Editing 5-HT receptor (section)

==Classification== 
5-hydroxytryptamine receptors or 5-HT receptors, or serotonin receptors are found in the [[Central nervous system|central]] and [[peripheral nervous system]]s.<ref name="pmid7938165"/><ref name="isbn0-397-51820-X"/> 
They can be divided into 7 families of [[G protein-coupled receptor]]s which activate an [[intracellular]] [[second messenger]] cascade to produce an excitatory or inhibitory response. The exception to this is the [[5-HT3 receptor|5-HT<sub>3</sub> receptor]] which is a [[ligand-gated ion channel]].  
In 2014, a novel 5-HT receptor was isolated from the small white butterfly, [[Pieris rapae]], and named pr5-HT<sub>8</sub>. It does not occur in mammals and shares relatively low similarity to the known 5-HT receptor classes.<ref name="pmid25187179">{{cite journal | vauthors = Qi YX, Xia RY, Wu YS, Stanley D, Huang J, Ye GY | title = Larvae of the small white butterfly, Pieris rapae, express a novel serotonin receptor | journal = Journal of Neurochemistry | volume = 131 | issue = 6 | pages = 767–777 | date = December 2014 | pmid = 25187179 | doi = 10.1111/jnc.12940 | s2cid = 21621635 }}</ref>

===Families===

{| class="wikitable"
! Family !! Type !! Mechanism !! Potential
 |-
 | '''[[5-HT1|5-HT<sub>1</sub>]]''' || [[Gi alpha subunit|G<sub>i</sub>/G<sub>o</sub>]]-protein coupled. || Decreasing cellular levels of [[cyclic adenosine monophosphate|cAMP]]. || Inhibitory
 |-
 | '''[[5-HT2|5-HT<sub>2</sub>]]''' || [[Gq protein|G<sub>q</sub>/G<sub>11</sub>]]-protein coupled. || Increasing cellular levels of [[inositol trisphosphate|IP<sub>3</sub>]] and [[diglyceride|DAG]]. || Excitatory
 |-
 | '''[[5-HT3|5-HT<sub>3</sub>]]''' || Ligand-gated [[sodium|Na<sup>+</sup>]] and [[potassium|K<sup>+</sup>]] [[cation channel]]. || [[depolarization|Depolarizing]] [[plasma membrane]]. || Excitatory
 |-
 | '''[[5-HT4|5-HT<sub>4</sub>]]''' || [[G(s)alpha|G<sub>s</sub>]]-protein coupled. || Increasing cellular levels of [[cyclic adenosine monophosphate|cAMP]]. || Excitatory
 |-
 | '''[[5-HT5A|5-HT<sub>5</sub>]]''' || [[Gi alpha subunit|G<sub>i</sub>/G<sub>o</sub>]]-protein coupled.<ref name="pmid9865521">{{cite journal | vauthors = Francken BJ, Jurzak M, Vanhauwe JF, Luyten WH, Leysen JE | title = The human 5-ht5A receptor couples to Gi/Go proteins and inhibits adenylate cyclase in HEK 293 cells | journal = European Journal of Pharmacology | volume = 361 | issue = 2–3 | pages = 299–309 | date = November 1998 | pmid = 9865521 | doi = 10.1016/S0014-2999(98)00744-4 }}</ref> || Decreasing cellular levels of [[cyclic adenosine monophosphate|cAMP]]. || Inhibitory
 |-
 | '''[[5-HT6|5-HT<sub>6</sub>]]''' || [[G(s)alpha|G<sub>s</sub>]]-protein coupled. || Increasing cellular levels of [[cyclic adenosine monophosphate|cAMP]]. || Excitatory
 |-
 | '''[[5-HT7|5-HT<sub>7</sub>]]''' || [[G(s)alpha|G<sub>s</sub>]]-protein coupled. || Increasing cellular levels of [[cyclic adenosine monophosphate|cAMP]]. || Excitatory
 |-
|}

===Subtypes===

The 7&nbsp;general serotonin receptor classes include a total of 14 known serotonin receptors.<ref name="NHM-14 receptors">{{cite book |vauthors=Malenka RC, Nestler EJ, Hyman SE |veditors=Sydor A, Brown RY | title = Molecular Neuropharmacology: A Foundation for Clinical Neuroscience | year = 2009 | publisher = McGraw-Hill Medical | location = New York | isbn = 9780071481274 | page = 4 | edition = 2nd |quote = Similarly, little is known about which of serotonin's 14 known receptors must be activated to achieve an antidepressant response. }}</ref> The 15th receptor 5-HT<sub>1P</sub>  has been distinguished on the basis of functional and radioligand binding studies, its existence has never been definitely affirmed or refuted.<ref>{{Cite book | vauthors = Brady ST |title=Basic Neurochemistry - Principles of Molecular, Cellular and Medical Neurobiology |publisher=USA: Elsevier |year=2012 |isbn=978-0-12-374947-5 |edition=8th |location= Waltham, MA |pages=320–321}}</ref><ref name=":1">{{cite journal | vauthors = Mitchell NA, Pepperell E, Ociepka S, Brown JD, Witherington J, Tuladhar B, Sanger GJ, Lee K, Cellek S | display-authors = 6 | title = 5-hydroxyindalpine, an agonist at the putative 5-HT receptor, has no activity on human recombinant monoamine receptors but accelerates distension-induced peristalsis in mouse isolated colon | journal = Neurogastroenterology and Motility | volume = 21 | issue = 7 | pages = 760–e48 | date = July 2009 | pmid = 19309442 | doi = 10.1111/j.1365-2982.2009.01275.x | s2cid = 9532359 }}</ref> The specific types have been characterized as follows:<ref name="urlSerotonin Receptor Subtypes and Ligands">{{cite web | url = http://www.acnp.org/g4/GN401000039/Ch039.html | title = Serotonin Receptor Subtypes and Ligands | access-date = 2008-04-11 |vauthors=Glennon RA, Dukat M, Westkaemper RB | date = 2000-01-01 | publisher = American College of Neurophyscopharmacology | archive-url= https://web.archive.org/web/20080421160353/http://www.acnp.org/g4/GN401000039/Ch039.html| archive-date= 21 April 2008 | url-status= live}}</ref><ref name="urlIUPHAR DATABASE | 5-HYDROXYTRYPTAMINE RECEPTORS">{{cite web | url = http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1288 | title = 5-Hydroxytryptamine Receptors | access-date = 2008-04-11 | work = IUPHAR Receptor Database | publisher = International Union of Basic and Clinical Pharmacology }}</ref><ref name="Wesolowska_2002">{{cite journal | vauthors = Wesołowska A | title = In the search for selective ligands of 5-HT5, 5-HT6 and 5-HT7 serotonin receptors | journal = Polish Journal of Pharmacology | volume = 54 | issue = 4 | pages = 327–341 | year = 2002 | pmid = 12523486 | url = http://www.if-pan.krakow.pl/pjp/pdf/2002/4_327.pdf }}</ref>

{| class="wikitable mw-collapsible"
!colspan=13|Information on serotonin receptors (human isoforms if nothing else is stated)
|-
!rowspan=2| Receptor
!rowspan=2| First [[Cloning|cloned]] – [[Protein Data Bank|PDB entries]]
!rowspan=2| Gene(s)
!colspan=6| Distribution
!rowspan=2| Function
!rowspan=2| [[Agonist]]s
!rowspan=2| [[Receptor antagonist|Antagonists]]
!rowspan=2| Uses of drugs that act on this receptor
|-
! [[Blood vessel]]s
! [[Central nervous system|CNS]]
! [[Gastrointestinal tract|GI Tract]]
! [[Platelet]]s
! [[Peripheral nervous system|PNS]]
! [[Smooth muscle tissue|Smooth Muscle]]
|-
| '''[[5-HT1A receptor|5-HT<sub>1A</sub>]]'''
|1987 – 
* 7e2x 
* 7e2y 
* 7e2z
[[File:7E2Y 5-HT1A receptor serotonin.png|60px]]
|
* {{Gene|HTR1A}}
| {{Yes}}
| {{Yes}}
| {{No}}
| {{No}}
| {{No}}
| {{No}}
|
* Addiction<ref name="pmid7862892">{{cite journal | vauthors = 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 | volume = 115 | issue = 1–2 | pages = 173–179 | date = June 1994 | pmid = 7862892 | doi = 10.1007/BF02244769 | s2cid = 38012716 }}</ref><ref name="pmid17316955">{{cite journal | vauthors = Müller CP, Carey RJ, Huston JP, De Souza Silva MA | title = Serotonin and psychostimulant addiction: focus on 5-HT1A-receptors | journal = Progress in Neurobiology | volume = 81 | issue = 3 | pages = 133–178 | date = February 2007 | pmid = 17316955 | doi = 10.1016/j.pneurobio.2007.01.001 | s2cid = 42788995 }}</ref><ref name="pmid15713268">{{cite journal | vauthors = 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 Research | volume = 1034 | issue = 1–2 | pages = 162–171 | date = February 2005 | pmid = 15713268 | doi = 10.1016/j.brainres.2004.12.012 | s2cid = 28356741 }}</ref>
* Aggression<ref name="pmid16310183">{{cite journal | vauthors = de Boer SF, Koolhaas JM | title = 5-HT1A and 5-HT1B receptor agonists and aggression: a pharmacological challenge of the serotonin deficiency hypothesis | journal = European Journal of Pharmacology | volume = 526 | issue = 1–3 | pages = 125–139 | date = December 2005 | pmid = 16310183 | doi = 10.1016/j.ejphar.2005.09.065 }}</ref>
* Anxiety<ref name="pmid9724773">{{cite journal | vauthors = Parks CL, Robinson PS, Sibille E, Shenk T, Toth M | title = Increased anxiety of mice lacking the serotonin1A receptor | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 95 | issue = 18 | pages = 10734–10739 | date = September 1998 | pmid = 9724773 | pmc = 27964 | doi = 10.1073/pnas.95.18.10734 | doi-access = free | bibcode = 1998PNAS...9510734P }}</ref>
* Appetite<ref name="pmid17609739">{{cite journal | vauthors = 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 and Findings in Experimental and Clinical Pharmacology | volume = 29 | issue = 4 | pages = 269–272 | date = May 2007 | pmid = 17609739 | doi = 10.1358/mf.2007.29.4.1075362 }}</ref>
* [[Autoreceptor]]
* Blood Pressure<ref name="pmid2842163">{{cite journal | vauthors = Wouters W, Tulp MT, Bevan P | title = Flesinoxan lowers blood pressure and heart rate in cats via 5-HT1A receptors | journal = European Journal of Pharmacology | volume = 149 | issue = 3 | pages = 213–223 | date = May 1988 | pmid = 2842163 | doi = 10.1016/0014-2999(88)90651-6 }}</ref><ref name="pmid18667366">{{cite journal | vauthors = 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 = Autonomic Neuroscience | volume = 142 | issue = 1–2 | pages = 71–76 | date = November 2008 | pmid = 18667366 | doi = 10.1016/j.autneu.2008.06.004 | s2cid = 20878941 }}</ref>
* Cardiovascular Function<ref name="pmid15802554">{{cite journal | vauthors = 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 = American Journal of Physiology. Regulatory, Integrative and Comparative Physiology | volume = 289 | issue = 2 | pages = R596–R604 | date = August 2005 | pmid = 15802554 | doi = 10.1152/ajpregu.00845.2004 | s2cid = 17426759 }}</ref>
* Emesis<ref name="pmid8013549">{{cite journal | vauthors = Lucot JB | title = Antiemetic effects of flesinoxan in cats: comparisons with 8-hydroxy-2-(di-n-propylamino)tetralin | journal = European Journal of Pharmacology | volume = 253 | issue = 1–2 | pages = 53–60 | date = February 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 | vauthors = 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 | date = April 2005 | pmid = 15688093 | doi = 10.1038/sj.npp.1300610 | doi-access = free }}</ref>
* Memory<ref name="pmid18394726">{{cite journal | vauthors = Ogren SO, Eriksson TM, Elvander-Tottie E, D'Addario C, Ekström JC, Svenningsson P, Meister B, Kehr J, Stiedl O | display-authors = 6 | title = The role of 5-HT(1A) receptors in learning and memory | journal = Behavioural Brain Research | volume = 195 | issue = 1 | pages = 54–77 | date = December 2008 | pmid = 18394726 | doi = 10.1016/j.bbr.2008.02.023 | s2cid = 140205386 }}</ref><ref name="pmid12562581">{{cite journal | vauthors = Yasuno F, Suhara T, Nakayama T, Ichimiya T, Okubo Y, Takano A, Ando T, Inoue M, Maeda J, Suzuki K | display-authors = 6 | title = Inhibitory effect of hippocampal 5-HT1A receptors on human explicit memory | journal = The American Journal of Psychiatry | volume = 160 | issue = 2 | pages = 334–340 | date = February 2003 | pmid = 12562581 | doi = 10.1176/appi.ajp.160.2.334 }}</ref>
* Mood<ref name="pmid2883013">{{cite journal | vauthors = Kennett GA, Dourish CT, Curzon G | title = Antidepressant-like action of 5-HT1A agonists and conventional antidepressants in an animal model of depression | journal = European Journal of Pharmacology | volume = 134 | issue = 3 | pages = 265–274 | date = February 1987 | pmid = 2883013 | doi = 10.1016/0014-2999(87)90357-8 }}</ref>
* Nausea<ref name="pmid8013549"/>
* Nociception<ref name="pmid12595749">{{cite 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 = 182–194 | date = April 2003 | pmid = 12595749 | doi = 10.1159/000068404 | s2cid = 25882138 }}</ref>
* Penile Erection<ref name="pmid9085055">{{cite journal | vauthors = Millan MJ, Perrin-Monneyron S | title = Potentiation of fluoxetine-induced penile erections by combined blockade of 5-HT1A and 5-HT1B receptors | journal = European Journal of Pharmacology | volume = 321 | issue = 3 | pages = R11–R13 | date = March 1997 | pmid = 9085055 | doi = 10.1016/S0014-2999(97)00050-2 }}</ref>
* Pupil Dilation<ref name="pmid8982715">{{cite journal | vauthors = Prow MR, Martin KF, Heal DJ | title = 8-OH-DPAT-induced mydriasis in mice: a pharmacological characterisation | journal = European Journal of Pharmacology | volume = 317 | issue = 1 | pages = 21–28 | date = December 1996 | pmid = 8982715 | doi = 10.1016/S0014-2999(96)00693-0 }}</ref>
* Respiration<ref name="pmid16166206">{{cite journal | vauthors = 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–R413 | date = February 2006 | pmid = 16166206 | doi = 10.1152/ajpregu.00440.2005 | s2cid = 224414 }}</ref>
* Sexual Behavior<ref name="pmid11965359">{{cite journal | vauthors = 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 = 609–618 | date = July 2002 | pmid = 11965359 | doi = 10.1016/S0306-4530(01)00097-X | s2cid = 25269315 }}</ref>
* Sleep<ref name="pmid10607047">{{cite journal | vauthors = 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 = Journal of Sleep Research | volume = 1 | issue = 3 | pages = 169–175 | date = September 1992 | pmid = 10607047 | doi = 10.1111/j.1365-2869.1992.tb00033.x | doi-access = free }}</ref>
* Sociability<ref name="pmid17383105">{{cite 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 = 509–514 | date = May 2007 | pmid = 17383105 | doi = 10.1016/j.neuroscience.2007.02.032 | s2cid = 15617471 }}</ref>
* Thermoregulation<ref name="pmid2951611">{{cite journal | vauthors = 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 = 1307–1313 | date = December 1986 | pmid = 2951611 | doi = 10.1016/0028-3908(86)90101-2 | s2cid = 2547042 }}</ref>
* Vasoconstriction<ref name="pmid16455061">{{cite journal | vauthors = 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 Research | volume = 1073-1074 | pages = 252–261 | date = February 2006 | pmid = 16455061 | doi = 10.1016/j.brainres.2005.12.031 | s2cid = 23178233 }}</ref>
|<!--5-HT1A AGONISTs-->
'''<span style="font-size:100%;">Selective (for 5-HT<sub>1A</sub> over other 5-HT receptors) </span>'''
* [[Vilazodone]] (Viibryd)
* [[F-15,599]] (research compound, highly potent and selective for 5-HT<sub>1A</sub>)
* [[Flesinoxan]] (potent, EC<sub>50</sub>&nbsp;=&nbsp;24&nbsp;nM)
* [[Gepirone]] ([[partial agonist]], K<sub>i</sub>&nbsp;=&nbsp;70&nbsp;nM)
* [[Haloperidol]]
* [[Ipsapirone]] (partial agonist, K<sub>i</sub>&nbsp;=&nbsp;12.1&nbsp;nM)
* [[Quetiapine]]
* [[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>&nbsp;=&nbsp;78&nbsp;nM)
* [[Yohimbine]] (unselective partial agonist)
* [[Tandospirone]] (potent and selective partial agonist)

'''<span style="font-size:100%;"> Nonselective </span>'''
* [[5-Carboxamidotryptamine|5-CT]] (potent – K<sub>i</sub>&nbsp;=&nbsp;250&nbsp;±&nbsp;50&nbsp;pM)
* [[8-OH-DPAT]] (potent)
* [[Aripiprazole]] (atypical antipsychotic)
* [[Asenapine]] (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)
* [[Vortioxetine]] (high-efficacy partial agonist)<ref name="vortioxetine">"BRINTELLIX (vortioxetine) tablets for oral use. Full Prescribing Information, Section 12.2 (Pharmacodynamics)." Takeda Pharmaceuticals America Inc. and Lundbeck, 2013. Revised September 2013. [http://general.takedapharm.com/content/file/pi.pdf?applicationcode=396066C6-E50F-4113-ABAD-54FE9525BF7E&filetypecode=BRINTELLIXPI] {{Webarchive|url=https://web.archive.org/web/20190918205248/http://general.takedapharm.com/content/file/pi.pdf?applicationcode=396066C6-E50F-4113-ABAD-54FE9525BF7E&filetypecode=BRINTELLIXPI|date=2019-09-18}}</ref>
* [[Ziprasidone]] (partial agonist, K<sub>i</sub>&nbsp;=&nbsp;3.4&nbsp;nM)
* [[Methylphenidate]] (weak agonist)

|<!--5-HT1A ANTAGONISTs-->
* [[BMY 7378]]
* [[Cyanopindolol]]
* [[Iodocyanopindolol]]
* [[Lecozotan]]
* [[Methiothepin]]
* [[Methysergide]]<ref>{{cite journal | vauthors = Saxena PR, Lawang A | title = A comparison of cardiovascular and smooth muscle effects of 5-hydroxytryptamine and 5-carboxamidotryptamine, a selective agonist of 5-HT1 receptors | journal = Archives Internationales de Pharmacodynamie et de Therapie | volume = 277 | issue = 2 | pages = 235–252 | date = October 1985 | pmid = 2933009 }}</ref>
* [[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]]<ref name="pmid9784072">{{cite journal | vauthors = 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 = 185–194 | date = October 1998 | pmid = 9784072 | doi = 10.1007/s002130050703 | s2cid = 9466299 }}</ref> (agonist and antagonist)
|-
| '''[[5-HT1B receptor|5-HT<sub>1B</sub>]]'''
|1992 – 
* 6g79  
|
* {{Gene|HTR1B}}
| {{Yes}}
| {{Yes}}
| {{No}}
| {{No}}
| {{No}}
| {{No}}
|
* Addiction<ref name="pmid10027505">{{cite journal | vauthors = 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 | volume = 141 | issue = 3 | pages = 242–250 | date = January 1999 | pmid = 10027505 | doi = 10.1007/s002130050831 | s2cid = 19974789 }}</ref>
* Aggression<ref name="pmid16310183"/>
* Anxiety<ref name="pmid15720791">{{cite journal | vauthors = Chojnacka-Wójcik E, Kłodzińska A, Tatarczyńska E | title = The anxiolytic-like effect of 5-HT1B receptor ligands in rats: a possible mechanism of action | journal = The Journal of Pharmacy and Pharmacology | volume = 57 | issue = 2 | pages = 253–257 | date = February 2005 | pmid = 15720791 | doi = 10.1211/0022357055399 | s2cid = 20743875 }}</ref><ref name="pmid11888549">{{cite journal | vauthors = Lin D, Parsons LH | title = Anxiogenic-like effect of serotonin(1B) receptor stimulation in the rat elevated plus-maze | journal = Pharmacology, Biochemistry, and Behavior | volume = 71 | issue = 4 | pages = 581–587 | date = April 2002 | pmid = 11888549 | doi = 10.1016/S0091-3057(01)00712-2 | s2cid = 21610537 }}</ref><ref name="pmid15577451">{{cite journal | vauthors = Tatarczyńska E, Kłodzińska 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 = Behavioural Pharmacology | volume = 15 | issue = 8 | pages = 523–534 | date = December 2004 | pmid = 15577451 | doi = 10.1097/00008877-200412000-00001 | s2cid = 6940756 }}</ref>
* [[Autoreceptor]]
* Learning<ref name="pmid18394658">{{cite journal | vauthors = 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 = 1041–1050 | date = June 2008 | pmid = 18394658 | doi = 10.1016/j.neuropharm.2008.02.007 | s2cid = 207223573 | hdl = 10616/40922 }}</ref>
* Locomotion<ref name="pmid10454466">{{cite journal | vauthors = 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 = The Journal of Pharmacology and Experimental Therapeutics | volume = 290 | issue = 3 | pages = 965–973 | date = September 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]]
* [[Vortioxetine]] (partial agonist, K<sub>i</sub>&nbsp;=&nbsp;33&nbsp;nM)<ref name="vortioxetine" />
|<!--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>]]'''
|1991 – 
* 7e32
[[File:7E32 5-HT1D receptor.png|60px]]
|
* {{Gene|HTR1D}}
| {{Yes}}
| {{Yes}}
| {{No}}
| {{No}}
| {{No}}
| {{No}}
|
* Anxiety<ref name="pmid15820416">{{cite journal | vauthors = 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 = European Neuropsychopharmacology | volume = 15 | issue = 3 | pages = 279–282 | date = May 2005 | pmid = 15820416 | doi = 10.1016/j.euroneuro.2004.12.002 | s2cid = 8382188 }}</ref><ref name="pmid8736648">{{cite journal | vauthors = 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 = Neuroscience Letters | volume = 209 | issue = 3 | pages = 210–214 | date = May 1996 | pmid = 8736648 | doi = 10.1016/0304-3940(96)12637-9 | s2cid = 27376524 | author5-link = Bernhard Landwehrmeyer }}</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]]
* [[Vortioxetine]] (K<sub>i</sub>&nbsp;=&nbsp;54&nbsp;nM)<ref name="vortioxetine" />
* [[Ziprasidone]]
|
* [[Migraines]] (e.g., [[triptans]])
|-
| '''[[5-HT1E|5-HT<sub>1E</sub>]]'''
|1992 – 
* 7e33
[[File:7E33 5-HT1E receptor.png|60px]]
|
* {{Gene|HTR1E}}
| {{Yes}}
| {{Yes}}
| {{No}}
| {{No}}
| {{No}}
| {{No}}
|
|
* [[BRL-54443]]
|
|
* None known
|-
| '''[[5-HT1F|5-HT<sub>1F</sub>]]'''
|1993 – 
* 7exd
[[File:7exd 5-HT1F receptor.png|60px]]
|
* {{Gene|HTR1F}}
| {{No}}
| {{Yes}}
| {{No}}
| {{No}}
| {{No}}
| {{No}}
|
* Migraine
|<!--5-HT1F AGONISTs-->
* [[BRL-54443]]
* [[Lasmiditan]]
* [[LY-334,370]]
* [[Naratriptan]]
* [[Eletriptan]]
|
|
* None known
|-
|'''5-HT<sub>1P</sub>'''
|Not cloned
|
| {{No}}
| {{No}}
| {{Yes}}
| {{No}}
| {{No}}
| {{No}}
|
* Peristalsis<ref name=":1" /><ref>{{cite journal | vauthors = Najjar SA, Hung LY, Margolis KG | title = Serotonergic Control of Gastrointestinal Development, Motility, and Inflammation | journal = Comprehensive Physiology | volume = 13 | issue = 3 | pages = 4851–4868 | date = June 2023 | pmid = 37358510 | doi = 10.1002/cphy.c220024 | pmc = 10373054 | isbn = 9780470650714 }}</ref>
|<!--5-HT1P AGONISTs-->
* [[5-hydroxyindalpine|5-OHIP]]<ref name=":1" /><ref>{{cite journal | vauthors = Branchek TA, Mawe GM, Gershon MD | title = Characterization and localization of a peripheral neural 5-hydroxytryptamine receptor subtype (5-HT1P) with a selective agonist, 3H-5-hydroxyindalpine | journal = The Journal of Neuroscience | volume = 8 | issue = 7 | pages = 2582–2595 | date = July 1988 | pmid = 3249244 | pmc = 6569501 | doi = 10.1523/JNEUROSCI.08-07-02582.1988 }}</ref>
* [[2-Methyl-5-hydroxytryptamine|2-Methyl-5-HT]]<ref>{{cite journal | vauthors = Mawe GM, Branchek TA, Gershon MD | title = Peripheral neural serotonin receptors: identification and characterization with specific antagonists and agonists | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 83 | issue = 24 | pages = 9799–9803 | date = December 1986 | pmid = 3467338 | pmc = 387229 | doi = 10.1073/pnas.83.24.9799 | doi-access = free | bibcode = 1986PNAS...83.9799M }}</ref>
* [[5-benzyloxyhydrazonoindalpine|5-BOHIP]]<ref>{{Cite journal |last1=Annaházi |first1=Anita |last2=Berger |first2=Thomas Erwin |last3=Demir |first3=Ihsan Ekin |last4=Zeller |first4=Florian |last5=Müller |first5=Michael |last6=Anneser |first6=Markus |last7=Skerra |first7=Arne |last8=Michel |first8=Klaus |last9=Schemann |first9=Michael |date=April 2022 |title=Metabotropic 5-HT receptor-mediated effects in the human submucous plexus |journal=Neurogastroenterology & Motility |language=en |volume=34 |issue=10 |pages=e14380 |doi=10.1111/nmo.14380 |pmid=35438222 |s2cid=248241342 |issn=1350-1925|doi-access=free }}</ref>
|<!--5-HT1P ANTAGONISTs-->
* [[5-hydroxytrytophan-dipeptide (5-hydroxytryptophyl-5-hydroxytryptophan amide)|5-HTP-DP]]<ref name=":1" />
|
* None known
|-
| '''[[5-HT2A receptor|5-HT<sub>2A</sub>]]'''
|1988
|
* {{Gene|HTR2A}}
| {{Yes}}
| {{Yes}}
| {{Yes}}
| {{Yes}}
| {{Yes}}
| {{Yes}}
|
* Addiction (potentially modulating)<ref name="Bubar">{{cite journal | vauthors = Bubar MJ, Cunningham KA | title = Serotonin 5-HT2A and 5-HT2C receptors as potential targets for modulation of psychostimulant use and dependence | journal = Current Topics in Medicinal Chemistry | volume = 6 | issue = 18 | pages = 1971–1985 | year = 2006 | pmid = 17017968 | doi = 10.2174/156802606778522131 }}</ref>
* Anxiety<ref name="pmid9539263">{{cite journal | vauthors = 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 | volume = 135 | issue = 4 | pages = 383–391 | date = February 1998 | pmid = 9539263 | doi = 10.1007/s002130050526 | s2cid = 22677071 }}</ref>
* Appetite
* Cognition
* Imagination
* Learning
* Memory
* Mood
* Perception
* Sexual Behavior<ref name="pmid12097814">{{cite journal | vauthors = 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 | date = July 2002 | pmid = 12097814 | doi = 10.1159/000063681 | s2cid = 42319246 }}</ref>
* Sleep<ref name="pmid16339018">{{cite journal | vauthors = Popa D, Léna C, Fabre V, Prenat C, Gingrich J, Escourrou P, Hamon M, Adrien J | display-authors = 6 | 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 = The Journal of Neuroscience | volume = 25 | issue = 49 | pages = 11231–11238 | date = December 2005 | pmid = 16339018 | pmc = 6725907 | doi = 10.1523/JNEUROSCI.1724-05.2005 }}</ref>
* Thermoregulation<ref name="pmid9106912">{{cite journal | vauthors = 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 | volume = 130 | issue = 2 | pages = 144–151 | date = March 1997 | pmid = 9106912 | doi = 10.1007/s002130050222 | s2cid = 22432569 | url = https://zenodo.org/record/1232625 }}</ref>
* Vasoconstriction<ref name="pmid12654345">{{cite journal | vauthors = 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 | s2cid = 53251590 }}</ref>
|<!--5-HT2A AGONISTs-->
* [[25I-NBOMe]] (Full  agonist)
* [[2C-B]]
* [[2C-I]]
* [[5-MeO-DMT]]
* [[Aripiprazole]] (very weak [[partial agonist]] or [[antagonist]]) 
* [[Benzylpiperazine|BZP]]
* [[Bufotenin]]
* [[Dimethyltryptamine|DMT]]
* [[2,5-Dimethoxy-4-methylamphetamine|DOM]]
* [[Ergonovine]]
* [[Lisuride]]
* [[LSD]]
* [[Mescaline]]
* [[PNU-22394]] (partial agonist)<ref name="McCall2001">{{cite conference| vauthors = McCall RB, Franklin SR, Hyslop DK, Knauer CS, Chio CL, Haber CL, Fitzgerald LW |title= PNU-22394, a 5-HT2C receptor agonist, reduced feeding in rodents and produces weight loss in humans |date= 2001 |conference= Society for Neuroscience |others= Presentation Number 309.2 | volume = 27 | issue = 309.2 |publisher= Society for Neuroscience Abstracts |url= http://www.sfn.org/Annual-Meeting/Past-and-Future-Annual-Meetings/Abstract-Archive/Abstract-Archive-Detail?AbsYear=2001&AbsID=4715 |page=TT-45| location=San Diego, CA |format= Online |access-date= 18 July 2014}}</ref><ref name="pmid19029184">{{cite journal | vauthors = Garfield AS, Heisler LK | title = Pharmacological targeting of the serotonergic system for the treatment of obesity | journal = The Journal of Physiology | volume = 587 | issue = 1 | pages = 49–60 | date = January 2009 | pmid = 19029184 | pmc = 2670022 | doi = 10.1113/jphysiol.2008.164152 }}</ref><ref name="Jensen2013">{{cite journal | vauthors = Jensen AA, Plath N, Pedersen MH, Isberg V, Krall J, Wellendorph P, Stensbøl TB, Gloriam DE, Krogsgaard-Larsen P, Frølund B | display-authors = 6 | title = Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties | journal = Journal of Medicinal Chemistry | volume = 56 | issue = 3 | pages = 1211–1227 | date = February 2013 | pmid = 23301527 | doi = 10.1021/jm301656h | citeseerx = 10.1.1.691.154 }}</ref>
* [[Psilocin]]
* [[Psilocybin]]
* [[TFMPP]] (partial agonist or antagonist)
|<!--5-HT2A ANTAGONISTs-->
* [[Atypical antipsychotic]]s
** [[Clozapine]]<ref name="pharmamotion" />
** [[Olanzapine]]
** [[Quetiapine]]
** [[Risperidone]]
** [[Ziprasidone]]
* [[Asenapine]]
* [[Amitriptyline]]
* [[Clomipramine]]
* [[Cyproheptadine]]
* [[Doxepin]]
* [[Eplivanserin]]
* [[Etoperidone]]
* [[Haloperidol]]
* [[Hydroxyzine]]
* [[Iloperidone]]
* [[Ketanserin]]<ref name=pharmamotion/> ([[antihypertensive]]<ref name=pharmamotion/>)
* [[Methysergide]]
* [[Mianserin]]
* [[Mirtazapine]]
* [[Nefazodone]]
* [[Pimavanserin]]
* [[Pizotifen]]
* [[Ritanserin]]
* [[Trazodone]]
* [[Yohimbine]]
|
* [[Atypical antipsychotic]]s (antagonist)
* [[Psychedelics]] (agonists)
* [[NaSSA]]s (antidepressants and anxiolytics; they serve as antagonists at this site)
* Treating [[serotonin syndrome]] (antagonists; e.g., [[cyproheptadine]])
* Sleeping aid (antagonists; e.g., trazodone)
|-
| '''[[5-HT2B receptor|5-HT<sub>2B</sub>]]'''
|1992
|
* {{Gene|HTR2B}}
| {{Yes}}
| {{Yes}}
| {{Yes}}
| {{Yes}}
| {{Yes}}
| {{Yes}}
|
* Anxiety<ref name="pmid8730737">{{cite journal | vauthors = 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 = British Journal of Pharmacology | volume = 117 | issue = 7 | pages = 1443–1448 | date = April 1996 | pmid = 8730737 | pmc = 1909458 | doi = 10.1111/j.1476-5381.1996.tb15304.x }}</ref><ref name="pmid9225285">{{cite journal | vauthors = 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 = 601–608 | year = 1997 | pmid = 9225285 | doi = 10.1016/S0028-3908(97)00042-7 | s2cid = 41471226 }}</ref><ref name="pmid9886683">{{cite journal | vauthors = 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 = 1603–1610 | date = December 1998 | pmid = 9886683 | doi = 10.1016/S0028-3908(98)00115-4 | s2cid = 7310462 }}</ref>
* Appetite<ref name="pmid9144661">{{cite journal | vauthors = 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 = 233–239 | date = February 1997 | pmid = 9144661 | doi = 10.1016/S0028-3908(96)00171-2 | s2cid = 23583570 }}</ref>
* Cardiovascular Function
* GI Motility<ref name="pmid11877320">{{cite journal | vauthors = Borman RA, Tilford NS, Harmer DW, Day N, Ellis ES, Sheldrick RL, Carey J, Coleman RA, Baxter GS | display-authors = 6 | title = 5-HT(2B) receptors play a key role in mediating the excitatory effects of 5-HT in human colon in vitro | journal = British Journal of Pharmacology | volume = 135 | issue = 5 | pages = 1144–1151 | date = March 2002 | pmid = 11877320 | pmc = 1573235 | doi = 10.1038/sj.bjp.0704571 }}</ref>
* Sleep<ref name="pmid16339018"/>
* Vasoconstriction
|<!--5-HT2B AGONISTs-->
* [[6-APB]] (full agonist)
* [[BW-723C86]]
* [[Fenfluramine]]
* [[MDMA]]
* [[Norfenfluramine]]
* [[PNU-22394]] (partial agonist)<ref name="McCall2001" /><ref name="pmid19029184" /><ref name="Jensen2013" />
* [[Ro60-0175]]
* [[Methylphenidate]] (weak agonist)

|<!--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>]]'''
|1988
|
* {{Gene|HTR2C}}
| {{Yes}}
| {{Yes}}
| {{Yes}}
| {{Yes}}
| {{Yes}}
| {{Yes}}
|
* Addiction (potentially modulating)<ref name="Bubar"/>
* Anxiety<ref name="pmid9225286">{{cite journal | vauthors = 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 | display-authors = 6 | title = SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist | journal = Neuropharmacology | volume = 36 | issue = 4–5 | pages = 609–620 | year = 1997 | pmid = 9225286 | doi = 10.1016/S0028-3908(97)00038-5 | s2cid = 23032157 }}</ref><ref name="pmid15289999">{{cite journal | vauthors = 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 | volume = 177 | issue = 4 | pages = 448–458 | date = February 2005 | pmid = 15289999 | doi = 10.1007/s00213-004-1962-z | s2cid = 20866665 }}</ref><ref name="pmid18523738">{{cite journal | vauthors = Dekeyne A, Mannoury la Cour C, Gobert A, Brocco M, Lejeune F, Serres F, Sharp T, Daszuta A, Soumier A, Papp M, Rivet JM, Flik G, Cremers TI, Muller O, Lavielle G, Millan MJ | display-authors = 6 | title = S32006, a novel 5-HT2C receptor antagonist displaying broad-based antidepressant and anxiolytic properties in rodent models | journal = Psychopharmacology | volume = 199 | issue = 4 | pages = 549–568 | date = September 2008 | pmid = 18523738 | doi = 10.1007/s00213-008-1177-9 | s2cid = 25063495 }}</ref>
* Appetite
* GI Motility<ref name="pmid19058784">{{cite journal | vauthors = Fujitsuka N, Asakawa A, Hayashi M, Sameshima M, Amitani H, Kojima S, Fujimiya M, Inui A | display-authors = 6 | title = Selective serotonin reuptake inhibitors modify physiological gastrointestinal motor activities via 5-HT2c receptor and acyl ghrelin | journal = Biological Psychiatry | volume = 65 | issue = 9 | pages = 748–759 | date = May 2009 | pmid = 19058784 | doi = 10.1016/j.biopsych.2008.10.031 | s2cid = 22053616 }}</ref>
* [[Heteroreceptor]] for [[norepinephrine]] and [[dopamine]]
* Locomotion
* Mood<ref name="pmid15289999"/><ref name="pmid18523738"/>
* Penile Erection<ref name="pmid9151932">{{cite journal | vauthors = 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 = European Journal of Pharmacology | volume = 325 | issue = 1 | pages = 9–12 | date = April 1997 | pmid = 9151932 | doi = 10.1016/S0014-2999(97)89962-1 }}</ref><ref name="pmid8001637">{{cite journal | vauthors = 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 = European Journal of Pharmacology | volume = 261 | issue = 1–2 | pages = 149–155 | date = August 1994 | pmid = 8001637 | doi = 10.1016/0014-2999(94)90313-1 }}</ref>
* Sexual Behavior<ref name="pmid12097814"/>
* Sleep<ref name="pmid12431861">{{cite journal | vauthors = 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 = 869–873 | date = November 2002 | pmid = 12431861 | pmc = 2452994 | doi = 10.1016/S0893-133X(02)00353-6 }}</ref>
* Thermoregulation<ref name="pmid9106912"/>
* Vasoconstriction
|<!--5-HT2C AGONISTs-->
*[[2C-B]] (partial agonist)<ref>{{cite journal | vauthors = Villalobos CA, Bull P, Sáez P, Cassels BK, Huidobro-Toro JP | title = 4-Bromo-2,5-dimethoxyphenethylamine (2C-B) and structurally related phenylethylamines are potent 5-HT2A receptor antagonists in Xenopus laevis oocytes | journal = British Journal of Pharmacology | volume = 141 | issue = 7 | pages = 1167–1174 | date = April 2004 | pmid = 15006903 | pmc = 1574890 | doi = 10.1038/sj.bjp.0705722 }}</ref>
*[[A-372,159]]
* [[AL-38022A]]
* [[Aripiprazole]]
* [[Ergonovine]]
* [[Lorcaserin]]
* [[PNU-22394]] (full agonist)<ref name="McCall2001" /><ref name="pmid19029184" /><ref name="Jensen2013" />
* [[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]]
* [[Haloperidol]]
* [[Iloperidone]]
* [[Ketanserin]]<ref name=pharmamotion/> ([[antihypertensive]]<ref name=pharmamotion/>)
* [[Lisuride]]
* [[Methysergide]]<ref name=Rang187>{{cite book | vauthors = Rang HP |title=Pharmacology |publisher=Churchill Livingstone |location=Edinburgh |year=2003 |isbn=978-0-443-07145-4 }} Page 187</ref>
* [[Mianserin]]
* [[Mirtazapine]]
* [[Nefazodone]]
* [[Olanzapine]]
* [[Paroxetine]]
* [[Quetiapine]]
* [[Risperidone]]
* [[Ritanserin]]
* [[SB-242084]]
* [[Tramadol]]
* [[Trazodone]]
* [[Ziprasidone]]
|
* [[Antidepressant]] (antagonists; e.g., [[agomelatine]], [[fluoxetine]], [[mirtazapine]])
* [[Orexigenic]] (e.g., mirtazapine, clozapine and olanzapine; antagonists)
* [[Anorectic]] (Lorcaserin; agonist)
* [[Antipsychotic]] (Vabicaserin; agonists)
|-
| '''[[5-HT3 receptor|5-HT<sub>3</sub>]]'''
|1993
|
* {{Gene|HTR3A}}
* {{Gene|HTR3B}}
* {{Gene|HTR3C}}
* {{Gene|HTR3D}}
* {{Gene|HTR3E}}
| {{No}}
| {{Yes}}
| {{Yes}}
| {{No}}
| {{Yes}}
| {{No}}
|
* Addiction
* Anxiety
* Emesis
* GI Motility<ref>{{cite journal | vauthors = Michel K, Zeller F, Langer R, Nekarda H, Kruger D, Dover TJ, Brady CA, Barnes NM, Schemann M | display-authors = 6 | title = Serotonin excites neurons in the human submucous plexus via 5-HT3 receptors | journal = Gastroenterology | volume = 128 | issue = 5 | pages = 1317–1326 | date = May 2005 | pmid = 15887114 | doi = 10.1053/j.gastro.2005.02.005 | doi-access = free }}</ref>
* Learning<ref name="pmid8115433">{{cite journal | vauthors = 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 = Pharmacology, Biochemistry, and Behavior | volume = 47 | issue = 1 | pages = 95–99 | date = January 1994 | pmid = 8115433 | doi = 10.1016/0091-3057(94)90116-3 | s2cid = 21800364 }}</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]]
* [[Vortioxetine]] (K<sub>i</sub>&nbsp;=&nbsp;3.7&nbsp;nM)<ref name="vortioxetine" />
|
* [[Antiemetic]]
* [[Antidepressant]] (e.g., mirtazpine)
* [[antipsychotic]] (e.g., olanzapine, quetiapine)
|-
| '''[[5-HT4 receptor|5-HT<sub>4</sub>]]'''
|1995
|
* {{Gene|HTR4}}
| {{No}}
| {{Yes}}
| {{Yes}}
| {{No}}
| {{Yes}}
| {{No}}
|
* Anxiety<ref name="pmid14676321">{{cite journal | vauthors = 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 = Proceedings of the National Academy of Sciences of the United States of America | volume = 100 | issue = 26 | pages = 15370–15375 | date = December 2003 | pmid = 14676321 | pmc = 307574 | doi = 10.1073/pnas.2436556100 | doi-access = free | bibcode = 2003PNAS..10015370S }}</ref><ref name="pmid9225297">{{cite journal | vauthors = 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 = 707–712 | year = 1997 | pmid = 9225297 | doi = 10.1016/S0028-3908(97)00037-3 | s2cid = 40341646 }}</ref>
* Appetite<ref name="pmid17913892">{{cite journal | vauthors = Jean A, Conductier G, Manrique C, Bouras C, Berta P, Hen R, Charnay Y, Bockaert J, Compan V | display-authors = 6 | title = Anorexia induced by activation of serotonin 5-HT4 receptors is mediated by increases in CART in the nucleus accumbens | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 104 | issue = 41 | pages = 16335–16340 | date = October 2007 | pmid = 17913892 | pmc = 2042207 | doi = 10.1073/pnas.0701471104 | doi-access = free | bibcode = 2007PNAS..10416335J }}</ref><ref name="pmid15146954">{{cite journal | vauthors = Compan V, Charnay Y, Dusticier N, Daszuta A, Hen R, Bockaert J | title = [Feeding disorders in 5-HT4 receptor knockout mice] | journal = Journal de la Société de Biologie | volume = 198 | issue = 1 | pages = 37–49 | year = 2004 | pmid = 15146954 | doi = 10.1051/jbio/2004198010037 | s2cid = 90408378 }}</ref>
* GI Motility
* Learning<ref name="Meneses A, Hong E 1997 347–51">{{cite journal | vauthors = Meneses A, Hong E | title = Effects of 5-HT4 receptor agonists and antagonists in learning | journal = Pharmacology, Biochemistry, and Behavior | volume = 56 | issue = 3 | pages = 347–351 | date = March 1997 | pmid = 9077568 | doi = 10.1016/S0091-3057(96)00224-9 | s2cid = 11866740 }}</ref><ref name="pmid9225295">{{cite journal | vauthors = 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 = 689–696 | year = 1997 | pmid = 9225295 | doi = 10.1016/S0028-3908(97)00055-5 | s2cid = 46510811 }}</ref>
* Memory<ref name="Meneses A, Hong E 1997 347–51"/><ref name="pmid9225295"/><ref name="pmid9732367">{{cite journal | vauthors = Galeotti N, Ghelardini C, Bartolini A | title = Role of 5-HT4 receptors in the mouse passive avoidance test | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 286 | issue = 3 | pages = 1115–1121 | date = September 1998 | pmid = 9732367 }}</ref>
* Mood<ref name="pmid17785179">{{cite journal | vauthors = 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 | display-authors = 6 | title = Serotonin(4) (5-HT(4)) receptor agonists are putative antidepressants with a rapid onset of action | journal = Neuron | volume = 55 | issue = 5 | pages = 712–725 | date = September 2007 | pmid = 17785179 | doi = 10.1016/j.neuron.2007.07.041 | s2cid = 14558104 | doi-access = free }}</ref><ref name="pmid17785173">{{cite journal | vauthors = Duman RS | title = A silver bullet for the treatment of depression? | journal = Neuron | volume = 55 | issue = 5 | pages = 679–681 | date = September 2007 | pmid = 17785173 | doi = 10.1016/j.neuron.2007.08.011 | doi-access = free }}</ref>
* Respiration<ref name="Manzke2003">{{cite journal | vauthors = Manzke T, Guenther U, Ponimaskin EG, Haller M, Dutschmann M, Schwarzacher S, Richter DW | title = 5-HT4(a) receptors avert opioid-induced breathing depression without loss of analgesia | journal = Science | volume = 301 | issue = 5630 | pages = 226–229 | date = July 2003 | pmid = 12855812 | doi = 10.1126/science.1084674 | s2cid = 13641423 | bibcode = 2003Sci...301..226M }}</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]]
|
* [[Prokinetic agent|Gastroprokinetics]] (e.g., Tegaserod)
|-
| '''[[5-HT5A receptor|5-HT<sub>5A</sub>]]'''
|1994

* [https://www.rcsb.org/structure/7UM4 7UM4]
* [https://www.rcsb.org/structure/7UM5 7UM5]
* [https://www.rcsb.org/structure/7UM6 7UM6]
* [https://www.rcsb.org/structure/7UM7 7UM7]
|
* {{Gene|HTR5A}}
| {{No}}
| {{Yes}}
| {{No}}
| {{No}}
| {{No}}
| {{No}}
|
* [[Autoreceptor]]
* Locomotion<ref name="pmid14965244">{{cite journal | vauthors = Nelson DL | title = 5-HT5 receptors | journal = Current Drug Targets. CNS and Neurological Disorders | volume = 3 | issue = 1 | pages = 53–58 | date = February 2004 | pmid = 14965244 | doi = 10.2174/1568007043482606 }}</ref>
* Sleep<ref name="pmid15921820">{{cite journal | vauthors = 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 Research. Molecular Brain Research | volume = 138 | issue = 2 | pages = 191–197 | date = August 2005 | pmid = 15921820 | pmc = 5805132 | doi = 10.1016/j.molbrainres.2005.04.009 }}</ref>
|<!--5-HT5A AGONISTs-->
* [[5-Carboxamidotryptamine|5-CT]]
* [[Ergotamine]]
* [[Lisuride]] (partial)<ref name=":0">{{cite journal | vauthors = Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL | display-authors = 6 | title = Inactive and active state structures template selective tools for the human 5-HT<sub>5A</sub> receptor | journal = Nature Structural & Molecular Biology | volume = 29 | issue = 7 | pages = 677–687 | date = July 2022 | pmid = 35835867 | pmc = 9299520 | doi = 10.1038/s41594-022-00796-6 }}</ref>
* [[Methylergometrine]] (full)<ref name=":0" />
* [[Valerenic acid|Valerenic Acid]] (partial agonist)<ref name="pmid15921820"/>
|<!--5-HT5A ANTAGONISTs-->
* [[Asenapine]]
* [[Dimebolin]]
* [[Methiothepin]]
* [[Ritanserin]]
* [[SB-699,551]]
* [[SB-699,551-A]]
* MS112<ref name=":0" /> 
|
* None thus far
|-
| '''[[5-HT5B receptor|5-HT<sub>5B</sub>]]'''
|1993
|
* {{Gene|HTR5BP}}
| {{No}}
| {{No}}
| {{No}}
| {{No}}
| {{No}}
| {{No}}
|
<small>Functions in rodents,<br/>[[pseudogene]] in humans</small>
|
|
|
* None thus far
|-
| '''[[5-HT6 receptor|5-HT<sub>6</sub>]]'''
|1993
|
* {{Gene|HTR6}}
| {{No}}
| {{Yes}}
| {{No}}
| {{No}}
| {{No}}
| {{No}}
|
* Anxiety<ref name="pmid18096153">{{cite journal | vauthors = Wesołowska 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 = 355–360 | date = February 2008 | pmid = 18096153 | doi = 10.1016/j.ejphar.2007.11.022 }}</ref><ref name="pmid17320917">{{cite journal | vauthors = Wesołowska 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 = 1274–1283 | date = April 2007 | pmid = 17320917 | doi = 10.1016/j.neuropharm.2007.01.007 | s2cid = 22664564 }}</ref>
* Cognition<ref name="pmid17069795">{{cite journal | vauthors = 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 | display-authors = 6 | 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 = 109–119 | date = December 2006 | pmid = 17069795 | doi = 10.1016/j.ejphar.2006.09.049 }}</ref>
* Learning<ref name="pmid15964617">{{cite journal | vauthors = 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 = 673–682 | date = July 2005 | pmid = 15964617 | doi = 10.1016/j.pbb.2005.05.005 | s2cid = 19789219 }}</ref>
* Memory<ref name="pmid15964617"/>
* Mood<ref name="pmid17320917"/><ref name="pmid18234190">{{cite journal | vauthors = Wesołowska 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 | date = March 2008 | pmid = 18234190 | doi = 10.1016/j.ejphar.2007.12.013 }}</ref>
|<!--5-HT6 AGONISTs-->
* [[EMD-386,088]]
* [[2-Ethyl-5-methoxy-N,N-dimethyltryptamine|EMDT]]
* [[WAY-181,187]]
* [[WAY-208,466]]
* [[E-6837]]
* N-(inden-5-yl)imidazothiazole-5-sulfonamide (43)<ref name="pmid19159187">{{cite journal | vauthors = Alcalde E, Mesquida N, López-Pérez S, Frigola J, Mercè R | title = Indene-based scaffolds. 2. An indole-indene switch: discovery of novel indenylsulfonamides as 5-HT<sub>6</sub> serotonin receptor agonists | journal = Journal of Medicinal Chemistry | volume = 52 | issue = 3 | pages = 675–87 | date = Feb 2009 | pmid = 19159187 | doi = 10.1021/jm8009469 }}</ref>
|<!--5-HT6 ANTAGONISTs-->
* [[Amitriptyline]]
* [[Aripiprazole]]
* [[Asenapine]]
* [[Clomipramine]]
* [[Clozapine]]
* [[Dimebolin]]
* [[EGIS-12233]]
* [[Haloperidol]]
* [[Iloperidone]]
* [[MS-245]]
* [[Olanzapine]]
* [[Ro04-6790]]
* [[SB-258,585]]
* [[SB-271,046]]<ref name="abpi2003">{{cite web|url=http://www.abpi.org.uk/publications/publication_details/targetSchizophrenia-2003/section5.asp |title=Target Schizophrenia - Possible future developments |access-date=2008-04-11 |publisher=The Association of the British Pharmaceutical Industry |archive-url=https://web.archive.org/web/20080612135635/http://www.abpi.org.uk/publications/publication_details/targetSchizophrenia-2003/section5.asp |archive-date=2008-06-12 |url-status=dead }}</ref>
* [[SB-357,134]]
* [[SB-399,885]]
|
* [[Antidepressant]] (antagonists and agonists)
* [[Anxiolytic]] (antagonists and agonist)
* [[Nootropic]] (antagonists)
* [[Anorectic]] (antagonists)
|-
| '''[[5-HT7 receptor|5-HT<sub>7</sub>]]'''
|1993
|
* {{Gene|HTR7}}
| {{Yes}}
| {{Yes}}
| {{Yes}}
| {{No}}
| {{No}}
| {{No}}
|
* Anxiety<ref name="pmid16018977">{{cite journal | vauthors = 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 = 831–837 | date = November 2005 | pmid = 16018977 | doi = 10.1016/j.biopsych.2005.05.012 | s2cid = 10998014 }}</ref><ref name="pmid16828124">{{cite journal | vauthors = Wesołowska A, Nikiforuk A, Stachowicz K, Tatarczyńska 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 = 578–586 | date = September 2006 | pmid = 16828124 | doi = 10.1016/j.neuropharm.2006.04.017 | s2cid = 39928418 }}</ref>
* [[Autoreceptor]]
* Memory<ref name="pmid18308404">{{cite journal | vauthors = 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 = 164–170 | date = December 2008 | pmid = 18308404 | doi = 10.1016/j.bbr.2007.12.020 | s2cid = 12910296 }}</ref><ref name="pmid18570192">{{cite journal | vauthors = 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 = 965–974 | year = 2008 | pmid = 18570192 | doi = 10.1002/hipo.20459 | s2cid = 20937527 }}</ref>
* Mood<ref name="pmid16018977"/><ref name="pmid16828124"/>
* Respiration<ref name="pmid16166206"/><ref name="pmid17314195">{{cite journal | vauthors = Bonaventure P, Kelly L, Aluisio L, Shelton J, Lord B, Galici R, Miller K, Atack J, Lovenberg TW, Dugovic C | display-authors = 6 | 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 = The Journal of Pharmacology and Experimental Therapeutics | volume = 321 | issue = 2 | pages = 690–698 | date = May 2007 | pmid = 17314195 | doi = 10.1124/jpet.107.119404 | s2cid = 14579645 }}</ref>
* Sleep<ref name="pmid16018977"/><ref name="pmid17314195"/><ref name="pmid12812993">{{cite journal | vauthors = 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 | display-authors = 6 | title = SB-656104-A, a novel selective 5-HT7 receptor antagonist, modulates REM sleep in rats | journal = British Journal of Pharmacology | volume = 139 | issue = 4 | pages = 705–714 | date = June 2003 | pmid = 12812993 | pmc = 1573887 | doi = 10.1038/sj.bjp.0705290 }}</ref>
* Thermoregulation
* Vasoconstriction
* Immunostimulation<ref>{{Cite journal |last1=León-Ponte |first1=Matilde |last2=Ahern |first2=Gerard P. |last3=O'Connell |first3=Peta J. |date=2007-04-15 |title=Serotonin provides an accessory signal to enhance T-cell activation by signaling through the 5-HT7 receptor |url=https://ashpublications.org/blood/article/109/8/3139/23709/Serotonin-provides-an-accessory-signal-to-enhance |journal=Blood |language=en |volume=109 |issue=8 |pages=3139–3146 |doi=10.1182/blood-2006-10-052787 |issn=0006-4971 |pmc=1852236 |pmid=17158224}}</ref>
|<!--5-HT7 AGONISTs-->
* [[5-Carboxamidotryptamine|5-CT]]
* [[8-OH-DPAT]]
* [[Aripiprazole]] ([[partial agonist]])<ref>Davies MA, Sheffler DJ, [[Bryan Roth|Roth BL]]. Aripiprazole: A Novel Atypical Antipsychotic Drug With a Uniquely Robust Pharmacology. CNS Drug Reviews [Internet]. 2004 [cited 2013 Aug 4];10(4):317–36. Available from: http://onlinelibrary.wiley.com/doi/10.1111/j.1527-3458.2004.tb00030.x/pdf</ref>
* [[AS-19 (drug)|AS-19]]
* [[E-55888]]
|<!--5-HT7 ANTAGONISTs-->
* [[Amitriptyline]]
* [[Asenapine]]
* [[Clomipramine]]
* [[Clozapine]]
* [[EGIS-12233]]
* [[Haloperidol]]
* [[Iloperidone]]
* [[Imipramine]]
* [[Ketanserin]]
* [[Mirtazapine]]
* [[Olanzapine]]
* [[1-(2-Diphenyl)piperazine|RA-7]]
* [[Ritanserin]]
* [[Risperidone]]
* [[SB-269,970]]
* [[Vortioxetine]] (K<sub>i</sub>&nbsp;=&nbsp;19&nbsp;nM)<ref name="vortioxetine" />
|
* [[Antidepressant]] (antagonists)
* [[Anxiolytics]] (antagonists)
* [[Nootropic]] (antagonists)
|}

Note that there is no 5-HT<sub>1C</sub> receptor since, after the receptor was cloned and further characterized, it was found to have more in common with the 5-HT<sub>2</sub> family of receptors and was redesignated as the 5-HT<sub>2C</sub> receptor.<ref>{{cite web |url= https://www.ncbi.nlm.nih.gov/gene?cmd=Retrieve&dopt=full_report&list_uids=3358 |title= HTR2C 5-hydroxytryptamine receptor 2C [ Homo sapiens (human) ] |date= 19 Mar 2017 |website= NCBI |access-date= 26 Mar 2017}}</ref>

Very nonselective agonists of 5-HT receptor subtypes include [[ergotamine]] (an [[antimigraine]]), which activates 5-HT<sub>1A</sub>, 5-HT<sub>1D</sub>, 5-HT<sub>1B</sub>, D<sub>2</sub> and [[norepinephrine receptor]]s.<ref name=pharmamotion/> LSD (a [[psychedelic drug|psychedelic]]) is a 5-HT<sub>1A</sub>, 5-HT<sub>2A</sub>, 5-HT<sub>2C</sub>, 5-HT<sub>5A</sub> and 5-HT<sub>6</sub> agonist.<ref name=pharmamotion/>