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Gene Review

Htr2c  -  5-hydroxytryptamine (serotonin) receptor 2C

Mus musculus

Synonyms: 5-HT-1C, 5-HT-2C, 5-HT1C, 5-HT2C, 5-HT2C receptor, ...
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Disease relevance of Htr2c


Psychiatry related information on Htr2c


High impact information on Htr2c

  • Sound-induced seizures in serotonin 5-HT2c receptor mutant mice [11].
  • Here we show that young adult mice with a targeted mutation of the serotonin 5-HT2C receptor gene consume more food despite normal responses to exogenous leptin administration [2].
  • To address these issues, we have generated mutant mice lacking functional 5-HT2C receptors (previously termed 5-HT1C), prominent G-protein-coupled receptors that are widely expressed throughout the brain and spinal cord and which have been proposed to mediate numerous central nervous system (CNS) actions of serotonin [3].
  • Introduction of functional 5HT1c receptors into NIH 3T3 cells results, at high frequency, in the generation of transformed foci [12].
  • Treatment of mice with fluoxetine alters the pattern of 5-HT2C transcript editing in the direction opposite that observed for suicide victims [13].

Biological context of Htr2c


Anatomical context of Htr2c


Associations of Htr2c with chemical compounds

  • Our present data indicate that the 5-HT2C receptor antagonist RS102221 suppresses MDMA-induced hyperlocomotion [21].
  • The electroencephalography defined sleep-waking pattern in rats produced by these two 5-HT2C agonists, as well as fluoxetine, included increased quiet-waking and decreased rapid-eye-movement sleep, which is characteristic of antidepressant drugs [7].
  • These results also confirm that 5-HT1B-R activation alone cannot account for the hyperactive response of 5-HT2C KO mice to mCPP [22].
  • In vitro, (S)-2-(chloro-5-fluoro-indol-1-yl)-1-methylethylamine 1:1 C4H4O4 and (S)-2-(4,4,7-trimethyl-1,4-dihydro-indeno[1, 2-b]pyrrol-1-yl)-1-methylethylamine 1:1 C4H4O4 exhibited high-affinity binding to the serotonin2C (5HT2C) receptors and stimulated turnover of inositol 1,4,5-triphosphate [7].
  • However, the combination of Ro 60-0175 with CP-94,253 induced a substantial increase in activity in 5-HT2C KO mice, an effect comparable to mCPP-induced hyperactivity [23].

Physical interactions of Htr2c

  • In particular, the hypolocomotion produced by m-CPP has been suggested to be mediated by 5-HT2C receptors. m-CPP binds with high affinity to 5-HT1 as well as 5-HT2 receptors, thus effects of m-CPP on locomotor activity may be due to the physiologic summation of the actions of m-CPP at 5-HT1 as well as 5-HT2 receptors [24].
  • Estimates of 5-HT2C receptor binding were similar in 5-HT1B KO and WT mice [25].
  • The reassociation of the 4-5 S receptor to form the 8 S complex is inhibited by RNase [26].

Regulatory relationships of Htr2c

  • In the present group of experiments, we evaluate the role of 5-HT1A, 5-HT1B and 5-HT2A receptors in mCPP-induced hyperactivity in 5-HT2C KO mice [23].
  • In contrast, a 4 d treatment with the 5-HT2A/2C agonist (+/-)-1-(4-iodo-2,5-dimethoxyphenyl)-2-aminopropane significantly increases the editing frequency at the C' site and leads to increased expression of 5-HT2C mRNA isoforms encoding receptors that activate G-protein least efficiently [27].

Other interactions of Htr2c

  • 5-HT2cR mutant mice develop a late-onset obesity that is associated with higher plasma leptin levels [28].
  • Finally, 5-MeO-DIPT had micromolar affinity for 5-HT 2A and 5-HT 2C receptors, but much higher affinity for 5-HT 1A receptors [29].
  • The effects of paroxetine (8 mg/kg) were not reversed by the selective 5-HT2C receptor antagonist, RS 10-2221 (0.1 mg/kg and 1 mg/kg) or the selective 5-HT2B/2C receptor antagonist SB 206553 (0.1 mg/kg and 1 mg/kg), at doses which lack an effect when administered alone [30].
  • Global increases in seizure susceptibility in mice lacking 5-HT2C receptors: a behavioral analysis [4].
  • Preincubation of cells with PTX showed that the G protein coupling of the 5-HT2C receptor to phospholipase C is PTX insensitive, while the G protein coupling to inhibition of adenylyl cyclase is PTX sensitive, even to concentrations as low as 20 ng/ml of PTX [31].

Analytical, diagnostic and therapeutic context of Htr2c

  • The obtained results suggest that the analgesia induced by m-CPP is mediated by 5-HT2C receptors [32].
  • Furthermore, primers specific for the rat 5HT1C receptor sequence did not detect significant levels of receptor mRNA in rat fundus, although the target sequence was amplified a minimum of 10(5)-fold in a polymerase chain reaction [33].
  • Here, we briefly describe the techniques of random transgene insertion and gene targeting and discuss how these methods were used to generate the epileptic jerky and 5-hydroxytryptamine (5-HT2C) receptor deficient mice [34].
  • Single cell RT-PCR profiling revealed that the vast majority of pyramidal neurons expressed detectable levels of 5-HT2a and/or 5-HT2c receptor mRNA with half of the cells expressing both mRNAs [35].
  • To show that the polypeptides detected on western blots and by immunoprecipitation represent the 5-HT2C receptor, binding studies of the 5-HT2C ligand [3H]-mesulergine to immunoprecipitates from extracts of pig choroid plexus were performed [36].


  1. Hyperphagia Alters Expression of Hypothalamic 5-HT2C and 5-HT1B Receptor Genes and Plasma Des-Acyl Ghrelin Levels in Ay Mice. Nonogaki, K., Nozue, K., Oka, Y. Endocrinology (2006) [Pubmed]
  2. Leptin-independent hyperphagia and type 2 diabetes in mice with a mutated serotonin 5-HT2C receptor gene. Nonogaki, K., Strack, A.M., Dallman, M.F., Tecott, L.H. Nat. Med. (1998) [Pubmed]
  3. Eating disorder and epilepsy in mice lacking 5-HT2c serotonin receptors. Tecott, L.H., Sun, L.M., Akana, S.F., Strack, A.M., Lowenstein, D.H., Dallman, M.F., Julius, D. Nature (1995) [Pubmed]
  4. Global increases in seizure susceptibility in mice lacking 5-HT2C receptors: a behavioral analysis. Applegate, C.D., Tecott, L.H. Exp. Neurol. (1998) [Pubmed]
  5. Role of nitric oxide on motor behavior. Del Bel, E.A., Guimarães, F.S., Bermúdez-Echeverry, M., Gomes, M.Z., Schiaveto-de-souza, A., Padovan-Neto, F.E., Tumas, V., Barion-Cavalcanti, A.P., Lazzarini, M., Nucci-da-Silva, L.P., de Paula-Souza, D. Cell. Mol. Neurobiol. (2005) [Pubmed]
  6. 5-HT1B receptor knockout mice show a compensatory reduction in 5-HT2C receptor function. Clifton, P.G., Lee, M.D., Somerville, E.M., Kennett, G.A., Dourish, C.T. Eur. J. Neurosci. (2003) [Pubmed]
  7. 5-HT2C receptor agonists: pharmacological characteristics and therapeutic potential. Martin, J.R., Bös, M., Jenck, F., Moreau, J., Mutel, V., Sleight, A.J., Wichmann, J., Andrews, J.S., Berendsen, H.H., Broekkamp, C.L., Ruigt, G.S., Köhler, C., Delft, A.M. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  8. Dysregulation of diurnal rhythms of serotonin 5-HT2C and corticosteroid receptor gene expression in the hippocampus with food restriction and glucocorticoids. Holmes, M.C., French, K.L., Seckl, J.R. J. Neurosci. (1997) [Pubmed]
  9. Sleep and sleep homeostasis in mice lacking the 5-HT2c receptor. Frank, M.G., Stryker, M.P., Tecott, L.H. Neuropsychopharmacology (2002) [Pubmed]
  10. Compulsive behavior in the 5-HT2C receptor knockout mouse. Chou-Green, J.M., Holscher, T.D., Dallman, M.F., Akana, S.F. Physiol. Behav. (2003) [Pubmed]
  11. Sound-induced seizures in serotonin 5-HT2c receptor mutant mice. Brennan, T.J., Seeley, W.W., Kilgard, M., Schreiner, C.E., Tecott, L.H. Nat. Genet. (1997) [Pubmed]
  12. Ectopic expression of the serotonin 1c receptor and the triggering of malignant transformation. Julius, D., Livelli, T.J., Jessell, T.M., Axel, R. Science (1989) [Pubmed]
  13. And now, transcriptomics. Garlow, S.J. Neuron (2002) [Pubmed]
  14. Agonist-induced phosphorylation of the serotonin 5-HT2C receptor regulates its interaction with multiple PDZ protein 1. Parker, L.L., Backstrom, J.R., Sanders-Bush, E., Shieh, B.H. J. Biol. Chem. (2003) [Pubmed]
  15. Endogenous serotonin-2A and -2C receptors in Balb/c-3T3 cells revealed in serotonin-free medium: desensitization and down-regulation by serotonin. Saucier, C., Morris, S.J., Albert, P.R. Biochem. Pharmacol. (1998) [Pubmed]
  16. 5-HT2A and 5-HT2C serotonin receptors differentially modulate mouse sexual arousal and the hypothalamo-pituitary-testicular response to the presence of a female. Popova, N.K., Amstislavskaya, T.G. Neuroendocrinology (2002) [Pubmed]
  17. Suppressive effects of isorhynchophylline on 5-HT2A receptor function in the brain: behavioural and electrophysiological studies. Matsumoto, K., Morishige, R., Murakami, Y., Tohda, M., Takayama, H., Sakakibara, I., Watanabe, H. Eur. J. Pharmacol. (2005) [Pubmed]
  18. In vivo electrophysiological examination of 5-HT2 responses in 5-HT2C receptor mutant mice. Rueter, L.E., Tecott, L.H., Blier, P. Naunyn Schmiedebergs Arch. Pharmacol. (2000) [Pubmed]
  19. Perturbed dentate gyrus function in serotonin 5-HT2C receptor mutant mice. Tecott, L.H., Logue, S.F., Wehner, J.M., Kauer, J.A. Proc. Natl. Acad. Sci. U.S.A. (1998) [Pubmed]
  20. Serotonin 5-HT2a and 5-HT2c receptors stimulate amyloid precursor protein ectodomain secretion. Nitsch, R.M., Deng, M., Growdon, J.H., Wurtman, R.J. J. Biol. Chem. (1996) [Pubmed]
  21. 3,4-N-methlenedioxymethamphetamine-induced hypophagia is maintained in 5-HT1B receptor knockout mice, but suppressed by the 5-HT2C receptor antagonist RS102221. Conductier, G., Crosson, C., Hen, R., Bockaert, J., Compan, V. Neuropsychopharmacology (2005) [Pubmed]
  22. Serotonin 1B and 2C receptor interactions in the modulation of feeding behaviour in the mouse. Dalton, G.L., Lee, M.D., Kennett, G.A., Dourish, C.T., Clifton, P.G. Psychopharmacology (Berl.) (2006) [Pubmed]
  23. mCPP-induced hyperactivity in 5-HT2C receptor mutant mice is mediated by activation of multiple 5-HT receptor subtypes. Dalton, G.L., Lee, M.D., Kennett, G.A., Dourish, C.T., Clifton, P.G. Neuropharmacology (2004) [Pubmed]
  24. Meta-chlorophenylpiperazine induced changes in locomotor activity are mediated by 5-HT1 as well as 5-HT2C receptors in mice. Gleason, S.D., Shannon, H.E. Eur. J. Pharmacol. (1998) [Pubmed]
  25. Reduced hypophagic effects of d-fenfluramine and the 5-HT2C receptor agonist mCPP in 5-HT1B receptor knockout mice. Lee, M.D., Somerville, E.M., Kennett, G.A., Dourish, C.T., Clifton, P.G. Psychopharmacology (Berl.) (2004) [Pubmed]
  26. Correlation of the 4-5 S form and the 8 S form of the cytosolic androgen receptor in murine skeletal muscle. Haase, A., Ofenloch, B., Eisele, K. Biochem. Int. (1983) [Pubmed]
  27. Modulation of serotonin 2C receptor editing by sustained changes in serotonergic neurotransmission. Gurevich, I., Englander, M.T., Adlersberg, M., Siegal, N.B., Schmauss, C. J. Neurosci. (2002) [Pubmed]
  28. Up-regulation of peroxisome proliferator-activated receptors (PPAR-alpha) and PPAR-gamma messenger ribonucleic acid expression in the liver in murine obesity: troglitazone induces expression of PPAR-gamma-responsive adipose tissue-specific genes in the liver of obese diabetic mice. Memon, R.A., Tecott, L.H., Nonogaki, K., Beigneux, A., Moser, A.H., Grunfeld, C., Feingold, K.R. Endocrinology (2000) [Pubmed]
  29. Hallucinogen-like actions of 5-methoxy-N,N-diisopropyltryptamine in mice and rats. Fantegrossi, W.E., Harrington, A.W., Kiessel, C.L., Eckler, J.R., Rabin, R.A., Winter, J.C., Coop, A., Rice, K.C., Woods, J.H. Pharmacol. Biochem. Behav. (2006) [Pubmed]
  30. Implication of 5-HT2 receptor subtypes in the mechanism of action of antidepressants in the four plates test. Nic Dhonnchadha, B.A., Ripoll, N., Clénet, F., Hascoët, M., Bourin, M. Psychopharmacology (Berl.) (2005) [Pubmed]
  31. Receptor subtype and density determine the coupling repertoire of the 5-HT2 receptor subfamily. Lucaites, V.L., Nelson, D.L., Wainscott, D.B., Baez, M. Life Sci. (1996) [Pubmed]
  32. Involvement of 5-HT2C receptors in the m-CPP-induced antinociception in mice. Chojnacka-Wójcik, E., Kłodzińska, A., Dereń-Wesołek, A. Polish journal of pharmacology. (1994) [Pubmed]
  33. Pharmacological and molecular evidence that the contractile response to serotonin in rat stomach fundus is not mediated by activation of the 5-hydroxytryptamine1C receptor. Baez, M., Yu, L., Cohen, M.L. Mol. Pharmacol. (1990) [Pubmed]
  34. Transgenic approaches to epilepsy. Toth, M., Tecott, L. Advances in neurology. (1999) [Pubmed]
  35. Serotonin receptor activation inhibits sodium current and dendritic excitability in prefrontal cortex via a protein kinase C-dependent mechanism. Carr, D.B., Cooper, D.C., Ulrich, S.L., Spruston, N., Surmeier, D.J. J. Neurosci. (2002) [Pubmed]
  36. Identification of the 5-hydroxytryptamine2C receptor as a 60-kDa N-glycosylated protein in choroid plexus and hippocampus. Abramowski, D., Staufenbiel, M. J. Neurochem. (1995) [Pubmed]
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