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Receptor de serotonina

Agosto 06, 2021

Los receptores de serotonina también conocidos como receptores de 5-hidroxitriptamina o receptores 5-HT son un tipo de receptor acoplado a proteínas G (en inglés GPCRs) y receptor ionotrópico (del inglés LGICs) ubicados en el sistema nervioso central y periférico.[1]​[2]​ Estos median la neurotransmisión tanto excitatoria como inhibitoria. Los receptores de serotonina (5HT), son activados por el neurotransmisor serotonina, el cual actúa como su ligando natural.

Los receptores de serotonina modulan la liberación de muchos neurotransmisores entre ellos el glutamato, GABA, dopamina, epinefrina / norepinefrina y acetilcolina, así como muchas hormonas, entre ellas oxitocina, prolactina, vasopresina, cortisol, corticotropina y sustancia P. Los receptores de serotonina modulan distintos procesos biológicos y neurológicos, como la agresión, la ansiedad, el apetito, la cognición, el aprendizaje, la memoria, el estado de ánimo, la náusea, el sueño y la termoregulación. Los receptores de serotonina son el objetivo de una variedad de fármacos y también de drogas no legales, que incluye muchos agentes antidepresivos, antipsicóticos, anorexígenos, antieméticos, procinéticos, antimigrañosos, alucinógenos, empatógenos y entactógenos.[3]​

Clasificación

Con la excepción del receptor 5-HT3, un canal iónico regulado por ligandos de la familia de receptores cys-loop, los demás receptores de serotonina son GPCRs que activan un segundo mensajero intracelular que produce una respuesta inhibitoria o excitatoria.

Familias

Familia Tipo Mecanismo Potencial
5-HT1 Gi/Go-acoplado a proteínas. Decrece los niveles celulares de cAMP. Inhibitorio
5-HT2 Gq/G11-acoplado a proteínas. Incrementa los niveles celulares de IP3 y DAG. Excitatorio
5-HT3 Receptor ionotrópico de Na+ y K+ canal iónico. despolarización membrana plasmática. Excitatorio
5-HT4 Gs-acoplado a proteínas. Incrementa los niveles intracelulares de cAMP. Excitatorio
5-HT5 Gi/Go-acoplado a proteínas.[4]​ Disminuye los niveles celulares de cAMP. Inhibitorio
5-HT6 Gs-acoplado a proteínas. Incrementa los niveles celulares de cAMP. Excitatorio
5-HT7 Gs-acoplado a proteínas. Incrementa los niveles celulares de cAMP. Excitatorio

Subtipos

Dentro de estos tipos de receptores de serotonina se ha caracterizado un número específico de subtipos:[5]​[6]​[7]​

Relación de receptores de serotonina
Receptor Gen(es) Distribución Función Agonistas Antagonistas
5-HT1A
  • Vasos sanguíneos
  • SNC
5-HT1B
  • Vasos sanguíneos
  • SNC
5-HT1D
  • Vasos sanguíneos
  • SNC
5-HT1E
  • Vasos sanguíneos
  • SNC
  • Metiotepin
5-HT1F
  • Vasos sanguíneos
  • SNC
  • Vasoconstricción
  • Metiotepin
5-HT2A
  • Vasos sanguíneos
  • SNC
  • Tracto GI
  • Plaquetas
  • SNP
  • Músculo liso
  • Adicción (potentially modulating)[41]​
  • Ansiedad[42]​
  • Apetito
  • Cognición
  • Imaginación
  • Aprendizaje
  • Memoria
  • Humor
  • Percepción
  • Comportamiento sexual[43]​
  • Sueño[44]​
  • Termoregulación[45]​
  • Vasoconstricción[46]​
5-HT2B
  • Vasos sanguíneos
  • SNC
  • Tracto GI
  • Plaquetas
  • SNP
  • Músculo liso
  • Ansiedad[47]​[48]​[49]​
  • Apetito[50]​
  • Función cardiovascular
  • Motilidad GI[51]​
  • Sueño[44]​
  • Vasoconstricción
5-HT2C
  • Vasos sanguíneos
  • SNC
  • Tracto GI
  • Plaquetas
  • SNP
  • Músculo liso
  • Adicción. (modulador potencial)[41]​
  • Ansiedad[52]​[53]​[54]​
  • Apetito
  • Motilidad GI[55]​
  • Movimiento
  • Estado de ánimo[54]​[53]​
  • Erección peneana[56]​[57]​
  • Comportamiento sexual[43]​
  • Sueño[58]​
  • Termoregulación[45]​
  • Vasoconstricción
5-HT3
  • SNC
  • Tracto GI
  • SNP
  • Adicción
  • Ansiedad
  • Vómito
  • Motilidad GI
  • Aprendizaje[60]​
  • Memoria[60]​
  • Náusea
  • 2-Metil-5-HT
  • BZP
  • Quipazina
  • RS-56812
5-HT4
  • SNC
  • Tracto GI
  • SNP
  • L-Lisina[61]​
  • Piboserod
5-HT5A
  • SNC
  • Asenapina
  • Dimebolin
  • Metiotepin
  • Ritanserin
  • SB-699,551
  • SB-699,551-A
5-HT6
  • CNS
  • EMD-386,088
  • EMDT
5-HT7
  • Vasos sanguíneo
  • SNC
  • TractoGI
  • 5-CT
  • 8-OH-DPAT
  • AS-19

Nótese que no existe el receptor 5-HT1C, después que el receptor fue clonado y luego caracterizado se encontró que tenía más en común con la familia de receptores 5-HT2 y fue designado como receptor 5-HT2C. Nótese también que no existe el receptor 5-HT5B receptor, este existe solamente en ratones y ratas, pero no en primates incluyendo los humanos.

Agonistas muy poco selectivos de los subtipos de receptor 5-HT incluye la ergotamina (un antimigrañoso), el cual activa los receptores 5-HT1A, 5-HT1D, 5-HT1B, D2 y el receptor de norepinefrina.[31]​ LSD (un psicodélico) es un agonista de los receptores 5-HT1A, 5-HT2A, 5-HT2C, 5-HT5A, 5-HT5, 5-HT6.[31]​

Referencias

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Enlaces externos

  • MeSH: Serotonin+Receptors (en inglés)
  • «5-Hydroxytryptamine Receptors». IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 
  • Rubenstein, LA, Lanzara RG (16 de febrero de 2005). «Activation of G protein-coupled receptors entails cysteine modulation of agonist binding». Cogprints. Consultado el 11 de abril de 2008. 
  •   Datos: Q238516

Agosto 06, 2021
receptor, serotonina, receptores, serotonina, también, conocidos, como, receptores, hidroxitriptamina, receptores, tipo, receptor, acoplado, proteínas, inglés, gpcrs, receptor, ionotrópico, inglés, lgics, ubicados, sistema, nervioso, central, periférico, estos. Los receptores de serotonina tambien conocidos como receptores de 5 hidroxitriptamina o receptores 5 HT son un tipo de receptor acoplado a proteinas G en ingles GPCRs y receptor ionotropico del ingles LGICs ubicados en el sistema nervioso central y periferico 1 2 Estos median la neurotransmision tanto excitatoria como inhibitoria Los receptores de serotonina 5HT son activados por el neurotransmisor serotonina el cual actua como su ligando natural Serotonina Los receptores de serotonina modulan la liberacion de muchos neurotransmisores entre ellos el glutamato GABA dopamina epinefrina norepinefrina y acetilcolina asi como muchas hormonas entre ellas oxitocina prolactina vasopresina cortisol corticotropina y sustancia P Los receptores de serotonina modulan distintos procesos biologicos y neurologicos como la agresion la ansiedad el apetito la cognicion el aprendizaje la memoria el estado de animo la nausea el sueno y la termoregulacion Los receptores de serotonina son el objetivo de una variedad de farmacos y tambien de drogas no legales que incluye muchos agentes antidepresivos antipsicoticos anorexigenos antiemeticos procineticos antimigranosos alucinogenos empatogenos y entactogenos 3 Indice 1 Clasificacion 1 1 Familias 1 2 Subtipos 2 Referencias 3 Enlaces externosClasificacion EditarCon la excepcion del receptor 5 HT3 un canal ionico regulado por ligandos de la familia de receptores cys loop los demas receptores de serotonina son GPCRs que activan un segundo mensajero intracelular que produce una respuesta inhibitoria o excitatoria Familias Editar Familia Tipo Mecanismo Potencial5 HT1 Gi Go acoplado a proteinas Decrece los niveles celulares de cAMP Inhibitorio5 HT2 Gq G11 acoplado a proteinas Incrementa los niveles celulares de IP3 y DAG Excitatorio5 HT3 Receptor ionotropico de Na y K canal ionico despolarizacion membrana plasmatica Excitatorio5 HT4 Gs acoplado a proteinas Incrementa los niveles intracelulares de cAMP Excitatorio5 HT5 Gi Go acoplado a proteinas 4 Disminuye los niveles celulares de cAMP Inhibitorio5 HT6 Gs acoplado a proteinas Incrementa los niveles celulares de cAMP Excitatorio5 HT7 Gs acoplado a proteinas Incrementa los niveles celulares de cAMP ExcitatorioSubtipos Editar Dentro de estos tipos de receptores de serotonina se ha caracterizado un numero especifico de subtipos 5 6 7 Relacion de receptores de serotoninaReceptor Gen es Distribucion Funcion Agonistas Antagonistas5 HT1A HGNC HTR1A Vasos sanguineos SNC Adiccion 8 9 10 Agresion 11 Ansiedad 12 Apetito 13 Presion sanguinea 14 15 Funcion cardiovascular 16 Vomito 17 Frecuencia cardiaca 14 15 Impulsividad 18 Memoria 19 20 Estado de animo 21 Nausea 17 Nocicepcion 22 Ereccion peneana 23 Dilatacion pupilar 24 Respiracion 25 Comportamiento sexual 26 Sueno 27 Sociabilidad 28 Termoregulacion 29 Vasoconstriccion 30 5 CT 8 OH DPAT Aripiprazola Buspirona 31 ansiolitico y antidepresivo 31 Cannabidiol Clozapina Dihidroergotamina Eltoprazina Ergotamina Flesinoxan Flibanserin Gepirone Ipsapirona Metisergida Nefazodona Quetiapina RU 24969 Tandospirona Trazodona Urapidil Xaliproden Yohimbina Ziprasidona Alprenolol Asenapina BMY 7378 Cyanopindolol Iodocyanopindolol Lecozotan Metiotepin NAN 190 Oxprenolol Pindolol Propranolol Robalzotan S15535 Spiperone UH 301 WAY 100 135 WAY 100 6355 HT1B HGNC HTR1B Vasos sanguineos SNC Adiccion 32 Agresion 11 Ansiedad 33 34 35 Aprendizaje 36 Movimiento 37 Memoria 36 Estado de animo 35 Ereccion peneana 23 Comportamiento sexual 26 Vasoconstriccion 5 CT CP 93 129 CP 94 253 Dihidroergotamina Eltoprazina Ergotamina Metisergida RU 24969 TFMPP Triptanes 31 antimigranoso 31 Zolmitriptan Eletriptan Sumatriptan Alprenolol AR A000002 Asenapina Cianopindolol GR 127935 Iodocianopindolol Isamoltana Metergolina Metiothepin Oxprenolol Pindolol Propanolol SB 216 641 Yohimbina5 HT1D HGNC HTR1D Vasos sanguineos SNC Ansiedad 38 39 Movimiento 37 Vasoconstriccion 5 CT Dihydroergotamina Ergotamina Metisergida Triptanes 31 antimigranoso 31 Almotriptan Eletriptan Frovatriptan Naratriptan Rizatriptan Sumatriptan Zolmitriptan Yohimbina BRL 15572 GR 127935 Ketanserina Metergolina Methiothepin Rauwolscina Ritanserin5 HT1E HGNC HTR1E Vasos sanguineos SNC Eletriptan Metisergida Triptamina Metiotepin5 HT1F HGNC HTR1F Vasos sanguineos SNC Vasoconstriccion Eletriptan Naratriptan Sumatriptan Lasmiditan 40 Metiotepin5 HT2A HGNC HTR2A Vasos sanguineos SNC Tracto GI Plaquetas SNP Musculo liso Adiccion potentially modulating 41 Ansiedad 42 Apetito Cognicion Imaginacion Aprendizaje Memoria Humor Percepcion Comportamiento sexual 43 Sueno 44 Termoregulacion 45 Vasoconstriccion 46 2C B 5 MeO DMT BZP Bufotenin DMT DOM Ergonovina Lisurida LSD Mescalina Myristicin Psilocina Psilocibina TFMPP Yohimbina 25i NBOMe Atypical antipsychotics Clozapina 31 Olanzapina Quetiapina Risperidona Ziprasidona Aripiprazol Asenapina Cyproheptadina Eplivanserin Etoperidona Iloperidona Ketanserina 31 antihipertensivo 31 Methysergida Mianserin Mirtazapina Nefazodona Pimavanserin Pizotifen Ritanserin Trazodona5 HT2B HGNC HTR2B Vasos sanguineos SNC Tracto GI Plaquetas SNP Musculo liso Ansiedad 47 48 49 Apetito 50 Funcion cardiovascular Motilidad GI 51 Sueno 44 Vasoconstriccion BW 723C86 Fenfluramina MDMA Norfenfluramina Ro60 0175 Agomelatina Asenapina BZP Ketanserina Methysergida Ritanserin Tegaserod Yohimbina5 HT2C HGNC HTR2C Vasos sanguineos SNC Tracto GI Plaquetas SNP Musculo liso Adiccion modulador potencial 41 Ansiedad 52 53 54 Apetito Motilidad GI 55 Movimiento Estado de animo 54 53 Ereccion peneana 56 57 Comportamiento sexual 43 Sueno 58 Termoregulacion 45 Vasoconstriccion A 372 159 AL 38022A Aripiprazol Ergonovina Lorcaserina Ro60 0175 TFMPP Trazodona 31 hipnotico 31 YM 348 Agomelatina 31 antidepresivo 31 Asenapina Clozapina 31 antisicotico 31 Ciproheptadina Dimebolin Eltoprazina Etoperidona Fluoxetina Iloperidona Ketanserina 31 antihipertensivo 31 Lisurida Metisergida 59 Mianserin Mirtazapina Nefazodona Olanzapina Quetiapina Risperidona Ritanserin Trazodona Ziprasidona5 HT3 HGNC HTR3A HGNC HTR3B HGNC HTR3C HGNC HTR3D HGNC HTR3E SNC Tracto GI SNP Adiccion Ansiedad Vomito Motilidad GI Aprendizaje 60 Memoria 60 Nausea 2 Metil 5 HT BZP Quipazina RS 56812 Alosetron Algunos antiemeticos 31 Dolasetron Ondansetron 31 Granisetron Tropisetron Clozapina Memantina Metoclopramida Mianserin Mirtazapina Olanzapina Quetiapina5 HT4 HGNC HTR4 SNC Tracto GI SNP Ansiedad 61 62 Apetito 63 64 Motilidad GI Aprendizaje 65 66 Memoria 65 66 67 Estado de animo 68 69 Respiracion 70 25 5 MT BIMU 8 Cinitaprida Cisaprida 31 procinetico Dazoprida Metoclopramida Mosaprida Prucaloprida RS 67333 Renzaprida Tegaserod Zacoprida L Lisina 61 Piboserod5 HT5A HGNC HTR5A SNC Movimiento 71 Sueno 72 5 CT Ergotamina Acido valerenico 72 Asenapina Dimebolin Metiotepin Ritanserin SB 699 551 SB 699 551 A5 HT6 HGNC HTR6 CNS Ansiedad 73 74 Cognicion 75 Aprendizaje 76 Memoria 76 Estado de animo 74 77 EMD 386 088 EMDT Aripiprazola Asenapina Clozapina Dimebolin EGIS 12233 Iloperidona MS 245 Olanzapina Ro04 6790 SB 258 585 SB 271 046 78 SB 357 134 SB 399 8855 HT7 HGNC HTR7 Vasos sanguineo SNC TractoGI Ansiedad 79 80 Memoria 81 82 Estado de animo 79 80 Respiracion 83 25 Sueno 79 83 84 Termoregulacion Vasoconstriccion 5 CT 8 OH DPAT AS 19 Aripiprazola Asenapina Clozapina EGIS 12233 Iloperidona Ketanserin Olanzapina Ritanserin SB 269 970Notese que no existe el receptor 5 HT1C despues que el receptor fue clonado y luego caracterizado se encontro que tenia mas en comun con la familia de receptores 5 HT2 y fue designado como receptor 5 HT2C Notese tambien que no existe el receptor 5 HT5B receptor este existe solamente en ratones y ratas pero no en primates incluyendo los humanos Agonistas muy poco selectivos de los subtipos de receptor 5 HT incluye la ergotamina un antimigranoso el cual activa los receptores 5 HT1A 5 HT1D 5 HT1B D2 y el receptor de norepinefrina 31 LSD un psicodelico es un agonista de los receptores 5 HT1A 5 HT2A 5 HT2C 5 HT5A 5 HT5 5 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sleep suppression induced by citalopram in rodents J Pharmacol Exp Ther 321 2 690 8 PMID 17314195 doi 10 1124 jpet 107 119404 Thomas DR Melotto S Massagrande M Gribble AD Jeffrey P Stevens AJ Deeks NJ Eddershaw PJ Fenwick SH Riley G Stean T Scott CM Hill MJ Middlemiss DN Hagan JJ Price GW Forbes IT 2003 SB 656104 A a novel selective 5 HT7 receptor antagonist modulates REM sleep in rats Br J Pharmacol 139 4 705 14 PMC 1573887 PMID 12812993 doi 10 1038 sj bjp 0705290 Enlaces externos EditarMeSH Serotonin Receptors en ingles 5 Hydroxytryptamine Receptors IUPHAR Database of Receptors and Ion Channels International Union of Basic and Clinical Pharmacology Rubenstein LA Lanzara RG 16 de febrero de 2005 Activation of G protein coupled receptors entails cysteine modulation of agonist binding Cogprints Consultado el 11 de abril de 2008 Datos Q238516Obtenido de https es wikipedia org w index php title Receptor de serotonina amp oldid 135902931, wikipedia, wiki, leyendo, leer, libro, 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