ketanserin Methysergide Ritanserin RS-127,445 Tegaserod Yohimbine	Migraines (antagonists)
5-HT_2C (1988)	HTR2C	Blood Vessels CNS GI Tract Platelets PNS Smooth Muscle	Addiction. (potentially modulating)^[47] Anxiety^[61]^[62]^[63] Appetite GI Motility^[64] Heteroreceptor for norepinephrine and dopamine Locomotion Mood^[62]^[63] Penile Erection^[65]^[66] Sexual Behavior^[49] Sleep^[67] Thermoregulation^[51] Vasoconstriction	A-372,159 AL-38022A Aripiprazole Ergonovine Lorcaserin PNU-22394 (Full agonist)^[53]^[54]^[55] Ro60-0175 TFMPP Trazodone^[35] (hypnotic^[35]) YM-348	Agomelatine^[35] (antidepressant^[35]) Amitriptyline Asenapine Clomipramine Clozapine^[35] (antipsychotic^[35]) Cyproheptadine Dimebolin Eltoprazine Etoperidone Fluoxetine Haloperidol Iloperidone Ketanserin^[35] (antihypertensive^[35]) Lisuride Methysergide^[68] Mianserin Mirtazapine Nefazodone Olanzapine Paroxetine Quetiapine Risperidone Ritanserin Tramadol Trazodone Ziprasidone	Antidepressant (e.g. agomelatine, fluoxetine, mirtazapine) Orexigenic (e.g. mirtazapine, clozapine and olanzapine; antagonists) Anorectic (Lorcaserin) Antipsychotic (Vabicaserin; agonists)
5-HT₃ (1993)	HTR3A HTR3B HTR3C HTR3D HTR3E	CNS GI Tract PNS	Addiction Anxiety Emesis GI Motility^[69] Learning^[70] Memory^[70] Nausea	2-Methyl-5-HT BZP Quipazine RS-56812	Alosetron Several antiemetics^[35] Dolasetron Ondansetron^[35] Granisetron Tropisetron Clozapine Memantine Metoclopramide Mianserin Mirtazapine Olanzapine Quetiapine Vortioxetine (K_i = 3.7 nM)^[36]	Antiemetic
5-HT₄ (1995)	HTR4	CNS GI Tract PNS	Anxiety^[71]^[72] Appetite^[73]^[74] GI Motility Learning^[75]^[76] Memory^[75]^[76]^[77] Mood^[78]^[79] Respiration^[80]	5-MT BIMU-8 Cinitapride Cisapride^[35] (gastroprokinetic) Dazopride Metoclopramide Mosapride Prucalopride RS-67333 Renzapride Tegaserod Zacopride	L-Lysine^[71] Piboserod	Gastroprokinetics (e.g. Tegaserod)
5-HT_5A (1994)	HTR5A	CNS	Autoreceptor Locomotion^[81] Sleep^[82]	5-CT Ergotamine Valerenic Acid (partial agonist)^[82]	Asenapine Dimebolin Methiothepin Ritanserin SB-699,551 SB-699,551-A	None thus far
5-HT_5B (1993)	HTR5BP	functions in rodents, pseudogene in humans				None thus far
5-HT₆ (1993)	HTR6	CNS	Anxiety^[83]^[84] Cognition^[85] Learning^[86] Memory^[86] Mood^[84]^[87]	EMD-386,088 EMDT	Amitriptyline Aripiprazole Asenapine Clomipramine Clozapine Dimebolin EGIS-12233 Haloperidol Iloperidone MS-245 Olanzapine Ro04-6790 SB-258,585 SB-271,046^[88] SB-357,134 SB-399,885	Antidepressant (antagonists and agonists) Anxiolytic (antagonists and agonist) Nootropic (antagonists) Anorectic (antagonists)
5-HT₇ (1993)	HTR7	Blood Vessels CNS GI Tract	Anxiety^[89]^[90] Autoreceptor Memory^[91]^[92] Mood^[89]^[90] Respiration^[29]^[93] Sleep^[89]^[93]^[94] Thermoregulation Vasoconstriction	5-CT 8-OH-DPAT Aripiprazole (weak partial agonist)^[95] AS-19 E-55888 RA-7	Amitriptyline Asenapine Clomipramine Clozapine EGIS-12233 Haloperidol Iloperidone Imipramine Ketanserin Mirtazapine Olanzapine Ritanserin Risperidone SB-269,970 Vortioxetine (K_i = 19 nM)^[36]	Antidepressant (antagonists) Anxiolytics (antagonists) Nootropic (antagonists)

Note that there is no 5-HT_1C receptor since, after the receptor was cloned and further characterized, it was found to have more in common with the 5-HT₂ family of receptors and was redesignated as the 5-HT_2C receptor.

Very nonselective agonists of 5-HT receptor subtypes include ergotamine (an antimigraine), which activates 5-HT1A, 5-HT1D, 5-HT1B, D2 and norepinephrine receptors.^[35] LSD (a psychedelic) is a 5-HT1A, 5-HT2A, 5-HT2C, 5-HT5A, 5-HT5, 5-HT6 agonist.^[35]

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External links

Serotonin Receptors at the US National Library of Medicine Medical Subject Headings (MeSH)
"5-Hydroxytryptamine Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
Rubenstein, LA, Lanzara RG (2005-02-16). "Activation of G protein-coupled receptors entails cysteine modulation of agonist binding". Cogprints. Retrieved 2008-04-11.

UpToDate Contents

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1. セロトニンモジュレータ：薬理学、投与、および副作用 serotonin modulators pharmacology administration and side effects
2. 選択的セロトニン再取り込み阻害剤：薬理学、投与方法、および副作用 selective serotonin reuptake inhibitors pharmacology administration and side effects
3. 統合失調症に対する薬物療法：持効性抗精神病薬注射製剤 pharmacotherapy for schizophrenia long acting injectable antipsychotic drugs
4. 麻酔後ケア病棟における合併症発生の概要 overview of complications occurring in the post anesthesia care unit
5. 制吐剤の特性 characteristics of antiemetic drugs

English Journal

Early maternal deprivation-induced modifications in the neurobiological, neurochemical and behavioral profile of adult rats.

Rentesi G, Antoniou K, Marselos M, Syrrou M, Papadopoulou-Daifoti Z, Konstandi M.SourceDepartment of Pharmacology, Medical School, University of Ioannina, Ioannina GR-45110, Greece.
Behavioural brain research.Behav Brain Res.2013 May 1;244:29-37. doi: 10.1016/j.bbr.2013.01.040. Epub 2013 Feb 6.
Early maternal deprivation (MD) is an animal model of neurodevelopmental stress associated with a variety of abnormalities during adulthood. The present study investigated specific behavioral, neurochemical and neurobiological parameters related to dopaminergic and serotonergic function in adult rat
PMID 23395600

Is behavioral sensitization to 3,4-methylenedioxymethamphetamine (MDMA) mediated in part by cholinergic receptors?

Lettfuss NY, Seeger-Armbruster S, von Ameln-Mayerhofer A.SourceDepartment of Neuropharmacology, Institute of Neurobiology, University of Tuebingen, Auf der Morgenstelle 28E, 72076 Tuebingen, Germany. Electronic address: nlettfuss@aol.com.
Behavioural brain research.Behav Brain Res.2013 May 1;244:116-9. doi: 10.1016/j.bbr.2013.01.033. Epub 2013 Feb 1.
Behavioral sensitization to the repeated administration of a psychostimulant presumably plays a key role in the pathogenesis of addiction and schizophrenia. Among other psychostimulants, 3,4-methylenedioxymethamphetamine (MDMA) is known to produce behavioral sensitization, too, but its mechanism of
PMID 23380677

The role of 5-HT7 receptor antagonism in the amelioration of MK-801-induced learning and memory deficits by the novel atypical antipsychotic drug lurasidone.

Horisawa T, Nishikawa H, Toma S, Ikeda A, Horiguchi M, Ono M, Ishiyama T, Taiji M.SourcePharmacology Research Laboratories, Dainippon Sumitomo Pharma Co., Ltd., 33-94 Enoki-cho, Suita, Osaka 564-0053, Japan. Electronic address: tomoko-horisawa@ds-pharma.co.jp.
Behavioural brain research.Behav Brain Res.2013 May 1;244:66-9. doi: 10.1016/j.bbr.2013.01.026. Epub 2013 Jan 31.
Lurasidone is a novel atypical antipsychotic with high affinity for dopamine D, serotonin 5-HT and 5-HT receptors. We previously reported that lurasidone and the selective 5-HT receptor antagonist, SB-656104-A improved learning and memory deficits induced by MK-801, an N-methyl-d-aspartate (NMDA) re
PMID 23376699

Japanese Journal

Anti-emetic Effect of Mosapride Citrate Hydrate, a 5-HT? Receptor Agonist, on Selective Serotonin Reuptake Inhibitors (SSRIs)-Induced Emesis in Experimental Animals

Mine Yukiko,Oku Seiko,Yoshida Naoyuki
Journal of pharmacological sciences 121(1), 58-66, 2013-01-00
NAID 40019554461

ストレス適応形成に関わる機能分子としての脳内5-HT_7受容体の役割

辻稔,竹内智子,宮川和也,武田弘志
日本神経精神薬理学雑誌 = Japanese journal of psychopharmacology 32(4), 187-193, 2012-08-25
NAID 10031055680

Serotonin Potentiates High-Glucose-Induced Endothelial Injury : the Role of Serotonin and 5-HT_<2A> Receptors in Promoting Thrombosis in Diabetes

YAMADA Kumi,NIKI Hisae,NAGAI Hitoshi,NISHIKAWA Masakuni,NAKAGAWA Haruto
Journal of pharmacological sciences 119(3), 243-250, 2012-07-20
NAID 10030986931

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★リンクテーブル★

リンク元	「serotonin receptor」「セロトニンレセプター」「5-HTレセプター」
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関: 5-HT receptor、5-HT1A receptor、5-HT1A serotonin receptor、5-HT1B receptor、5-HT2A receptor、5-HT2C receptor、5-HT3 receptor

「セロトニンレセプター」

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英: serotonin receptor、5-HT receptor
関: セロトニン受容体、5-HTレセプター、5-HT受容体

「5-HTレセプター」

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英: 5-HT receptor
関: セロトニン受容体、セロトニンレセプター、5-HT受容体

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[pharmamotion-35] ^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k ^l ^m ⁿ ^o ^p ^q ^r ^s ^t ^u Pharmacology Corner > Serotonin (5-HT): receptors, agonists and antagonists By Flavio Guzmán, M.D. on 9/08/09

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