wikipedia - 5-ht receptor (for check)

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The 5-HT1B receptor as an example ofa metabotropic serotonin receptor. Itscrystallographic structure in ribbonrepresentation

5-HT receptorFrom Wikipedia, the free encyclopedia

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 excitatoryand 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, andsubstance 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 ofpharmaceutical drugs, including many antidepressants, antipsychotics, anorectics, antiemetics, gastroprokinetic agents, antimigraine agents,hallucinogens, and entactogens.[3]

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

Contents1 Classification

1.1 Families1.2 Subtypes

2 References3 External links

ClassificationWith 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 messengercascade 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 Potential5-HT1 Gi/Go-protein coupled. Decreasing cellular levels of cAMP. Inhibitory5-HT2 Gq/G11-protein coupled. Increasing cellular levels of IP3 and DAG. Excitatory5-HT3 Ligand-gated Na+ and K+ cation channel. Depolarizing plasma membrane. Excitatory5-HT4 Gs-protein coupled. Increasing cellular levels of cAMP. Excitatory5-HT5 Gi/Go-protein coupled.[7] Decreasing cellular levels of cAMP. Inhibitory5-HT6 Gs-protein coupled. Increasing cellular levels of cAMP. Excitatory5-HT7 Gs-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(firstcloned)

Gene(s) Distribution Function Agonists Antagonists Uses of drugs that acton this receptor

Selective (for 5-HT1Aover other 5-HTreceptors)

F-15,599 (researchcompound, highlypotent andselective for 5-HT1A)Flesinoxan (potent,EC50 = 24 nM)Gepirone (partial



5-HT1A(1987)

HTR1A(http://www.genenames.org/data/hgnc_data.php?match=HTR1A)

BloodVesselsCNS

Addiction [12][13][14]Aggression[15]Anxiety[16]Appetite[17]AutoreceptorBloodPressure[18][19]CardiovascularFunction[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]

agonist, Ki = 70nM)HaloperidolIpsapirone (partialagonist, Ki = 12.1nM)QuetiapineTrazodone (SARI,selective in thesense that on allother 5-HTreceptors it acts aseither an antagonistor has no action.Kd = 78nM)Yohimbine(unselective partialagonist)Tandospirone(potent andselective partialagonist)

Nonselective

5-CT (potent - Ki =25050 pM)8-OH-DPAT(potent)Aripiprazole(atypicalantipsychotic)Asenapine(atypicalantipsychotic)Buspirone[35](partial agonist)Vortioxetine (high-efficacy partialagonist)[36]Ziprasidone(Partial agonist, Ki= 3.4 nM)

BMY 7378CyanopindololIodocyanopindololLecozotanMethiothepinMethysergide[37]NAN-190NebivololNefazodoneWAY-100,135WAY-100,635Mefway

Analgesics(agonists)Antidepressants(post-synapticreceptor agonistsand pre-synapticautoreceptorantagonists serveasantidepressants)Anxiolytics(antagonist)

5-HT1B(1992)

HTR1B(http://www.genenames.org/data/hgnc_data.php?match=HTR1B)

BloodVesselsCNS

Addiction [39]Aggression[15]Anxiety[40][41][42]AutoreceptorLearning[43]Locomotion[44]Memory[43]Mood[42]Penile Erection[27]Sexual Behavior[30]Vasoconstriction

5-CTCGS-12066ACP-93,129CP-94,253DihydroergotamineEltoprazineErgotamineMethysergideRU 24969TFMPPTriptans[35](antimigraine[35])

ZolmitriptanEletriptanSumatriptan

Vortioxetine(partial agonist, Ki= 33 nM)[36]

AlprenololAR-A000002AsenapineCyanopindololGR-127,935IodocyanopindololIsamoltaneMetergolineMethiothepinOxprenololPindololPropranololSB-216,641Yohimbine

Migrainestriptans

5-HT1D(1991)

HTR1D(http://www.genenames.org/data/hgnc_data.php?match=HTR1D)

BloodVesselsCNS

Anxiety[45][46]AutoreceptorLocomotion[44]Vasoconstriction

5-CTCP-135,807DihydroergotamineErgotamineMethysergideTriptans[35](antimigraine[35])

AlmotriptanEletriptanFrovatriptanNaratriptan

BRL-15572GR-127,935KetanserinMetergolineMethiothepinRauwolscineRitanserinVortioxetine (Ki = 54

Migrainestriptans



RizatriptanSumatriptanZolmitriptan

Yohimbine

nM)[36]Ziprasidone

5-HT1E(1992)

HTR1E(http://www.genenames.org/data/hgnc_data.php?match=HTR1E)

BloodVesselsCNS

BRL-54443 None known

5-HT1F(1993)

HTR1F(http://www.genenames.org/data/hgnc_data.php?match=HTR1F)

CNS MigraineBRL-54443LasmiditanLY-334,370Naratriptan

None known

5-HT2A(1988)


BloodVesselsCNSGI TractPlateletsPNSSmoothMuscle

Addiction(potentiallymodulating) [47]Anxiety[48]AppetiteCognitionImaginationLearningMemoryMoodPerceptionSexual Behavior[49]Sleep[50]Thermoregulation[51]Vasoconstriction[52]

25I-NBOMe (Fullagonist)2C-B5-MeO-DMTBZPBufoteninDMTDOMErgonovineLisurideLSDMescalineMyristicinPNU-22394(Partialagonist)[53][54][55]PsilocinPsilocybinTFMPP (partialagonist orantagonist)

Atypicalantipsychotics

Clozapine[35]OlanzapineQuetiapineRisperidoneZiprasidone

AripiprazoleAsenapineAmitriptylineClomipramineCyproheptadineEplivanserinEtoperidoneHaloperidolHydroxyzineIloperidoneKetanserin[35](antihypertensive[35])MethysergideMianserinMirtazapineNefazodonePimavanserinPizotifenRitanserinTrazodoneYohimbine

Atypicalantipsychotics(antagonist)Psychedelics(partial agonists)NaSSAs(antidepressantsand anxiolytics;they serve asantagonists atthis site)Treatingserotoninsyndrome(antagonists; e.g.cyproheptadineSleeping aid(antagonists; e.g.trazodone)

5-HT2B(1992)

HTR2B(http://www.genenames.org/data/hgnc_data.php?match=HTR2B)

BloodVesselsCNSGI TractPlateletsPNSSmoothMuscle

Anxiety[56][57][58]Appetite[59]CardiovascularFunctionGI Motility[60]Sleep[50]Vasoconstriction

BW-723C86FenfluramineMDMANorfenfluraminePNU-22394(Partialagonist)[53][54][55]Ro60-0175

AgomelatineAsenapineBZPKetanserinMethysergideRitanserinRS-127,445TegaserodYohimbine

Migraines(antagonists)

5-HT2C(1988)

HTR2C(http://www.genenames.org/data/hgnc_data.php?match=HTR2C)

BloodVesselsCNSGI TractPlateletsPNS

Addiction.(potentiallymodulating)[47]Anxiety[61][62][63]AppetiteGI Motility[64]Heteroreceptor fornorepinephrine anddopamineLocomotionMood[62][63]

A-372,159AL-38022AAripiprazoleErgonovineLorcaserinPNU-22394 (Fullagonist)[53][54][55]Ro60-0175TFMPP

Agomelatine[35](antidepressant[35])AmitriptylineAsenapineClomipramineClozapine[35](antipsychotic[35])CyproheptadineDimebolinEltoprazineEtoperidoneFluoxetineHaloperidolIloperidoneKetanserin[35](antihypertensive[35])

Antidepressant(e.g.agomelatinefluoxetinemirtazapineOrexigenicmirtazapine,clozapine andolanzapine;antagonists)



SmoothMuscle

PenileErection[65][66]Sexual Behavior[49]Sleep[67]Thermoregulation[51]Vasoconstriction

Trazodone[35](hypnotic[35])YM-348

LisurideMethysergide[68]MianserinMirtazapineNefazodoneOlanzapineParoxetineQuetiapineRisperidoneRitanserinTramadolTrazodoneZiprasidone

Anorectic(Lorcaserin)Antipsychotic(Vabicaserin;agonists)

5-HT3(1993)

HTR3A(http://www.genenames.org/data/hgnc_data.php?match=HTR3A)HTR3B(http://www.genenames.org/data/hgnc_data.php?match=HTR3B)HTR3C(http://www.genenames.org/data/hgnc_data.php?match=HTR3C)HTR3D(http://www.genenames.org/data/hgnc_data.php?match=HTR3D)HTR3E(http://www.genenames.org/data/hgnc_data.php?match=HTR3E)

CNSGI TractPNS

AddictionAnxietyEmesisGI Motility[69]Learning[70]Memory[70]Nausea

2-Methyl-5-HTBZPQuipazineRS-56812

AlosetronSeveralantiemetics[35]

DolasetronOndansetron[35]GranisetronTropisetron

ClozapineMemantineMetoclopramideMianserinMirtazapineOlanzapineQuetiapineVortioxetine (Ki = 3.7nM)[36]

Antiemetic

5-HT4(1995)

HTR4(http://www.genenames.org/data/hgnc_data.php?match=HTR4)

CNSGI TractPNS

Anxiety[71][72]Appetite[73][74]GI MotilityLearning[75][76]Memory[75][76][77]Mood[78][79]Respiration[29][80]

5-MTBIMU-8CinitaprideCisapride[35](gastroprokinetic)DazoprideMetoclopramideMosapridePrucaloprideRS-67333RenzaprideTegaserodZacopride

L-Lysine[71]Piboserod

Gastroprokinetics(e.g. Tegaserod)

5-HT5A(1994)


CNSAutoreceptorLocomotion[81]Sleep[82]

5-CTErgotamineValerenic Acid(partial agonist)[82]

AsenapineDimebolinMethiothepinRitanserinSB-699,551SB-699,551-A

None thus far

5-HT5B(1993)

HTR5BP(http://www.genenames.org/data/hgnc_data.php?match=HTR5BP)

functions inrodents,pseudogene inhumans

None thus far

5-HT6(1993)


CNS

Anxiety[83][84]Cognition[85]Learning[86]Memory[86]Mood[84][87]

EMD-386,088EMDT

AmitriptylineAripiprazoleAsenapineClomipramineClozapineDimebolinEGIS-12233HaloperidolIloperidoneMS-245OlanzapineRo04-6790SB-258,585

Antidepressant(antagonists andagonists)Anxiolytic(antagonists andagonist)Nootropic(antagonists)Anorectic(antagonists)



SB-271,046[88]SB-357,134SB-399,885

5-HT7(1993)


BloodVesselsCNSGI Tract

Anxiety[89][90]AutoreceptorMemory[91][92]Mood[89][90]Respiration[29][93]Sleep[89][93][94]ThermoregulationVasoconstriction

5-CT8-OH-DPATAripiprazole (weakpartial agonist)[95]AS-19E-55888RA-7

AmitriptylineAsenapineClomipramineClozapineEGIS-12233HaloperidolIloperidoneImipramineKetanserinMirtazapineOlanzapineRitanserinRisperidoneSB-269,970Vortioxetine (Ki = 19nM)[36]

Antidepressant(antagonists)Anxiolytics(antagonists)Nootropic(antagonists)

Note that there is no 5-HT1C 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 andwas redesignated as the 5-HT2C 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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90. Wesolowska A, Nikiforuk A, Stachowicz K, Tatarczynska E (September 2006). "Effect of the selective 5-HT7 receptor antagonist SB 269970 in animal models of anxiety and depression".Neuropharmacology 51 (3): 57886. doi:10.1016/j.neuropharm.2006.04.017 (https://dx.doi.org/10.1016%2Fj.neuropharm.2006.04.017). PMID 16828124(https://www.ncbi.nlm.nih.gov/pubmed/16828124).

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External linksSerotonin Receptors (https://www.nlm.nih.gov/cgi/mesh/2011/MB_cgi?mode=&term=Serotonin+Receptors) at the US National Library of Medicine Medical SubjectHeadings (MeSH)"5-Hydroxytryptamine Receptors" (http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1288). 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" (http://cogprints.org/4095/).Cogprints. Retrieved 2008-04-11.

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Categories: G protein coupled receptors Ionotropic receptors

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95. Davies MA, Sheffler DJ, Roth BL. Aripiprazole: A Novel Atypical Antipsychotic Drug With a Uniquely Robust Pharmacology. CNS Drug Reviews [Internet]. 2004 [cited 2013 Aug 4];10(4):31736. Available from: http://onlinelibrary.wiley.com/doi/10.1111/j.1527-3458.2004.tb00030.x/pdf

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