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5-hydroxytryptamine (serotonin) receptor 2C
Identifiers
Symbols HTR2C; 5-HT2C; HTR1C
External IDs OMIM: 312861 MGI: 96281 HomoloGene: 20242 IUPHAR: 5-HT2C GeneCards: HTR2C Gene
RNA expression pattern
PBB GE HTR2C 211479 s at tn.png
PBB GE HTR2C 207307 at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez 3358 15560
Ensembl ENSG00000147246 ENSMUSG00000041380
UniProt P28335 Q8BUB1
RefSeq (mRNA) NM_000868 XM_978183
RefSeq (protein) NP_000859 XP_983277
Location (UCSC) Chr X:
113.72 - 114.05 Mb		 Chr X:
142.21 - 142.44 Mb
PubMed search [1] [2]

5-hydroxytryptamine (serotonin) receptor 2C, also known as HTR2C, is a 5-HT2 receptor, but it also denotes the human gene encoding it.[1]

Contents

[edit] Function

The 5-HT2C receptor is one of the many binding sites for serotonin. Activation of this receptor by serotonin inhibits dopamine and norepinephrine release in certain areas of the brain.[4]

[edit] Clinical significance

Question book-new.svg
 This section needs additional citations for verification.
Please help improve this article by adding reliable references. Unsourced material may be challenged and removed. (July 2009)

Research indicates that some suicide victims have an abnormally high number of 5HT2C receptors in the prefrontal cortex.[5] Agomelatine, a 5HT2C antagonist, functions as an effective antidepressant due to its antagonism of 5HT2C receptors, thus causing a rise in dopamine and norepinephrine levels in many areas of the brain. Fluoxetine (Prozac) and other SSRIs indirectly stimulates 5HT2C function by increasing the level of serotonin in the synapse. In contrast, some atypical antipsychotics partially block 5HT2C receptors. Fluoxetine does also act as a direct 5HT2C antagonist in addition to inhibiting serotonin reuptake.[6]

The 5HT2C receptor when activated causes anxiety, social anxiety, depression, and compulsive behaviors in human and rat subjects. A significant portion of depressed, anxious, and socially anxious individuals may have an overactivity of 5HT2C receptors in the brain. Activation of 5HT2C by serotonin is responsible for many of the negative side effects of SSRI medications, such as sertraline, paroxetine, venlafaxine, and others. Some of the intitial anxiety caused by SSRIs is due to excessive signalling at this receptor. Over a period of 1–2 weeks, the receptor begins to downregulate, along with the downregulation of 5HT2A receptors. This downregulation parallels the clinical benefit of SSRIs.

The 5HT2C receptor is subject to rapid downregulation by serotonin and serotonin agonists.

5HT2C receptors mediate the release of dopamine in response to many drugs,[7][8] including caffeine, nicotine, amphetamine, morphine, and many others. 5HT2C antagonism will result in a much greater release of dopamine in response to drugs, and any dopaminergic stimulus. Sex, consumption of beverages and food, along with social interaction are all releasers of dopamine in the brain. A higher number of 5HT2C receptors in the brain will decrease the dopamine release in response to these activities. 5HT2C agonism will result in anorexic behavior, as 5HT2C antagonism will result in a higher consuption of food. 5HT2C agonism causes a hypolocomotor effect in rats and humans, suggesting the 5HT2C receptors cause depressive and anxiety symptoms.

Many G-protein coupled receptors downregulate in response to agonists for the receptor, and upregulate in response to antagonists. The 5HT2A and 5HT2C receptors appear to downregulate in response to both antagonists and agonists. Chronic treatment with antipsychotic drugs, which possess 5HT2 antagonist activity, results in down regulation of both 5HT2A and 5HT2C, as does chronic treatment with SSRIs and other 5HT agonists.[9]

Conditions that increase cytokine levels in the human body may have potential to raise 5HT2C gene expression in the brain. This could possibly comprise a link between viral infections and associated depression. Cytokine therapy has been shown to increase 5ht2c gene expression, resulting in increased activity of 5ht2c receptors in the brain.

[edit] Ligands

Numerous (ex-)prescription, illicit and research drugs contain a 5-HT2C component in their binding profile, including fluoxetine, mianserin, clozapine, agomelatine, dextro-norfenfluramine, psilocin, DOI, α-methyl-serotonin, MK-212, Org 37684, m-CPP, FG-7142,[10] Ro60-0175,[11] mesulergine, metergoline, ritanserin, methiothepin, 5-methoxygramine, and many more.[12] Some compounds with a more pronounced selectivity for the 5-HT2C receptor subtype are listed below. Note, that in the following context the term "functional selectivity" does not refer to differentiation of transductional pathways.

[edit] Agonists

[edit] Antagonists

  • FR-260,010: high affinity, selective over 5-HT2A and many other receptors; orally active.[23]
  • RS-102,221: 100-fold selectivity compared to the 5-HT2A and -HT2B receptor subtypes[24]
  • SB-200,646: mixed 5-HT2B/2C antagonist
  • SB-206,553: mixed 5-HT2B/2C antagonist
  • SB-221,284: mixed 5-HT2B/2C antagonist
  • compound 15k: IC50 = 0.5 nM; >2000x selective over 5-HT1A, 5-HT-2A, and 5-HT-6, and dopamine D2–D4 receptors[26]

[edit] Inverse agonists

  • SB-228,357: mixed 5-HT2C inverse agonist / 5-HT2B antagonist
  • SB-243,213: selective 5-HT2C inverse agonist

[edit] Mixed response

[edit] Interactions

5-HT2C receptor has been shown to interact with MPDZ.[29][30]

[edit] See also

[edit] References

  1. ^ Stam NJ, Vanderheyden P, van Alebeek C, Klomp J, de Boer T, van Delft AM, Olijve W (November 1994). "Genomic organisation and functional expression of the gene encoding the human serotonin 5-HT2C receptor". Eur. J. Pharmacol. 269 (3): 339–48. doi:10.1016/0922-4106(94)90042-6. PMID 7895773. 
  2. ^ Heisler LK, Zhou L, Bajwa P, Hsu J, Tecott LH (July 2007). "Serotonin 5-HT2C receptors regulate anxiety-like behavior". Genes, Brain and Behavior 6 (5): 491–6. doi:10.1111/j.1601-183X.2007.00316.x. PMID 17451451. 
  3. ^ Speake T, Kibble JD, Brown PD (March 2004). "Kv1.1 and Kv1.3 channels contribute to the delayed-rectifying K+ conductance in rat choroid plexus epithelial cells". Am. J. Physiol., Cell Physiol. 286 (3): C611–20. doi:10.1152/ajpcell.00292.2003. PMID 14602579. 
  4. ^ Alex KD, Yavanian GJ, McFarlane HG, Pluto CP, Pehek EA (March 2005). "Modulation of dopamine release by striatal 5-HT2C receptors". Synapse 55 (4): 242–51. doi:10.1002/syn.20109. PMID 15668911. 
  5. ^ Niswender, C.M.; Herrick-davis, K.; Dilley, G.E.; Meltzer, H.Y.; Overholser, J.C.; Stockmeier, C.A.; Emeson, R.B.; Sanders-bush, E. (2001), "RNA editing of the human serotonin 5-HT2C receptor. alterations in suicide and implications for serotonergic pharmacotherapy", Neuropsychopharmacology 24 (5): 478–91, PMID 11282248 
  6. ^ a b Ni YG, Miledi R. (1997). "Blockage of 5HT2C serotonin receptors by fluoxetine (Prozac).". Proc Natl Acad Sci USA 94 (5): 2036–40. doi:10.1073/pnas.94.5.2036. PMID 9050900. 
  7. ^ Esposito E (February 2006). "Serotonin-dopamine interaction as a focus of novel antidepressant drugs". Curr Drug Targets 7 (2): 177–85. doi:10.2174/138945006775515455. PMID 16475959. 
  8. ^ Bubar MJ, Cunningham KA (2006). "Serotonin 5-HT2A and 5-HT2C receptors as potential targets for modulation of psychostimulant use and dependence". Curr Top Med Chem 6 (18): 1971–85. PMID 17017968. 
  9. ^ Gray JA, Roth BL (November 2001). "Paradoxical trafficking and regulation of 5-HT2A receptors by agonists and antagonists". Brain Res. Bull. 56 (5): 441–51. doi:10.1016/S0361-9230(01)00623-2. PMID 11750789. 
  10. ^ Hackler EA, Turner GH, Gresch PJ, Sengupta S, Deutch AY, Avison MJ, Gore JC, Sanders-Bush E (2007). "5-Hydroxytryptamine2C receptor contribution to m-chlorophenylpiperazine and N-methyl-beta-carboline-3-carboxamide-induced anxiety-like behavior and limbic brain activation". J. Pharmacol. Exp. Ther. 320 (3): 1023–9. doi:10.1124/jpet.106.113357. PMID 17138863. 
  11. ^ Higgins GA, Ouagazzal AM, Grottick AJ (2001). "Influence of the 5-HT(2C) receptor antagonist SB242,084 on behaviour produced by the 5-HT2 agonist Ro60-0175 and the indirect 5-HT agonist dexfenfluramine". Br. J. Pharmacol. 133 (4): 459–66. doi:10.1038/sj.bjp.0704082. PMID 11399662. 
  12. ^ Lacivita E, Leopoldo M (2006). "Selective agents for serotonin 2C (5-HT2C) receptor". Curr Top Med Chem 6 (18): 1927–70. doi:10.2174/156802606778522168. PMID 17017967. 
  13. ^ Thomsen WJ, Grottick AJ, Menzaghi F, Reyes-Saldana H, Espitia S, Yuskin D, Whelan K, Martin M, Morgan M, Chen W, Al-Shama H, Smith B, Chalmers D, Behan D (2008). "Lorcaserin, A Novel Selective Human 5-HT2C Agonist: In Vitro and In Vivo Pharmacological Characterization". J. Pharmacol. Exp. Ther. 325: 577. doi:10.1124/jpet.107.133348. PMID 18252809. 
  14. ^ Smith BM, Smith JM, Tsai JH, Schultz JA, Gilson CA, Estrada SA, Chen RR, Park DM, Prieto EB, Gallardo CS, Sengupta D, Thomsen WJ, Saldana HR, Whelan KT, Menzaghi F, Webb RR, Beeley NR (2005). "Discovery and SAR of new benzazepines as potent and selective 5-HT2C receptor agonists for the treatment of obesity". Bioorg. Med. Chem. Lett. 15 (5): 1467–70. doi:10.1016/j.bmcl.2004.12.080. PMID 15713408. 
  15. ^ Lam DD, Przydzial MJ, Ridley SH, Yeo GS, Rochford JJ, O'Rahilly S, Heisler LK (2008). "Serotonin 5-HT2C Receptor Agonist Promotes Hypophagia via Downstream Activation of Melanocortin 4 Receptors". Endocrinology 149 (3): 1323–8. doi:10.1210/en.2007-1321. PMID 18039773. 
  16. ^ Garfield AS, Heisler LK (January 2009). "Pharmacological targeting of the serotonergic system for the treatment of obesity". J. Physiol. (Lond.) 587 (Pt 1): 49–60. doi:10.1113/jphysiol.2008.164152. PMID 19029184. 
  17. ^ Sabb AL, Vogel RL, Welmaker GS, Sabalski JE, Coupet J, Dunlop J, Rosenzweig-Lipson S, Harrison B. Cycloalkyl[b][1,4]benzodiazepinoindoles are agonists at the human 5-HT2C receptor. Bioorganic and Medicinal Chemistry Letters. 2004 May 17;14(10):2603-7. PMID 15109661
  18. ^ Kimura Y, Hatanaka K, Naitou Y, Maeno K, Shimada I, Koakutsu A, Wanibuchi F, Yamaguchi T (2004). "Pharmacological profile of YM348, a novel, potent and orally active 5-HT2C receptor agonist". Eur. J. Pharmacol. 483 (1): 37–43. doi:10.1016/j.ejphar.2003.10.004. PMID 14709324. 
  19. ^ Shimada I, Maeno K, Kazuta K, Kubota H, Kimizuka T, Kimura Y, Hatanaka K, Naitou Y, Wanibuchi F, Sakamoto S, Tsukamoto S (2008). "Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists". Bioorg. Med. Chem. 16 (4): 1966–82. doi:10.1016/j.bmc.2007.10.100. PMID 18035544. 
  20. ^ Richter HG, Adams DR, Benardeau A, Bickerdike MJ, Bentley JM, Blench TJ, Cliffe IA, Dourish C, Hebeisen P, Kennett GA, Knight AR, Malcolm CS, Mattei P, Misra A, Mizrahi J, Monck NJ, Plancher JM, Roever S, Roffey JR, Taylor S, Vickers SP (2006). "Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT2C receptor agonists". Bioorg. Med. Chem. Lett. 16 (5): 1207–11. doi:10.1016/j.bmcl.2005.11.083. PMID 16361098. 
  21. ^ Wacker DA, Varnes JG, Malmstrom SE, Cao X, Hung CP, Ung T, Wu G, Zhang G, Zuvich E, Thomas MA, Keim WJ, Cullen MJ, Rohrbach KW, Qu Q, Narayanan R, Rossi K, Janovitz E, Lehman-McKeeman L, Malley MF, Devenny J, Pelleymounter MA, Miller KJ, Robl JA (2007). "Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a selective, orally active agonist of the 5-HT2C receptor". J. Med. Chem. 50 (6): 1365–79. doi:10.1021/jm0612968. PMID 17315987. 
  22. ^ Wu J, Li Q, Bezprozvanny I (2008). "Evaluation of Dimebon in cellular model of Huntington's disease". Mol Neurodegener 3: 15. doi:10.1186/1750-1326-3-15. PMID 18939977. 
  23. ^ Harada K, Aota M, Inoue T, Matsuda R, Mihara T, Yamaji T, Ishibashi K, Matsuoka N (2006). "Anxiolytic activity of a novel potent serotonin 5-HT2C receptor antagonist FR260010: a comparison with diazepam and buspirone". Eur. J. Pharmacol. 553 (1-3): 171–84. doi:10.1016/j.ejphar.2006.09.042. PMID 17074317. 
  24. ^ Bonhaus DW, Weinhardt KK, Taylor M, DeSouza A, McNeeley PM, Szczepanski K, Fontana DJ, Trinh J, Rocha CL, Dawson MW, Flippin LA, Eglen RM (1997). "RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist". Neuropharmacology 36 (4-5): 621–9. doi:10.1016/S0028-3908(97)00049-X. PMID 9225287. 
  25. ^ Bromidge SM, Duckworth M, Forbes IT, Ham P, King FD, Thewlis KM, Blaney FE, Naylor CB, Blackburn TP, Kennett GA, Wood MD, Clarke SE (October 1997). "6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]- indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist". J. Med. Chem. 40 (22): 3494–6. doi:10.1021/jm970424c. PMID 9357513. 
  26. ^ Park CM, Kim SY, Park WK, Park NS, Seong CM (2008). "Synthesis and structure-activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: a novel series of 5-HT2C receptor antagonists". Bioorg. Med. Chem. Lett. 18 (14): 3844–7. doi:10.1016/j.bmcl.2008.06.064. PMID 18602261. 
  27. ^ Wood MD, Reavill C, Trail B, Wilson A, Stean T, Kennett GA, Lightowler S, Blackburn TP, Thomas D, Gager TL, Riley G, Holland V, Bromidge SM, Forbes IT, Middlemiss DN (2001). "SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety". Neuropharmacology 41 (2): 186–99. doi:10.1016/S0028-3908(01)00054-5. PMID 11489455. 
  28. ^ Berg KA, Navailles S, Sanchez TA, Silva YM, Wood MD, Spampinato U, Clarke WP (2006). "Differential effects of 5-methyl-1-{[2-[(2-methyl-3-pyridyl)oxyl]-5-pyridyl]carbamoyl}-6-trifluoromethylindone (SB 243213) on 5-hydroxytryptamine (2C) receptor-mediated responses". J. Pharmacol. Exp. Ther. 319 (1): 260–8. doi:10.1124/jpet.106.104448. PMID 16807362. 
  29. ^ Becamel, C; Figge A, Poliak S, Dumuis A, Peles E, Bockaert J, Lubbert H, Ullmer C (Apr. 2001). "Interaction of serotonin 5-hydroxytryptamine type 2C receptors with PDZ10 of the multi-PDZ domain protein MUPP1". J. Biol. Chem. (United States) 276 (16): 12974–82. doi:10.1074/jbc.M008089200. ISSN 0021-9258. PMID 11150294. 
  30. ^ Ullmer, C; Schmuck K, Figge A, Lübbert H (Mar. 1998). "Cloning and characterization of MUPP1, a novel PDZ domain protein". FEBS Lett. (NETHERLANDS) 424 (1-2): 63–8. ISSN 0014-5793. PMID 9537516. 

[edit] Further reading

  • Niswender CM, Sanders-Bush E, Emeson RB (1999). "Identification and characterization of RNA editing events within the 5-HT2C receptor.". Ann. N. Y. Acad. Sci. 861: 38–48. doi:10.1111/j.1749-6632.1998.tb10171.x. PMID 9928237. 
  • Hoyer D, Hannon JP, Martin GR (2002). "Molecular, pharmacological and functional diversity of 5-HT receptors.". Pharmacol. Biochem. Behav. 71 (4): 533–54. doi:10.1016/S0091-3057(01)00746-8. PMID 11888546. 
  • Raymond JR, Mukhin YV, Gelasco A, et al. (2002). "Multiplicity of mechanisms of serotonin receptor signal transduction.". Pharmacol. Ther. 92 (2-3): 179–212. doi:10.1016/S0163-7258(01)00169-3. PMID 11916537. 
  • Van Oekelen D, Luyten WH, Leysen JE (2003). "5-HT2A and 5-HT2C receptors and their atypical regulation properties.". Life Sci. 72 (22): 2429–49. doi:10.1016/S0024-3205(03)00141-3. PMID 12650852. 
  • Reynolds GP, Templeman LA, Zhang ZJ (2005). "The role of 5-HT2C receptor polymorphisms in the pharmacogenetics of antipsychotic drug treatment.". Prog. Neuropsychopharmacol. Biol. Psychiatry 29 (6): 1021–8. doi:10.1016/j.pnpbp.2005.03.019. PMID 15953671. 
  • Millan MJ (2006). "Serotonin 5-HT2C receptors as a target for the treatment of depressive and anxious states: focus on novel therapeutic strategies.". Therapie 60 (5): 441–60. PMID 16433010. 
  • Milatovich A, Hsieh CL, Bonaminio G, et al. (1993). "Serotonin receptor 1c gene assigned to X chromosome in human (band q24) and mouse (bands D-F4).". Hum. Mol. Genet. 1 (9): 681–4. doi:10.1093/hmg/1.9.681. PMID 1302605. 
  • Saltzman AG, Morse B, Whitman MM, et al. (1992). "Cloning of the human serotonin 5-HT2 and 5-HT1C receptor subtypes.". Biochem. Biophys. Res. Commun. 181 (3): 1469–78. doi:10.1016/0006-291X(91)92105-S. PMID 1722404. 
  • Lappalainen J, Zhang L, Dean M, et al. (1995). "Identification, expression, and pharmacology of a Cys23-Ser23 substitution in the human 5-HT2c receptor gene (HTR2C).". Genomics 27 (2): 274–9. doi:10.1006/geno.1995.1042. PMID 7557992. 
  • Tecott LH, Sun LM, Akana SF, et al. (1995). "Eating disorder and epilepsy in mice lacking 5-HT2c serotonin receptors.". Nature 374 (6522): 542–6. doi:10.1038/374542a0. PMID 7700379. 
  • Stam NJ, Vanderheyden P, van Alebeek C, et al. (1995). "Genomic organisation and functional expression of the gene encoding the human serotonin 5-HT2C receptor.". Eur. J. Pharmacol. 269 (3): 339–48. PMID 7895773. 
  • Xie E, Zhu L, Zhao L, Chang LS (1996). "The human serotonin 5-HT2C receptor: complete cDNA, genomic structure, and alternatively spliced variant.". Genomics 35 (3): 551–61. doi:10.1006/geno.1996.0397. PMID 8812491. 
  • Burns CM, Chu H, Rueter SM, et al. (1997). "Regulation of serotonin-2C receptor G-protein coupling by RNA editing.". Nature 387 (6630): 303–8. doi:10.1038/387303a0. PMID 9153397. 
  • Brennan TJ, Seeley WW, Kilgard M, et al. (1997). "Sound-induced seizures in serotonin 5-HT2c receptor mutant mice.". Nat. Genet. 16 (4): 387–90. doi:10.1038/ng0897-387. PMID 9241279. 
  • Ullmer C, Schmuck K, Figge A, Lübbert H (1998). "Cloning and characterization of MUPP1, a novel PDZ domain protein.". FEBS Lett. 424 (1-2): 63–8. doi:10.1016/S0014-5793(98)00141-0. PMID 9537516. 
  • Samochowiec J, Smolka M, Winterer G, et al. (1999). "Association analysis between a Cys23Ser substitution polymorphism of the human 5-HT2c receptor gene and neuronal hyperexcitability.". Am. J. Med. Genet. 88 (2): 126–30. doi:10.1002/(SICI)1096-8628(19990416)88:2<126::AID-AJMG6>3.0.CO;2-M. PMID 10206230. 
  • Cargill M, Altshuler D, Ireland J, et al. (1999). "Characterization of single-nucleotide polymorphisms in coding regions of human genes.". Nat. Genet. 22 (3): 231–8. doi:10.1038/10290. PMID 10391209. 
  • Marshall SE, Bird TG, Hart K, Welsh KI (2000). "Unified approach to the analysis of genetic variation in serotonergic pathways.". Am. J. Med. Genet. 88 (6): 621–7. doi:10.1002/(SICI)1096-8628(19991215)88:6<621::AID-AJMG9>3.0.CO;2-H. PMID 10581480. 
  • Backstrom JR, Price RD, Reasoner DT, Sanders-Bush E (2000). "Deletion of the serotonin 5-HT2C receptor PDZ recognition motif prevents receptor phosphorylation and delays resensitization of receptor responses.". J. Biol. Chem. 275 (31): 23620–6. doi:10.1074/jbc.M000922200. PMID 10816555. 

This article incorporates text from the United States National Library of Medicine, which is in the public domain.


v • d • e
Transmembrane receptor: G protein-coupled receptors
Class A: Rhodopsin like
α1 (A, B, D) · α2 (A, B, C) · β1 · β2 · β3
CysLT (1, 2) · LTB4 (1, 2) · FPRL1 · OXE · Prostaglandin (DP (1, 2), EP (1, 2, 3, 4), FP) · Prostacyclin · Thromboxane
B/W (1, 2) · FF (1, 2) · S · Y (1, 2, 4, 5) · Neuromedin (B, U (1, 2)) · Neurotensin (1, 2)
GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 82, 83, 84, 85, 87, 88, 92, 101, 103, 109A, 109B, 119, 120, 132, 135, 137B, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 173, 174, 176, 177, 182)
Adenosine (A1, A2A, A2B, A3) · P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(all but 5-HT3) 5-HT1 (A, B, D, E, F) · 5-HT2 (A, B, C) · 5-HT (4, 5A, 6, 7)
Other
Acetylcholine (M1, M2, M3, M4, M5) · Adrenomedullin · Anaphylatoxin (C3a, C5a) · Angiotensin (1, 2) · Apelin · Bile acid · Bombesin (BRS3, GRPR, NMBR) · Bradykinin (B1, B2) · Cannabinoid (CB1, CB2) · Chemokine · Cholecystokinin (A, B) · Dopamine (D1, D2, D3, D4, D5) · EBI2 · Endothelin (A, B) · Estrogen · Formyl peptide (1, 2, 3) · Free fatty acid (1, 2, 3, 4) · FSH · Galanin (1, 2, 3) · Gonadotropin-releasing hormone (1, 2) · GHB receptor · Ghrelin · Histamine (H1, H2, H3, H4) · Kisspeptin · Luteinizing hormone/choriogonadotropin · lysophosphatidic acid (1, 2, 3)  · Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) · MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) · Melanocortin (1, 2, 3, 4, 5) · MCHR (1, 2) · Melatonin (1A, 1B, 1C) · Niacin (1, 2) · Motilin · Opioid (Delta, Kappa, Mu, Nociceptin & Zeta, but not Sigma) · Olfactory · Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) · Orexin (1, 2) · Oxytocin · Oxoglutarate · PAF · Prokineticin (1, 2) · Prolactin-releasing peptide · Protease-activated (1, 2, 3, 4) · Relaxin (1, 2, 3, 4) · Somatostatin (1, 2, 3, 4, 5) · Sphingosine-1-phosphate (1, 2, 3, 4, 5) · SREB · Succinate · TAAR (1, 2, 3, 5, 6, 8, 9) · Tachykinin (1, 2, 3) · Thyrotropin · Thyrotropin-releasing hormone · Urotensin-II · Vasopressin (1A, 1B, 2)
Class B: Secretin like
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157)
Other
Class C: Metabotropic
glutamate / pheromone
TAS1R (1, 2, 3) · TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50)
Other
Frizzled / Smoothened
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) · Smoothened
v • d • e
Cell signaling
Key concepts
Processes
Signaling pathways
Agents
Other
v • d • e
Serotonergics
Receptor
ligands

Agonists: Azapirones: Alnespirone • Binospirone • Buspirone • Eptapirone • Gepirone • Ipsapirone • Perospirone • Tandospirone • Tiospirone • Zalospirone; Lysergamides: Dihydroergotamine • Ergotamine • Methysergide • LSD; Piperazines: Eltoprazine • Flesinoxan • Flibanserin; Tryptamines: 5-CT • 5-MeO-DMT • 5-MT • DMT • Psilocin • Psilocybin • Rauwolscine • Yohimbine; Atypical Antipsychotics: Aripiprazole • Asenapine • Clozapine • Quetiapine • Ziprasidone; Others: 8-OH-DPAT • Befiradol • F-11440 • Lesopitron • Lu AA21004 • LY-293,284 • LY-301,317 • MKC-242 • Osemozotan • Piclozotan • PRX-00023 • Repinotan • RU-24969 • S-15535 • Sarizotan • SSR-181,507 • Sunepitron • U-92016A • Urapidil • Vilazodone • Xaliproden
Antagonists: Beta Blockers: Alprenolol • Cyanopindolol • Iodocyanopindolol • Oxprenolol • Pindobind • Pindolol • Propranolol; Piperazines: Nefazodone • Trazodone • WAY-100,135 • WAY-100,635; Others: AV965 • BMY-7378 • Dotarizine • GR-46611 • Isamoltane • Lecozotan • Methiothepin • MPPF • NAN-190 • Robalzotan • S-15535 • SB-649915 • SDZ 216-525 • Spiperone • Spiramide • Spiroxatrine • UH-301 • WAY-100,135 •

WAY-100,635 • Xylamidine
Agonists: Lysergamides: Dihydroergotamine • Ergotamine • Methysergide; Piperazines: Eltoprazine • TFMPP; Triptans: Eletriptan • Sumatriptan • Zolmitriptan; Tryptamines: 5-CT • 5-MT; Others: CGS-12066A • CP-93,129 • CP-94,253 • CP-135,807 • RU-24969
Antagonists: Lysergamides: Metergoline • Methiothepin; Tryptamines: Yohimbine; Others: AR-A000002 • GR-127,935 • Isamoltane • SB-216,641 • SB-224,289 • SB-236,057
Agonists: Lysergamides: Dihydroergotamine • Methysergide; Triptans: Almotriptan • Eletriptan • Frovatriptan • Naratriptan • Rizatriptan • Sumatriptan • Zolmitriptan; Tryptamines: 5-CT • 5-MT; Others: CP-135,807 • CP-286,601 • GR-46611 • L-694,247 • L-772,405 • PNU-109,291 • PNU-142,633
Antagonists: Lysergamides: Metergoline • Methiothepin; Tryptamines: Rauwolscine • Yohimbine; Others: Alniditan BRL-15572 • GR-127,935 • Ketanserin • LY-310,762 • LY-367,642 • LY-456,219 • LY-456,220 • Ritanserin • Ziprasidone
Agonists: Lysergamides: Methysergide; Triptans: Eletriptan; Tryptamines: Tryptamine
Antagonists: Methiothepin
Agonists: Triptans: Eletriptan • Naratriptan • Sumatriptan; Tryptamines: 5-MT; Others: LY-334,370
Antagonists: Methiothepin
Agonists: Lysergamides: ALD-52 • Ergonovine • Lisuride • LA-SS-Az • LSD • Lysergic acid 2-butyl amide • Methysergide; Phenethylamines: 25I-NBMD • 25I-NBOH • 25I-NBOMe • 2C-B • 2C-B-FLY • 2C-E • 2C-I • 2C-T-2 • 2C-T-7 • 2C-T-21 • 2CBCB-NBOMe • 2CBFly-NBOMe • Bromo-DragonFLY • DOB • DOC • DOI • DOM • MDA • MDMA • Mescaline • Myristicin • TCB-2 • TFMFly; Piperazines: BZP • Quipazine • TFMPP; Tryptamines: 5-CT • 5-MeO-α-ET • 5-MeO-α-MT • 5-MeO-DET • 5-MeO-DiPT • 5-MeO-DMT • 5-MeO-DPT • 5-MT • α-ET • α-Methyl-5-HT • α-MT • Bufotenin • DET • DiPT • DMT • DPT • Psilocin • Psilocybin; Others: AL-34662 • AL-37350A • PNU-22394
Antagonists: Atypical Antipsychotics: Amperozide • Aripiprazole • Clozapine • Iloperidone • Melperone • Olanzapine • Paliperidone • Pimozide • Quetiapine • Risperidone • Sertindole • Ziprasidone • Zotepine; Typical Antipsychotics: Loxapine • Pipamperone; Antidepressants: Amitriptyline • Amoxapine • Etoperidone • Mianserin • Mirtazapine • Nefazodone • Trazodone; Others: 5-I-R91150 • AC-90179 • Altanserin • AMDA • APD-215 • Blonanserin • Cinanserin • Cyproheptadine • Deramciclane • Dotarizine • Eplivanserin • Fananserin • Flibanserin • Ketanserin • KML-010 • Lubazodone • Methiothepin • Nantenine • Pimavanserin • Pizotifen • Ritanserin • Sarpogrelate • Setoperone • Spiperone • Spiramide • SR-46349B • Volinanserin • Xylamidine • Yohimbine
Agonists: Oxazolines: 4-Methylaminorex • Aminorex; Phenethylamines: Chlorphentermine • DOB • DOC • DOI • DOM • Fenfluramine • MDA • MDMA • Norfenfluramine; Tryptamines: 5-CT • 5-MT • α-Methyl-5-HT; Others: BW-723C86 • Cabergoline • mCPP • Pergolide • PNU-22394 • Ro60-0175
Antagonists: Agomelatine • Asenapine • EGIS-7625 • Ketanserin • Lisuride • LY-272,015 • Rauwolscine • Ritanserin • RS-127,445 • Sarpogrelate • SB-200,646 • SB-204,741 • SB-206,553 • SB-215,505 • SB-221,284 • SB-228,357 • SDZ SER-082 • Tegaserod • Yohimbine
Agonists: Phenethylamines: 2C-B • 2C-E • 2C-I • 2C-T-2 • 2C-T-7 • 2C-T-21 • DOB • DOC • DOI • DOM • MDA • MDMA • Mescaline • Myristicin; Piperazines: Aripiprazole • mCPP • TFMPP; Tryptamines: 5-CT • 5-MeO-α-ET • 5-MeO-α-MT • 5-MeO-DET • 5-MeO-DiPT • 5-MeO-DMT • 5-MeO-DPT • 5-MT • α-ET • α-Methyl-5-HT • α-MT • Bufotenin • DET • DiPT • DMT • DPT • Psilocin • Psilocybin; Others: A-372,159 • AL-38022A • CP-809,101 • Lorcaserin • MK-212 • Org 37684 • PNU-22394 • Ro60-0175 • Vabicaserin • WAY-629 • WAY-161,503 • YM-348
Antagonists: Atypical Antipsychotics: Clozapine • Iloperidone • Melperone • Olanzapine • Paliperidone • Pimozide • Quetiapine • Risperidone • Sertindole • Ziprasidone • Zotepine; Typical Antipsychotics: Chlorpromazine • Loxapine • Pipamperone; Antidepressants: Agomelatine • Amitriptyline • Amoxapine • Etoperidone • Fluoxetine • Mianserin • Mirtazapine • Nefazodone • Nortriptyline • Trazodone; Others: Cinanserin • Cyproheptadine • Deramciclane • Dimebolin • Dotarizine • Eltoprazine • FR-260,010 • Ketanserin • Ketotifen • Methysergide • Pizotifen • Ritanserin • RS-102,221 • SB-200,646 • SB-206,553 • SB-221,284 • SB-228,357 • SB-242,084 • SB-243,213 • SDZ SER-082 • Xylamidine
Agonists: Piperazines: BZP • Quipazine; Tryptamines: 2-Methyl-5-HT • 5-CT; Others: Chlorophenylbiguanide • RS-56812 • SR-57,227 • SR-57,227-A • YM-31636
Antagonists: Antiemetics: AS-8112 • Alosetron • Azasetron • Batanopride • Bemesetron • Cilansetron • Dolasetron • Granisetron • Lerisetron • Ondansetron • Palonosetron • Ramosetron • Renzapride • Tropisetron • Zacopride • Zatosetron; Atypical Antipsychotics: Clozapine • Olanzapine • Quetiapine; Tetracyclic Antidepressants: Amoxapine • Mianserin • Mirtazapine; Others: ICS-205,930 • Lu AA21004 • MDL-72,222 • Memantine • Ricasetron
Agonists: Gastroprokinetic Agents: Cisapride • Metoclopramide • Mosapride • Prucalopride • Renzapride • Tegaserod • Zacopride; Others: 5-MT • BIMU-8 • CJ-033,466 • PRX-03140 • RS-67333 • RS-67506 • TD-5108
Antagonists: GR-113,808 • GR-125,487 • L-Lysine • Piboserod • RS-39604 • RS-67532 • SB-203,186
Agonists: Lysergamides: Ergotamine • LSD; Tryptamines: 5-CT; Others: Valerenic Acid
Antagonists: Asenapine • Dimebolin • Methiothepin • Ritanserin • SB-699,551
Agonists: Lysergamides: Ergotamine • LSD
Antagonists: Methiothepin
* Note that the 5-HT5B receptor is not functional in humans.
Agonists: Lysergamides: Lisuride • LSD • Metergoline; Tryptamines: 5-CT • 5-MT • E-6801 • E-6837 • EMD-386,088 • EMDT • LY-586,713 • WAY-181,187 • WAY-208,466
Antagonists: Antidepressants: Amitriptyline • Amoxapine • Clomipramine • Doxepin • Mianserin • Nortriptyline; Atypical Antipsychotics: Aripiprazole • Asenapine • Clozapine • Fluperlapine • Iloperidone • Olanzapine • Tiospirone; Typical Antipsychotics: Chlorpromazine • Loxapine; Others: BGC20-760 • BVT-5182 • BVT-74316 • Dimebolin • EGIS-12233 • GW-742,457 • Ketanserin • Methiothepin • MS-245 • PRX-07034 • Ritanserin • Ro 04-6790 • Ro 63-0563 • SB-258,585 • SB-271,046 • SB-357,134 • SB-399,885
Agonists: Lysergamides: LSD; Tryptamines: 5-CT • 5-MT; Others: 8-OH-DPAT • AS-19 • Bifeprunox • LP-12 • LP-44 • Sarizotan
Antagonists: Antidepressants: Amitriptyline • Amoxapine • Clomipramine • Imipramine • Maprotiline • Mianserin; Atypical Antipsychotics: Amisulpride • Aripiprazole • Clozapine • Olanzapine • Risperidone • Sertindole • Tiospirone • Ziprasidone • Zotepine; Typical Antipsychotics: Chlorpromazine • Loxapine; Others: EGIS-12233 • LY-215,840 • Mesulergine • Metergoline • Methiothepin • Pimozide • Ritanserin • SB-258,719 • SB-258,741 • SB-269,970 • SB-656,104 • SB-656,104-A • SB-691,673 • SLV-313 • SLV-314 • Spiperone • SSR-181,507
Reuptake
inhibitors
SERT inhibitors
Selective Serotonin Reuptake Inhibitors (SSRIs): Alaproclate • Citalopram • Dapoxetine • Desmethylcitalopram • Desmethylsertraline • Elzasonan • Escitalopram • Femoxetine • Fluoxetine • Fluvoxamine • Indalpine • Litoxetine • Lubazodone • Norfluoxetine • Paroxetine • RTI-353 • Sertraline • Vilazodone • Zimelidine; Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs): Bicifadine • Desvenlafaxine • Duloxetine • Milnacipran • Venlafaxine; Serotonin-Norepinephrine-Dopamine Reuptake Inhibitors (SNDRIs): Brasofensine • Diclofensine • DOV-102,677 • DOV-21,947 • DOV-216,303 • NS-2359 • SEP-225,289 • SEP-227,162 • Tesofensine; Tricyclic Antidepressants (TCAs): Amitriptyline • Butriptyline • Cianopramine • Clomipramine • Desipramine • Dosulepin • Doxepin • Imipramine • Lofepramine • Nortriptyline • Protriptyline • Trimipramine; Tetracyclic Antidepressants (TeCAs): Amoxapine; Piperazines: Nefazodone • Trazodone; Antihistamines: Brompheniramine • Chlorpheniramine • Diphenhydramine • Mepyramine (Pyrilamine) • Pheniramine • Tripelennamine; Opioids: Meperidine (Pethidine) • Methadone • Propoxyphene • Tramadol; Others: Cocaine • Cyclobenzaprine (CBZ) • Dextromethorphan (DXM) • Mesembrine • Nefopam • SB-649,915 • Sibutramine • Ziprasidone
TRPC6 activators
VMAT Inhibitors
Releasing
agents
Aminoindanes: 5-Iodoaminoindane (5-IAI) • Ethyltrifluoromethylaminoindane (ETAI) • Methylenedioxyaminoindane (MDAI) • Methylenedioxymethylaminoindane (MDMAI) • Methoxymethylaminoindane (MMAI) • Trifluoromethylaminoindane (TAI); Aminotetralins: 6-Chloroaminotetralin (6-CAT) • 8-Hydroxydipropylaminotetralin (8-OH-DPAT) • Methylenedioxyaminotetralin (MDAT); Oxazolines: 4-Methylaminorex (4-MAR, 4-MAX) • Aminorex • Clominorex • Fluminorex; Phenethylamines (also Amphetamines, Cathinones, Phentermines, etc): 4-Methylthioamphetamine (4-MTA) • Benzodioxolylbutanamine (BDB) • Benzodioxolylhydroxybutanamine (BOH) • Brephedrone • Butylone • Chlorphentermine • Diethylcathinone (Diethylpropion, Amfepramone) • Dimethoxyamphetamine (DMA) • Dimethoxymethamphetamine (DMMA) • Dimethylcathinone (Dimethylpropion, Metamfepramone) • Ethylbenzodioxolylbutanamine (EBDB) • Ethylone • Fenfluramine (Dexfenfluramine) • Flephedrone • Lophophine (Homomyristicylamine) • Mephedrone • Methedrone • Methoxymethylamphetamine (MMA) • Methoxymethylenedioxyamphetamine (MMDA) • Methoxymethylenedioxymethamphetamine (MMDMA) • Methylbenzodioxolylbutanamine (MBDB) • Methylenedioxyamphetamine (MDA; Tenamfetamine) • Methylenedioxyethylamphetamine (MDEA) • Methylenedioxyhydroxyamphetamine (MDOH) • Methylenedioxymethamphetamine (MDMA) • Methylenedioxymethylphenethylamine (MDMPEA; Homarylamine) • Methylenedioxyphenethylamine (MDPEA; Homopiperonylamine) • Methylone • Norfenfluramine • Parabromoamphetamine (PBA) • Parachloroamphetamine (PCA) • Parafluoroamphetamine (PFA) • Parafluoromethamphetamine (PFMA) • Parahydroxyamphetamine (PHA) • Paraiodoamphetamine (PIA) • Paramethoxyamphetamine (PMA) • Paramethoxyethylamphetamine (PMEA) • Paramethoxymethamphetamine (PMMA); Piperazines: 2,5-Dimethoxy-4-bromobenzylpiperazine (2C-B-BZP) • Benzylpiperazine (BZP) • Metachlorophenylpiperazine (mCPP) • Methoxyphenylpiperazine (MeOPP; Paraperazine) • Methylbenzylpiperazine (MBZP) • Methylenedioxybenzylpiperazine (MDBZP; Piperonylpiperazine) • Parafluorophenylpiperazine (pFPP; Fluoperazine) • Trifluoromethylphenylpiperazine (TFMPP); Quinolines: PK-7059 • Viqualine; Tryptamines: α-Ethyltryptamine (αET; Etryptamine) • α-Methyltryptamine (αMT; Metryptamine); Others: 5-Aminopropyldihydrobenzofuran (5-APDB; 5-Desoxy-MDA) • Indanylaminopropane (IAP) • Naphthylaminopropane (NAP)
Enzyme
inhibitors
TPH inhibitors
Others
Others
Activity enhancers: Benzofuranylpropylaminopentane (BPAP) • Phenylpropylaminopentane (PPAP); Reuptake enhancers: Tianeptine
v • d • e
Anxiety disorder: Obsessive–compulsive disorder
History
Biology
Neuroanatomy
Receptors
5-HT1Dβ · 5-HT2A · 5-HT2C · μ Opioid · H2 · NK1 · M4 · NMDA · non-NMDA
Symptoms
Treatment
Other
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