Серотониновые рецепторы: различия между версиями

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===Подтипы===
===Подтипы===
===Subtypes===

Within these general classes of serotonin receptors, a number of specific types have been characterized:<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 | authorlink = | coauthors = | date = 2000-01-01 | work = | publisher = American College of Neurophyscopharmacology | pages = | language = | quote = | archiveurl= http://web.archive.org/web/20080421160353/http://www.acnp.org/g4/GN401000039/Ch039.html| archivedate= 21 April 2008 <!--DASHBot-->| deadurl= no}}</ref><ref name="urlIUPHAR DATABASE | 5-HYDROXYTRYPTAMINE RECEPTORS">{{cite web | url = http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1288 | title = 5-Hydroxytryptamine Receptors | accessdate = 2008-04-11 | author = | authorlink = | coauthors = | date = | format = | work = IUPHAR Receptor Database | publisher = International Union of Basic and Clinical Pharmacology | pages = | language = | archiveurl = | archivedate = | quote = }}</ref><ref name="Wesolowska_2002">{{cite journal |author=Wesolowska A |title=In the search for selective ligands of 5-HT<sub>5</sub>, 5-HT<sub>6</sub> and 5-HT<sub>7</sub> serotonin receptors |journal=Polish Journal of Pharmacology |volume=54 |issue=4 |pages=327–41 |year=2002 |pmid=12523486 |url=http://www.if-pan.krakow.pl/pjp/pdf/2002/4_327.pdf|format=PDF}}</ref>

{| class="wikitable"
|colspan=7| <center>
=== Обзор серотониновых рецепторов ===
</center>
|-
| '''Рецептор''' <br>(впервые клонирован)
! Ген
! Размещение
! Функция
! [[Агонист]]
! [[Антагонист]]
! Uses of drugs that act on this receptor
|-
| '''[[5-HT1A receptor|5-HT<sub>1A</sub>]]''' <br>(1987)
|
* {{Gene|HTR1A}}
|
* Blood Vessels
* CNS
|
* Addiction <ref name="pmid7862892">{{cite journal | author = 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">{{cite journal | author = 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 | author = 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>
* Aggression<ref name="pmid16310183">{{cite journal | author = 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>
* Anxiety<ref name="pmid9724773">{{cite journal | author = 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 = 195 | issue = 18 | pages = 10734–9 | year = 1998 | pmid = 9724773 | pmc = 27964 | doi=10.1073/pnas.95.18.10734}}</ref>
* Appetite<ref name="pmid17609739">{{cite journal | author = 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 = 1998 | pmid = 17609739 | doi = 10.1358/mf.2007.29.4.1075362 }}</ref>
* [[Autoreceptor]]
* Blood Pressure<ref name="pmid2842163">{{cite journal | author = Wouters W, Tulp MT, Bevan P | title = Flesinoxan lowers blood pressure and heart rate in cats via 5-HT1A receptors | journal = Eur J Pharmacol. | volume = 149 | issue = 3 | pages = 213–23 | year = 1998 | pmid = 2842163 | doi = 10.1016/0014-2999(88)90651-6 }}</ref><ref name="pmid18667366">{{cite journal | author = Horiuchi J, McDowall LM, Dampney RA | title = Role of 5-HT(1A) receptors in the lower brainstem on the cardiovascular response to dorsomedial hypothalamus activation | journal = Auton Neurosci. | volume = 142 | issue = 1–2 | pages = 71–6 | year = 2008 | pmid = 18667366 | doi = 10.1016/j.autneu.2008.06.004 }}</ref>
* Cardiovascular Function<ref name="pmid15802554">{{cite journal | author = Nalivaiko E, Ootsuka Y, Blessing WW. | title = Activation of 5-HT1A receptors in the medullary raphe reduces cardiovascular changes elicited by acute psychological and inflammatory stresses in rabbits | journal = Am J Physiol Regul Integr Comp Physiol. | volume = 289 | issue = 2 | pages = R596–R604 | year = 2005 | pmid = 15802554 | doi = 10.1152/ajpregu.00845.2004 }}</ref>
* Emesis<ref name="pmid8013549">{{cite journal | author = 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 | pmid = 8013549 | doi = 10.1016/0014-2999(94)90756-0 }}</ref>
* Heart Rate<ref name="pmid2842163"/><ref name="pmid18667366"/>
* Impulsivity<ref name="pmid15688093">{{cite journal | author = 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 = 669–682 | year = 2005 | pmid = 15688093 | doi = 10.1038/sj.npp.1300610 }}</ref>
* Memory<ref name="pmid18394726">{{cite journal | author = 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><ref name="pmid12562581">{{cite journal | author = Yasuno F, Suhara T, Nakayama T, Ichimiya T, Okubo Y, Takano A, Ando T, Inoue M, Maeda J, Suzuki K | title = Inhibitory effect of hippocampal 5-HT1A receptors on human explicit memory | journal = Am J Psychiatry | volume = 160 | issue = 2 | pages = 334–40 | year = 2003 | pmid = 12562581 | doi = 10.1176/appi.ajp.160.2.334 }}</ref>
* Mood<ref name="pmid2883013">{{cite journal | author = 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>
* Nausea<ref name="pmid8013549"/>
* Nociception<ref name="pmid12595749">{{cite journal | author = 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 = 182–194 | year = 2003 | pmid = 12595749 | doi = 10.1159/000068404 }}</ref>
* Penile Erection<ref name="pmid9085055">{{cite journal | author = 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 = 11–3 | year = 1997 | pmid = 9085055 | doi=10.1016/S0014-2999(97)00050-2}}</ref>
* Pupil Dilation<ref name="pmid8982715">{{cite journal | author = 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>
* Respiration<ref name="pmid16166206">{{cite journal | author = 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 = American Journal of Physiology. Regulatory, Integrative and Comparative Physiology | volume = 290 | issue = 2 | pages = R405–13 | year = 2006 | month = February | pmid = 16166206 | doi = 10.1152/ajpregu.00440.2005 | url = | issn = }}</ref>
* Sexual Behavior<ref name="pmid11965359">{{cite journal | author = Popova NK, Amstislavskaya TG | title = Involvement of the 5-HT(1A) and 5-HT(1B) serotonergic receptor subtypes in sexual arousal in male mice | journal = Psychoneuroendocrinology | volume = 27 | issue = 5 | pages = 609–18 | year = 2002 | pmid = 11965359 | doi = 10.1016/S0306-4530(01)00097-X }}</ref>
* Sleep<ref name="pmid10607047">{{cite journal | author = 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>
* Sociability<ref name="pmid17383105">{{cite journal | author = 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>
* Thermoregulation<ref name="pmid2951611">{{cite journal | author = Gudelsky GA, Koenig JI, Meltzer HY | title = Thermoregulatory responses to serotonin (5-HT) receptor stimulation in the rat. Evidence for opposing roles of 5-HT2 and 5-HT1A receptors | journal = Neuropharmacology | volume = 25 | issue = 12 | pages = 1307–13 | year = 1986 | pmid = 2951611 | doi = 10.1016/0028-3908(86)90101-2 }}</ref>
* Vasoconstriction<ref name="pmid16455061">{{cite journal | author = 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>
| <!--5-HT1A AGONISTs-->
'''<span style="font-size:100%;"> Selective (for 5-HT<sub>1A</sub> over other 5-HT receptors) </span>'''
* [[Cannabidiol]] (Unknown potency and efficacy)
* [[F-15,599]] (Research compound, highly potent and selective for 5-HT<sub>1A</sub>)
* [[Flesinoxan]] (Potent, EC<sub>50</sub> =24nM)
* [[Gepirone]] ([[Partial agonist]], K<sub>i</sub> = 70nM)
* [[Ipsapirone]] (Partial agonist, K<sub>i</sub>=12.1nM. Has antidepressant and anxiolytic properties)
* [[Trazodone]] ([[Serotonin antagonist and reuptake inhibitor|SARI]] Selective in the sense that on all other 5-HT receptors it acts as either an antagonist or has no action. K<sub>d</sub>=78nM)
* [[Yohimbine]] (Unselective partial agonist, moderate affinity. All other sites are antagonized. An [[Indole alkaloid]], used to treat [[sexual dysfunction]])
* [[Tandospirone]] (Potent and selective partial agonist. K<sub>i</sub> =27 ± 5 nM [[Anxiolytic]] and [[antidepressant]])

'''<span style="font-size:100%;"> Nonselective </span>'''
* [[5-Carboxamidotryptamine|5-CT]] (Potent - K<sub>i</sub> =250 ± 50pM)
* [[8-OH-DPAT]] (Potent, almost selective (some affinity for [[5-HT7 receptor|5-HT<sub>7</sub>]], [[Serotonin transporter|SERT]] and as a [[serotonin releasing agent]]))
* [[Aripiprazole]] (Atypical antipsychotic.)
* [[Buspirone]]<ref name=pharmamotion>[http://pharmacologycorner.com/serotonin-5ht-receptors-agonists-antagonist/ Pharmacology Corner > Serotonin (5-HT): receptors, agonists and antagonists] By Flavio Guzmán, M.D. on 9/08/09</ref> (Partial agonist, IA = 0.465. [[Anxiolytic]] and [[antidepressant]])<ref name=pharmamotion/>
* [[Ziprasidone]] (Atypical antipsychotic. Partial agonist - K<sub>i</sub>=3.4nM)

|<!--5-HT1A ANTAGONISTs-->
* [[BMY 7378]]
* [[Cyanopindolol]]
* [[Iodocyanopindolol]]
* [[Lecozotan]]
* [[Methiothepin]]
* [[Methysergide]] (http://www.ncbi.nlm.nih.gov/pubmed/2933009)
* [[NAN-190]]
* [[Nebivolol]]
* [[Nefazodone]] (SARI. Acts as an antagonist see http://pubchem.ncbi.nlm.nih.gov[[WAY-100,135]]
* [[WAY-100,635]]
* [[Mefway]]
|
* [[Analgesics]] (full agonists serve as analgesics by regulating the release of [[β-endorphin]])
* [[Antidepressants]] (full and partial agonists serve as antidepressants and antagonists can by blocking presynaptic autoreceptors)
* [[Anxiolytics]] (e.g. [[buspirone]] (partial agonist), [[U-92,016-A]] (full agonist), [[LY297996]] <ref name="pmid9784072">{{cite journal |author=Cao BJ, Rodgers RJ |title=Comparative effects of novel 5-HT1A receptor ligands, LY293284, LY315712 and LY297996, on plus-maze anxiety in mice |journal=Psychopharmacology |volume=139 |issue=3 |pages=185–94 |year=1998 |month=October |pmid=9784072 |doi= 10.1007/s002130050703|url=}}</ref> (antagonist))
* [[Nootropic]] (antagonists; e.g. [[Lecozotan]])
* Relieving negative symptoms of [[psychosis]]
|-
| '''[[5-HT1B receptor|5-HT<sub>1B</sub>]]''' <br>(1992)
|
* {{Gene|HTR1B}}
|
* Blood Vessels
* CNS
|
* Addiction <ref name="pmid10027505">{{cite journal | author = Harrison AA, Parsons LH, Koob GF, Markou A | title = RU 24969, a 5-HT1A/1B agonist, elevates brain stimulation reward thresholds: an effect reversed by GR 127935, a 5-HT1B/1D antagonist | journal = Psychopharmacology (Berl). | volume = 141 | issue = 3 | pages = 242–50 | year = 1999 | pmid = 10027505 | doi = 10.1007/s002130050831 }}</ref>
* Aggression<ref name="pmid16310183"/>
* Anxiety<ref name="pmid15720791">{{cite journal | author = Chojnacka-Wójcik E, Klodzinska A, Tatarczynska E | title = The anxiolytic-like effect of 5-HT1B receptor ligands in rats: a possible mechanism of action | journal = J Pharm Pharmacol. | volume = 57 | issue = 2 | pages = 253–7 | year = 2005 | pmid = 15720791 | doi = 10.1211/0022357055399 }}</ref><ref name="pmid11888549">{{cite journal | author = Lin D, Parsons LH | title = Anxiogenic-like effect of serotonin(1B) receptor stimulation in the rat elevated plus-maze | journal = Pharmacol Biochem Behav. | volume = 71 | issue = 4 | pages = 581–7 | year = 2002 | pmid = 11888549 | doi = 10.1016/S0091-3057(01)00712-2 }}</ref><ref name="pmid15577451">{{cite journal | author = Tatarczynska E, Klodzinska A, Stachowicz K, Chojnacka-Wójcik E | title = Effects of a selective 5-HT1B receptor agonist and antagonists in animal models of anxiety and depression | journal = Behav Pharmacol. | volume = 15 | issue = 8 | pages = 523–34 | year = 2004 | pmid = 15577451 | doi = 10.1097/00008877-200412000-00001 }}</ref>
* [[Autoreceptor]]
* Learning<ref name="pmid18394658">{{cite journal | author = Eriksson TM, Madjid N, Elvander-Tottie E, Stiedl O, Svenningsson P, Ogren SO | title = Blockade of 5-HT 1B receptors facilitates contextual aversive learning in mice by disinhibition of cholinergic and glutamatergic neurotransmission | journal = Neuropharmacology | volume = 54 | issue = 7 | pages = 1041–50 | year = 2008 | pmid = 18394658 | doi = 10.1016/j.neuropharm.2008.02.007 }}</ref>
* Locomotion<ref name="pmid10454466">{{cite journal | author = McCreary AC, Bankson MG, Cunningham KA | title = Pharmacological studies of the acute and chronic effects of (+)-3, 4-methylenedioxymethamphetamine on locomotor activity: role of 5-hydroxytryptamine(1A) and 5-hydroxytryptamine(1B/1D) receptors | journal = J Pharmacol Exp Ther. | volume = 290 | issue = 3 | pages = 965–73 | year = 1999 | pmid = 10454466 }}</ref>
* Memory<ref name="pmid18394658"/>
* Mood<ref name="pmid15577451"/>
* Penile Erection<ref name="pmid9085055"/>
* Sexual Behavior<ref name="pmid11965359"/>
* Vasoconstriction
|<!--5-HT1B AGONISTs-->
* [[5-Carboxamidotryptamine|5-CT]]
* [[CGS-12066A]]
* [[CP-93,129]]
* [[CP-94,253]]
* [[Dihydroergotamine]]
* [[Eltoprazine]]
* [[Ergotamine]]
* [[Methysergide]]
* [[RU 24969]]
* [[TFMPP]]
* [[Triptans]]<ref name=pharmamotion/> ([[antimigraine]]<ref name=pharmamotion/>)
** [[Zolmitriptan]]
** [[Eletriptan]]
** [[Sumatriptan]]
|<!--5-HT1B ANTAGONISTs-->
* [[Alprenolol]]
* [[AR-A000002]]
* [[Asenapine]]
* [[Cyanopindolol]]
* [[GR-127,935]]
* [[Iodocyanopindolol]]
* [[Isamoltane]]
* [[Metergoline]]
* [[Methiothepin]]
* [[Oxprenolol]]
* [[Pindolol]]
* [[Propranolol]]
* [[SB-216,641]]
* [[Yohimbine]]
|
* [[Migraines]] (e.g. [[triptans]])
|-
| '''[[5-HT1D receptor|5-HT<sub>1D</sub>]]''' <br>(1991)
|
* {{Gene|HTR1D}}
|
* Blood Vessels
* CNS
|
* Anxiety<ref name="pmid15820416">{{cite journal | author = Amital D, Fostick L, Sasson Y, Kindler S, Amital H, Zohar J | title = Anxiogenic effects of Sumatriptan in panic disorder: a double-blind, placebo-controlled study | journal = Eur Neuropsychopharmacol. | volume = 15 | issue = 3 | pages = 279–82 | year = 2005 | pmid = 15820416 | doi = 10.1016/j.euroneuro.2004.12.002 }}</ref><ref name="pmid8736648">{{cite journal | author = Feuerstein TJ, Hüring H, van Velthoven V, Lücking CH, Landwehrmeyer GB | title = 5-HT1D-like receptors inhibit the release of endogenously formed [3H]GABA in human, but not in rabbit, neocortex | journal = Neurosci Lett. | volume =209 | issue = 3 | pages = 210–4 | year = 1996 | pmid = 8736648 | doi = 10.1016/0304-3940(96)12637-9 }}</ref>
* [[Autoreceptor]]
* Locomotion<ref name="pmid10454466"/>
* Vasoconstriction
|<!--5-HT1D AGONISTs-->
* [[5-Carboxamidotryptamine|5-CT]]
* [[CP-135,807]]
* [[Dihydroergotamine]]
* [[Ergotamine]]
* [[Methysergide]]
* [[Triptans]]<ref name=pharmamotion/> ([[antimigraine]]<ref name=pharmamotion/>)
** [[Almotriptan]]
** [[Eletriptan]]
** [[Frovatriptan]]
** [[Naratriptan]]
** [[Rizatriptan]]
** [[Sumatriptan]]
** [[Zolmitriptan]]
* [[Yohimbine]]
|<!--5-HT1D ANTAGONISTs-->
* [[BRL-15572]]
* [[GR-127,935]]
* [[Ketanserin]]
* [[Metergoline]]
* [[Methiothepin]]
* [[Rauwolscine]]
* [[Ritanserin]]
* [[Ziprasidone]]
|
* [[Migraines]] (e.g. [[triptans]])
|-
| '''[[5-HT1E|5-HT<sub>1E</sub>]]''' <br>(1992)
|
* {{Gene|HTR1E}}
|
* Blood Vessels
* CNS
|
|
* [[BRL-54443]]
|
|
* None known
|-
| '''[[5-HT1F|5-HT<sub>1F</sub>]]''' <br>(1993)
|
* {{Gene|HTR1F}}
|
* CNS
|
* Migraine
|<!--5-HT1F AGONISTs-->
* [[BRL-54443]]
* [[Lasmiditan]]
* [[LY-334,370]]
* [[Naratriptan]]
|
|
* None known
|-
| '''[[5-HT2A receptor|5-HT<sub>2A</sub>]]''' <br>(1988)
|
* {{Gene|HTR2A}}
|
* Blood Vessels
* CNS
* GI Tract
* Platelets
* PNS
* Smooth Muscle
|
* Addiction (potentially modulating) <ref name="Bubar">[http://www.ncbi.nlm.nih.gov/pubmed/17017968] Bubar MJ, Cunningham KA. Serotonin 5-HT2A and 5-HT2C receptors as potential targets for modulation of psychostimulant use and dependence. Curr Top Med Chem. 2006;6(18):1971-85.</ref>
* Anxiety<ref name="pmid9539263">{{cite journal | author = Schreiber R, Melon C, De Vry J | title = The role of 5-HT receptor subtypes in the anxiolytic effects of selective serotonin reuptake inhibitors in the rat ultrasonic vocalization test | journal = Psychopharmacology (Berl). | volume = 135 | issue = 4 | pages = 383–91 | year = 1998 | pmid = 9539263 | doi = 10.1007/s002130050526 }}</ref>
* Appetite
* Cognition
* Imagination
* Learning
* Memory
* Mood
* Perception
* Sexual Behavior<ref name="pmid12097814">{{cite journal | author = Popova NK, Amstislavskaya TG | title = 5-HT2A and 5-HT2C serotonin receptors differentially modulate mouse sexual arousal and the hypothalamo-pituitary-testicular response to the presence of a female | journal = Neuroendocrinology | volume = 76 | issue = 1 | pages = 28–34 | year = 2002 | pmid = 12097814 | doi = 10.1159/000063681 }}</ref>
* Sleep<ref name="pmid16339018">{{cite journal | author = Popa D, Léna C, Fabre V, Prenat C, Gingrich J, Escourrou P, Hamon M, Adrien J | title = Contribution of 5-HT2 receptor subtypes to sleep-wakefulness and respiratory control, and functional adaptations in knock-out mice lacking 5-HT2A receptors | journal = J Neurosci. | volume = 25 | issue = 49 | pages = 11231–8 | year = 2005 | pmid = 16339018 | doi = 10.1523/JNEUROSCI.1724-05.2005 }}</ref>
* Thermoregulation<ref name="pmid9106912">{{cite journal | author = Mazzola-Pomietto P, Aulakh CS, Tolliver T, Murphy DL | title = Functional subsensitivity of 5-HT2A and 5-HT2C receptors mediating hyperthermia following acute and chronic treatment with 5-HT2A/2C receptor antagonists| journal = Psychopharmacology (Berl). | volume = 130 | issue = 2 | pages = 144–51 | year = 1997 | pmid = 9106912 | doi = 10.1007/s002130050222 }}</ref>
* Vasoconstriction<ref name="pmid12654345">{{cite journal | author = Blessing WW, Seaman B. | title = 5-hydroxytryptamine(2A) receptors regulate sympathetic nerves constricting the cutaneous vascular bed in rabbits and rats | journal = Neuroscience. | volume = 117 | issue = 4 | pages = 939–948 | year = 2003 | pmid = 12654345 | doi = 10.1016/S0306-4522(02)00810-2 }}</ref>
|<!--5-HT2A AGONISTs-->
* [[25I-NBOMe]] (Full agonist)
* [[2C-B]]
* [[5-MeO-DMT]]
* [[Benzylpiperazine|BZP]]
* [[Bufotenin]]
* [[Dimethyltryptamine|DMT]]
* [[2,5-Dimethoxy-4-methylamphetamine|DOM]]
* [[Ergonovine]]
* [[Lisuride]]
* [[LSD]]
* [[Mescaline]]
* [[Myristicin]]
* [[Psilocin]]
* [[Psilocybin]]
* [[TFMPP]] (partial agonist or antagonist)
* [[Yohimbine]]
|<!--5-HT2A ANTAGONISTs-->
* [[Atypical antipsychotic]]s
** [[Clozapine]]<ref name=pharmamotion/>
** [[Olanzapine]]
** [[Quetiapine]]
** [[Risperidone]]
** [[Ziprasidone]]
* [[Aripiprazole]]
* [[Asenapine]]
* [[Amitriptyline]]
* [[Clomipramine]]
* [[Cyproheptadine]]
* [[Eplivanserin]]
* [[Etoperidone]]
* [[Iloperidone]]
* [[Ketanserin]]<ref name=pharmamotion/> ([[antihypertensive]]<ref name=pharmamotion/>)
* [[Methysergide]]
* [[Mianserin]]
* [[Mirtazapine]]
* [[Nefazodone]]
* [[Pimavanserin]]
* [[Pizotifen]]
* [[Ritanserin]]
* [[Trazodone]]
|
* [[Atypical antipsychotic]]s (antagonist)
* [[Psychedelics]] (partial agonists)
* [[NaSSA]]s (antidepressants and anxiolytics)
|-
| '''[[5-HT2B receptor|5-HT<sub>2B</sub>]]''' <br>(1992)
|
* {{Gene|HTR2B}}
|
* Blood Vessels
* CNS
* GI Tract
* Platelets
* PNS
* Smooth Muscle
|
* Anxiety<ref name="pmid8730737">{{cite journal | author = Kennett GA, Bright F, Trail B, Baxter GS, Blackburn TP | title = Effects of the 5-HT2B receptor agonist, BW 723C86, on three rat models of anxiety | journal = Br J Pharmacol. | volume = 117 | issue = 7 | pages = 1443–8 | year = 1996 | pmid = 8730737 | pmc = 1909458 }}</ref><ref name="pmid9225285">{{cite journal | author = Duxon MS, Kennett GA, Lightowler S, Blackburn TP, Fone KC | title = Activation of 5-HT2B receptors in the medial amygdala causes anxiolysis in the social interaction test in the rat | journal = Neuropharmacology | volume = 36 | issue = 4–5 | pages = 601–8 | year = 1997 | pmid = 9225285 | doi = 10.1016/S0028-3908(97)00042-7 }}</ref><ref name="pmid9886683">{{cite journal | author = Kennett GA, Trail B, Bright F | title = Anxiolytic-like actions of BW 723C86 in the rat Vogel conflict test are 5-HT2B receptor mediated | journal = Neuropharmacology | volume = 37 | issue = 12 | pages = 1603–10 | year = 1998 | pmid = 9886683 | doi = 10.1016/S0028-3908(98)00115-4 }}</ref>
* Appetite<ref name="pmid9144661">{{cite journal | author = Kennett GA, Ainsworth K, Trail B, Blackburn TP | title = BW 723C86, a 5-HT2B receptor agonist, causes hyperphagia and reduced grooming in rats | journal = Neuropharmacology | volume = 36 | issue = 2 | pages = 233–9 | year = 1997 | pmid = 9144661 | doi = 10.1016/S0028-3908(96)00171-2 }}</ref>
* Cardiovascular Function
* GI Motility<ref name="pmid11877320">{{cite journal | author = Borman RA, Tilford NS, Harmer DW, Day N, Ellis ES, Sheldrick RL, Carey J, Coleman RA, Baxter GS. | title = 5-HT(2B) receptors play a key role in mediating the excitatory effects of 5-HT in human colon in vitro | journal = Br J Pharmacol. | volume = 135 | issue = 5 | pages = 1144–1151 | year = 2002 | pmid = 11877320 | doi = 10.1038/sj.bjp.0704571 | pmc = 1573235 }}</ref>
* Sleep<ref name="pmid16339018"/>
* Vasoconstriction
|<!--5-HT2B AGONISTs-->
* [[BW-723C86]]
* [[Fenfluramine]]
* [[MDMA]]
* [[Norfenfluramine]]
* [[Ro60-0175]]
|<!--5-HT2B ANTAGONISTs-->
* [[Agomelatine]]
* [[Asenapine]]
* [[Benzylpiperazine|BZP]]
* [[Ketanserin]]
* [[Methysergide]]
* [[Ritanserin]]
* [[RS-127,445]]
* [[Tegaserod]]
* [[Yohimbine]]
|
* [[Migraines]] (antagonists)
|-
| '''[[5-HT2C receptor|5-HT<sub>2C</sub>]]''' <br>(1988)
|
* {{Gene|HTR2C}}
|
* Blood Vessels
* CNS
* GI Tract
* Platelets
* PNS
* Smooth Muscle
|
*Addiction. (potentially modulating)<ref name="Bubar"/>
* Anxiety<ref name="pmid9225286">{{cite journal | author = Kennett GA, Wood MD, Bright F, Trail B, Riley G, Holland V, Avenell KY, Stean T, Upton N, Bromidge S, Forbes IT, Brown AM, Middlemiss DN, Blackburn TP | title = SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist | journal = Neuropharmacology. | volume = 36 | issue = 4–5 | pages = 609–20 | year = 1997 | pmid = 9225286 | doi = 10.1016/S0028-3908(97)00038-5 }}</ref><ref name="pmid15289999">{{cite journal | author = Millan MJ, Brocco M, Gobert A, Dekeyne A | title = Anxiolytic properties of agomelatine, an antidepressant with melatoninergic and serotonergic properties: role of 5-HT2C receptor blockade | journal = Psychopharmacology (Berl). | volume = 177 | issue = 4 | pages = 448–58 | year = 2005 | pmid = 15289999 | doi = 10.1007/s00213-004-1962-z }}</ref><ref name="pmid18523738">{{cite journal | author = Millan MJ, Brocco M, Gobert A, Dekeyne A | title = S32006, a novel 5-HT2C receptor antagonist displaying broad-based antidepressant and anxiolytic properties in rodent models | journal = Psychopharmacology (Berl). | volume = 199 | issue = 4 | pages = 549–68 | year = 2008 | pmid = 18523738 | doi = 10.1007/s00213-008-1177-9 }}</ref>
* Appetite
* GI Motility<ref name="pmid19058784">{{cite journal | author = Fujitsuka N, Asakawa A, Hayashi M, Sameshima M, Amitani H, Kojima S, Fujimiya M, Inui A. | title = Selective serotonin reuptake inhibitors modify physiological gastrointestinal motor activities via 5-HT2c receptor and acyl ghrelin | journal = Biol Psychiatry. | volume = 65 | issue = 9 | pages = 748–759 | year = 2009 | pmid = 19058784 | doi = 10.1016/j.biopsych.2008.10.031 }}</ref>
* [[Heteroreceptor]] for [[norepinephrine]] and [[dopamine]]
* Locomotion
* Mood<ref name="pmid15289999"/><ref name="pmid18523738"/>
* Penile Erection<ref name="pmid9151932">{{cite journal | author = Millan MJ, Peglion JL, Lavielle G, Perrin-Monneyron S | title = 5-HT2C receptors mediate penile erections in rats: actions of novel and selective agonists and antagonists | journal = Eur J Pharmacol. | volume = 325 | issue = 1 | pages = 9–12 | year = 1997 | pmid = 9151932 | doi = 10.1016/S0014-2999(97)89962-1 }}</ref><ref name="pmid8001637">{{cite journal | author = Stancampiano R, Melis MR, Argiolas A | title = Penile erection and yawning induced by 5-HT1C receptor agonists in male rats: relationship with dopaminergic and oxytocinergic transmission | journal = Eur J Pharmacol. | volume = 261 | issue = 1–2 | pages = 149–55 | year = 1994 | pmid = 8001637 | doi = 10.1016/0014-2999(94)90313-1 }}</ref>
* Sexual Behavior<ref name="pmid12097814"/>
* Sleep<ref name="pmid12431861">{{cite journal | author = Frank MG, Stryker MP, Tecott LH | title = Sleep and sleep homeostasis in mice lacking the 5-HT2c receptor | journal = Neuropsychopharmacology | volume = 27 | issue = 5 | pages = 869–73 | year = 2002 | pmid = 12431861 | doi = 10.1016/S0893-133X(02)00353-6 | pmc = 2452994 }}</ref>
* Thermoregulation<ref name="pmid9106912"/>
* Vasoconstriction
|<!--5-HT2C AGONISTs-->
* [[A-372,159]]
* [[AL-38022A]]
* [[Aripiprazole]]
* [[Ergonovine]]
* [[Lorcaserin]]
* [[Ro60-0175]]
* [[TFMPP]]
* [[Trazodone]]<ref name=pharmamotion/> ([[hypnotic]]<ref name=pharmamotion/>)
* [[YM-348]]
|<!--5-HT2C ANTAGONISTs-->
* [[Agomelatine]]<ref name=pharmamotion/> ([[antidepressant]]<ref name=pharmamotion/>)
* [[Amitriptyline]]
* [[Asenapine]]
* [[Clomipramine]]
* [[Clozapine]]<ref name=pharmamotion/> ([[antipsychotic]]<ref name=pharmamotion/>)
* [[Cyproheptadine]]
* [[Dimebolin]]
* [[Eltoprazine]]
* [[Etoperidone]]
* [[Fluoxetine]]
* [[Iloperidone]]
* [[Ketanserin]]<ref name=pharmamotion/> ([[antihypertensive]]<ref name=pharmamotion/>)
* [[Lisuride]]
* [[Methysergide]]<ref name=Rang187>{{cite book |author=Rang, H. P. |title=Pharmacology |publisher=Churchill Livingstone |location=Edinburgh |year=2003 |pages= |isbn=0-443-07145-4 |oclc= |doi=}} Page 187</ref>
* [[Mianserin]]
* [[Mirtazapine]]
* [[Nefazodone]]
* [[Olanzapine]]
* [[Paroxetine]]
* [[Quetiapine]]
* [[Risperidone]]
* [[Ritanserin]]
* [[Tramadol]]
* [[Trazodone]]
* [[Ziprasidone]]
|
* [[Antidepressant]] (e.g. [[agomelatine]], [[fluoxetine]])
|-
| '''[[5-HT3 receptor|5-HT<sub>3</sub>]]''' <br>(1993)
|
* {{Gene|HTR3A}}
* {{Gene|HTR3B}}
* {{Gene|HTR3C}}
* {{Gene|HTR3D}}
* {{Gene|HTR3E}}
|
* CNS
* GI Tract
* PNS
|
* Addiction
* Anxiety
* Emesis
* GI Motility
* Learning<ref name="pmid8115433">{{cite journal | author = Pitsikas N, Brambilla A, Borsini F. | title = Effect of DAU 6215, a novel 5-HT3 receptor antagonist, on scopolamine-induced amnesia in the rat in a spatial learning task | journal = Pharmacol Biochem Behav. | volume = 47 | issue = 1 | pages = 95–99 | year = 1994 | pmid = 8115433 | doi = 10.1016/0091-3057(94)90116-3 }}</ref>
* Memory<ref name="pmid8115433"/>
* Nausea
|<!--5-HT3 AGONISTs-->
* [[2-methyl-5-hydroxytryptamine|2-Methyl-5-HT]]
* [[Benzylpiperazine|BZP]]
* [[Quipazine]]
* [[RS-56812]]
|<!--5-HT3 ANTAGONISTs-->
* [[Alosetron]]
* Several [[antiemetics]]<ref name=pharmamotion/>
** [[Dolasetron]]
** [[Ondansetron]]<ref name=pharmamotion/>
** [[Granisetron]]
** [[Tropisetron]]
* [[Clozapine]]
* [[Memantine]]
* [[Metoclopramide]]
* [[Mianserin]]
* [[Mirtazapine]]
* [[Olanzapine]]
* [[Quetiapine]]
|
* [[Antiemetic]]
|-
| '''[[5-HT4 receptor|5-HT<sub>4</sub>]]''' <br>(1995)
|
* {{Gene|HTR4}}
|
* CNS
* GI Tract
* PNS
|
* Anxiety<ref name="pmid14676321">{{cite journal | author = Smriga M, Torii K | title = L-Lysine acts like a partial serotonin receptor 4 antagonist and inhibits serotonin-mediated intestinal pathologies and anxiety in rats | journal = Proc Natl Acad Sci U S A. | volume = 100 | issue = 26 | pages = 15370–5 | year = 2003 | pmid = 14676321 | doi = 10.1073/pnas.2436556100 | pmc = 307574 }}</ref><ref name="pmid9225297">{{cite journal | author = Kennett GA, Bright F, Trail B, Blackburn TP, Sanger GJ | title = Anxiolytic-like actions of the selective 5-HT4 receptor antagonists SB 204070A and SB 207266A in rats | journal = Neuropharmacology | volume = 36 | issue = 4–5 | pages = 707–12 | year = 1997 | pmid = 9225297 | doi = 10.1016/S0028-3908(97)00037-3 }}</ref>
* Appetite<ref name="pmid17913892">{{cite journal | author = Jean A, Conductier G, Manrique C, Bouras C, Berta P, Hen R, Charnay Y, Bockaert J, Compan V | title = Anorexia induced by activation of serotonin 5-HT4 receptors is mediated by increases in CART in the nucleus accumbens | journal = Proc Natl Acad Sci U S A. | volume = 104 | issue = 41 | pages = 16335–40 | year = 2007 | pmid = 17913892 | doi = 10.1073/pnas.0701471104 | pmc = 2042207 }}</ref><ref name="pmid15146954">{{cite journal | author = J Soc Biol. | title = Compan V, Charnay Y, Dusticier N, Daszuta A, Hen R, Bockaert J | journal = J Soc Biol. | volume = 198 | issue = 1 | pages = 37–49 | year = 2004 | pmid = 15146954 | last2 = Charnay | first2 = Y | last3 = Dusticier | first3 = N | last4 = Daszuta | first4 = A | last5 = Hen | first5 = R | last6 = Bockaert | first6 = J }}</ref>
* GI Motility
* Learning<ref name="Meneses A, Hong E 1997 347–51">{{cite journal |author=Meneses A, Hong E |title=Effects of 5-HT4 receptor agonists and antagonists in learning |journal=Pharmacol Biochem Behav |volume=56 |issue=3 |pages=347–51 |year=1997 |pmid=9077568 |doi=10.1016/S0091-3057(96)00224-9}}</ref><ref name="pmid9225295">{{cite journal | author = Fontana DJ, Daniels SE, Wong EH, Clark RD, Eglen RM | title = The effects of novel, selective 5-hydroxytryptamine (5-HT)4 receptor ligands in rat spatial navigation | journal = Neuropharmacology | volume = 36 | issue = 4–5 | pages = 689–96 | year = 1997 | pmid = 9225295 | doi = 10.1016/S0028-3908(97)00055-5 }}</ref>
* Memory<ref name="Meneses A, Hong E 1997 347–51"/><ref name="pmid9225295"/><ref name="pmid9732367">{{cite journal | author = Fontana DJ, Daniels SE, Wong EH, Clark RD, Eglen RM | title = Role of 5-HT4 receptors in the mouse passive avoidance test | journal = J Pharmacol Exp Ther. | volume = 286 | issue = 3 | pages = 1115–21 | year = 1998 | pmid = 9732367 }}</ref>
* Mood<ref name="pmid17785179">{{cite journal | author = Lucas G, Rymar VV, Du J, Mnie-Filali O, Bisgaard C, Manta S, Lambas-Senas L, Wiborg O, Haddjeri N, Piñeyro G, Sadikot AF, Debonnel G | title = Serotonin(4) (5-HT(4)) receptor agonists are putative antidepressants with a rapid onset of action | journal = Neuron | volume = 55 | issue = 5 | pages = 679–81 | year = 2007 | pmid = 17785179 | doi = 10.1016/j.neuron.2007.07.041 }}</ref><ref name="pmid17785173">{{cite journal | author = Duman RS | title = A silver bullet for the treatment of depression? | journal = Neuron | volume = 55 | issue = 5 | pages = 712–25 | year = 2007 | pmid = 17785173 | doi = 10.1016/j.neuron.2007.08.011 | last2 = Rymar | first2 = VV | last3 = Du | first3 = J | last4 = Mnie-Filali | first4 = O | last5 = Bisgaard | first5 = C | last6 = Manta | first6 = S | last7 = Lambas-Senas | first7 = L | last8 = Wiborg | first8 = O | last9 = Haddjeri | first9 = N }}</ref>
* Respiration<ref name="pmid16166206"/><ref>{{cite journal |author=Manzke T, Guenther U, Ponimaskin E, Haller M, Dutschmann M, Schwarzacher S, Richter D |title=5-HT4(a) receptors avert opioid-induced breathing depression without loss of analgesia |journal=Science |volume=301 |issue=5630 |pages=226–9 |year=2003 |pmid=12855812 |doi=10.1126/science.1084674}}</ref>
|<!--5-HT4 AGONISTs-->
* [[5-Methoxytryptamine|5-MT]]
* [[BIMU-8]]
* [[Cinitapride]]
* [[Cisapride]]<ref name=pharmamotion/> ([[prokinetic agent|gastroprokinetic]])
* [[Dazopride]]
* [[Metoclopramide]]
* [[Mosapride]]
* [[Prucalopride]]
* [[RS-67333]]
* [[Renzapride]]
* [[Tegaserod]]
* [[Zacopride]]
|<!--5-HT4 ANTAGONISTs-->
* [[L-Lysine]]<ref name="pmid14676321"/>
* [[Piboserod]]
|
* None known
|-
| '''[[5-HT5A receptor|5-HT<sub>5A</sub>]]''' <br>(1994)
|
* {{Gene|HTR5A}}
|
* CNS
|
* [[Autoreceptor]]
* Locomotion<ref name="pmid14965244">{{cite journal | author = Nelson DL | title = 5-HT5 receptors | journal = Curr Drug Targets CNS Neurol Disord. | volume =3 | issue = 1 | pages = 53–8 | year = 2004 | pmid = 14965244 | doi = 10.2174/1568007043482606 }}</ref>
* Sleep<ref name="pmid15921820">{{cite journal | author = Dietz BM, Mahady GB, Pauli GF, Farnsworth NR | title = Valerian extract and valerenic acid are partial agonists of the 5-HT5a receptor in vitro | journal = Brain Res Mol Brain Res. | volume = 138 | issue = 2 | pages = 191–7 | year = 2005 | pmid = 15921820 | doi = 10.1016/j.molbrainres.2005.04.009 }}</ref>
|<!--5-HT5A AGONISTs-->
* [[5-Carboxamidotryptamine|5-CT]]
* [[Ergotamine]]
* [[Valerenic acid|Valerenic Acid]]<ref name="pmid15921820"/>
|<!--5-HT5A ANTAGONISTs-->
* [[Asenapine]]
* [[Dimebolin]]
* [[Methiothepin]]
* [[Ritanserin]]
* [[SB-699,551]]
* [[SB-699,551-A]]
|
* None thus far
|-
| '''[[5-HT5B receptor|5-HT<sub>5B</sub>]]''' <br>(1993)
|
* {{Gene|HTR5BP}}
|
<small>functions in rodents,<br>[[pseudogene]] in humans</small>
|
|
|
|
* None thus far
|-
| '''[[5-HT6 receptor|5-HT<sub>6</sub>]]''' <br>(1993)
|
* {{Gene|HTR6}}
|
* CNS
|
* Anxiety<ref name="pmid18096153">{{cite journal | author = Wesolowska A | title = The anxiolytic-like effect of the selective 5-HT6 receptor antagonist SB-399885: the impact of benzodiazepine receptors | journal = European Journal of Pharmacology | volume = 580 | issue = 3 | pages = 355–60 | year = 2008 | month = February | pmid = 18096153 | doi = 10.1016/j.ejphar.2007.11.022 | url = | issn = }}</ref><ref name="pmid17320917">{{cite journal | author = Wesolowska A, Nikiforuk A | title = Effects of the brain-penetrant and selective 5-HT6 receptor antagonist SB-399885 in animal models of anxiety and depression | journal = Neuropharmacology | volume = 52 | issue = 5 | pages = 1274–83 | year = 2007 | month = April | pmid = 17320917 | doi = 10.1016/j.neuropharm.2007.01.007 | url = | issn = }}</ref>
* Cognition<ref name="pmid17069795">{{cite journal | author = Hirst WD, Stean TO, Rogers DC, Sunter D, Pugh P, Moss SF, Bromidge SM, Riley G, Smith DR, Bartlett S, Heidbreder CA, Atkins AR, Lacroix LP, Dawson LA, Foley AG, Regan CM, Upton N | title = SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models | journal = European Journal of Pharmacology | volume = 553 | issue = 1–3 | pages = 109–19 | year = 2006 | month = December | pmid = 17069795 | doi = 10.1016/j.ejphar.2006.09.049 | url = | issn = }}</ref>
* Learning<ref name="pmid15964617">{{cite journal | author = Perez-García G, Meneses A | title = Oral administration of the 5-HT6 receptor antagonists SB-357134 and SB-399885 improves memory formation in an autoshaping learning task | journal = Pharmacology, Biochemistry, and Behavior | volume = 81 | issue = 3 | pages = 673–82 | year = 2005 | month = July | pmid = 15964617 | doi = 10.1016/j.pbb.2005.05.005 | url = | issn = }}</ref>
* Memory<ref name="pmid15964617"/>
* Mood<ref name="pmid17320917"/><ref name="pmid18234190">{{cite journal | author = Wesolowska A, Nikiforuk A | title = The selective 5-HT(6) receptor antagonist SB-399885 enhances anti-immobility action of antidepressants in rats | journal = European Journal of Pharmacology | volume = 582 | issue = 1–3 | pages = 88–93 | year = 2008 | month = March | pmid = 18234190 | doi = 10.1016/j.ejphar.2007.12.013 | url = | issn = }}</ref>
|<!--5-HT6 AGONISTs-->
* [[EMD-386,088]]
* [[2-Ethyl-5-methoxy-N,N-dimethyltryptamine|EMDT]]
|<!--5-HT6 ANTAGONISTs-->
* [[Amitriptyline]]
* [[Aripiprazole]]
* [[Asenapine]]
* [[Clomipramine]]
* [[Clozapine]]
* [[Dimebolin]]
* [[EGIS-12233]]
* [[Iloperidone]]
* [[MS-245]]
* [[Olanzapine]]
* [[Ro04-6790]]
* [[SB-258,585]]
* [[SB-271,046]]<ref name="titleTarget Schizophrenia - Possible future developments">{{cite web | url = http://www.abpi.org.uk/publications/publication_details/targetSchizophrenia-2003/section5.asp | title = Target Schizophrenia - Possible future developments | accessdate = 2008-04-11 | author = | authorlink = | coauthors = | date = | format = | work = | publisher = The Association of the British Pharmaceutical Industry | pages = | language = |archiveurl = http://web.archive.org/web/20080612135635/http://www.abpi.org.uk/publications/publication_details/targetSchizophrenia-2003/section5.asp <!-- Bot retrieved archive --> |archivedate = 2008-06-12 | quote = }}</ref>
* [[SB-357,134]]
* [[SB-399,885]]
|
* None thus far
|-
| '''[[5-HT7 receptor|5-HT<sub>7</sub>]]''' <br>(1993)
|
* {{Gene|HTR7}}
|
* Blood Vessels
* CNS
* GI Tract
|
* Anxiety<ref name="pmid16018977">{{cite journal | author = Hedlund PB, Huitron-Resendiz S, Henriksen SJ, Sutcliffe JG | title = 5-HT7 receptor inhibition and inactivation induce antidepressantlike behavior and sleep pattern | journal = Biological Psychiatry | volume = 58 | issue = 10 | pages = 831–7 | year = 2005 | month = November | pmid = 16018977 | doi = 10.1016/j.biopsych.2005.05.012 | url = | issn = }}</ref><ref name="pmid16828124">{{cite journal | author = Wesolowska A, Nikiforuk A, Stachowicz K, Tatarczynska E | title = Effect of the selective 5-HT7 receptor antagonist SB 269970 in animal models of anxiety and depression | journal = Neuropharmacology | volume = 51 | issue = 3 | pages = 578–86 | year = 2006 | month = September | pmid = 16828124 | doi = 10.1016/j.neuropharm.2006.04.017 | url = | issn = }}</ref>
* [[Autoreceptor]]
* Memory<ref name="pmid18308404">{{cite journal | author = Gasbarri A, Cifariello A, Pompili A, Meneses A | title = Effect of 5-HT(7) antagonist SB-269970 in the modulation of working and reference memory in the rat | journal = Behavioural Brain Research | volume = 195 | issue = 1 | pages = 164–70 | year = 2008 | month = December | pmid = 18308404 | doi = 10.1016/j.bbr.2007.12.020 | url = | issn = }}</ref><ref name="pmid18570192">{{cite journal | author = Liy-Salmeron G, Meneses A | title = Effects of 5-HT drugs in prefrontal cortex during memory formation and the ketamine amnesia-model | journal = Hippocampus | volume = 18 | issue = 9 | pages = 965–74 | year = 2008 | pmid = 18570192 | doi = 10.1002/hipo.20459 | url = | issn = }}</ref>
* Mood<ref name="pmid16018977"/><ref name="pmid16828124"/>
* Respiration<ref name="pmid16166206">{{cite journal | author = 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 = 405–13 | year = 2006 | pmid = 16166206 | doi = 10.1152/ajpregu.00440.2005 }}</ref><ref name="pmid17314195">{{cite journal | author = Bonaventure P, Kelly L, Aluisio L, Shelton J, Lord B, Galici R, Miller K, Atack J, Lovenberg TW, Dugovic C | title = Selective blockade of 5-hydroxytryptamine (5-HT)7 receptors enhances 5-HT transmission, antidepressant-like behavior, and rapid eye movement sleep suppression induced by citalopram in rodents | journal = J Pharmacol Exp Ther. | volume = 321 | issue = 2 | pages = 690–8 | year = 2007 | pmid = 17314195 | doi = 10.1124/jpet.107.119404 }}</ref>
* Sleep<ref name="pmid16018977"/><ref name="pmid17314195"/><ref name="pmid12812993">{{cite journal | author = 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 | title = SB-656104-A, a novel selective 5-HT7 receptor antagonist, modulates REM sleep in rats | journal = Br J Pharmacol. | volume = 139 | issue = 4 | pages = 705–14 | year = 2003 | pmid = 12812993 | doi = 10.1038/sj.bjp.0705290 | pmc = 1573887 }}</ref>
* Thermoregulation
* Vasoconstriction
|<!--5-HT7 AGONISTs-->
* [[5-Carboxamidotryptamine|5-CT]]
* [[8-OH-DPAT]]
* [[AS-19 (drug)|AS-19]]
* [[E-55888]]
* [[1-(2-Diphenyl)piperazine|RA-7]]
|<!--5-HT7 ANTAGONISTs-->
* [[Amitriptyline]]
* [[Aripiprazole]]
* [[Asenapine]]
* [[Clomipramine]]
* [[Clozapine]]
* [[EGIS-12233]]
* [[Iloperidone]]
* [[Imipramine]]
* [[Ketanserin]]
* [[Mirtazapine]]
* [[Olanzapine]]
* [[Ritanserin]]
* [[Risperidone]]
* [[SB-269,970]]
|
* [[Antidepressant]]
|}


== См. также ==
== См. также ==

Версия от 16:15, 16 марта 2013

Серотонин.

Серотониновые рецепторы (5-HT рецепторы) — мембранные рецепторы 5-гидрокситриптамина (5-HT), нейромедиатора и гормона, известного под названием серотонин, взаимодействующие также с множеством медицинских препаратов и психоактивных веществ. Активация рецепторов запускает внутриклеточные процессы, влияющие на активность других медиаторных систем — глутаматной, дофаминовой и ГАМК.

Классификация

Впервые неоднородность серотониновых рецепторов была показана в опытах Gaddum, Picarell (1957): способность серотонина сокращать гладкие мышцы блокировалась диэтиламидом Д-лизергиновой кислоты (ЛСД), а свойство возбуждать вегетативные ганглии предотвращалось морфином. Соответствующие рецепторы были названы Д- и М- серотониновыми рецепторами. И. Н. Пидевич (1962, 1965) показала, что рефлекторные реакции на серотонин, возникающие с серотониновых рецепторов чувствительных волокон блуждающего нерва, не угнетаются ЛСД и морфином, но конкурентно блокируются типиндолом. Соответствующие рецепторы были названы рецепторами серотонина Т типа. Позднее места связывания серотонина стали изучать с помощью меченых лигандов, удалось клонировать рецепторы. С использованием новых возможностей были выделены семь семейств рецепторов серотонина: 5-НТ1, 5-НТ2 (Leysen и соавторами,1979, 1981), 5-НТ3, 5-НТ4, 5-НТ5, 5-НТ6 и 5-НТ7. Некоторые из этих семейств рецепторов имеют подтипы. По мере накопления данных, касающихся роли и фармакологической характеристики рецепторов 5-НТ1-7, появились основания предполагать, что рецепторы 5-НТ2 близки или идентичны Д-рецепторам серотонина; рецепторы 5-НТ3 соответствуют рецепторам серотонина Т-типа; рецепторы 5-НТ4 сходны с М-серотониновыми рецепторами. Однако, вопрос о соотношении серотониновых рецепторов Д-, М- и Т-типа с семействами 5-НТ1-7 нуждается в дальнейшем исследовании. Рецепторы серотонина метаботропны, состоят из семи доменов и связаны с G-белками, за исключением ионотропного семейства 5-HT3.

Семейство Тип Механизм действия
5-HT1 Gi/Go-связанные снижение клеточного уровня cAMP
5-HT2 Gq/G11-связанные повышение клеточного уровня инозитол трифосфата (IP3) и Диацилглицерина (DAG)
5-HT3 лиганд-открываемые Na+ and K+ катионный каналы деполяризация мембраны
5-HT4 Gs-связанные повышение клеточного уровня cAMP
5-HT5A G-белок-связанные; основная связь показана с Gi/o ингибирование активности аденилатциклазы.[1]
5-HT6 Gs-связанные повышение клеточных уровней cAMP
5-HT7 Gs-связанные повышение клеточных уровней cAMP

Подтипы

Subtypes

Within these general classes of serotonin receptors, a number of specific types have been characterized:[2][3][4]

Обзор серотониновых рецепторов

Рецептор
(впервые клонирован) 		Ген Размещение Функция Агонист Антагонист Uses of drugs that act on this receptor
5-HT1A
(1987)
  • Blood Vessels
  • CNS

Selective (for 5-HT1A over other 5-HT receptors)

Nonselective

5-HT1B
(1992)
  • Blood Vessels
  • CNS
5-HT1D
(1991)
  • Blood Vessels
  • CNS
5-HT1E
(1992)
  • Blood Vessels
  • CNS
  • None known
5-HT1F
(1993)
  • CNS
  • Migraine
  • None known
5-HT2A
(1988)
  • Blood Vessels
  • CNS
  • GI Tract
  • Platelets
  • PNS
  • Smooth Muscle
  • Addiction (potentially modulating) [38]
  • Anxiety[39]
  • Appetite
  • Cognition
  • Imagination
  • Learning
  • Memory
  • Mood
  • Perception
  • Sexual Behavior[40]
  • Sleep[41]
  • Thermoregulation[42]
  • Vasoconstriction[43]
5-HT2B
(1992)
  • Blood Vessels
  • CNS
  • GI Tract
  • Platelets
  • PNS
  • Smooth Muscle
5-HT2C
(1988)
  • Blood Vessels
  • CNS
  • GI Tract
  • Platelets
  • PNS
  • Smooth Muscle
5-HT3
(1993)
  • CNS
  • GI Tract
  • PNS
  • Addiction
  • Anxiety
  • Emesis
  • GI Motility
  • Learning[57]
  • Memory[57]
  • Nausea
5-HT4
(1995)
  • CNS
  • GI Tract
  • PNS
  • None known
5-HT5A
(1994)
  • CNS
  • None thus far
5-HT5B
(1993)

functions in rodents,
pseudogene in humans

  • None thus far
5-HT6
(1993)
  • CNS
  • None thus far
5-HT7
(1993)
  • Blood Vessels
  • CNS
  • GI Tract

См. также

Ссылки

Примечания

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