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Gene Review

Mchr1  -  melanin-concentrating hormone receptor 1

Mus musculus

Synonyms: AW049955, G-protein coupled receptor 24, Gpr24, Gpr24-9, MCH receptor 1, ...
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Disease relevance of Mchr1

  • Consistent with the hyperactivity, Mch1r-/- mice are less susceptible to diet-induced obesity [1].
  • Mch1r-/- mice have normal body weights, yet are lean and have reduced fat mass [1].
  • Importantly, chronic central infusions of MCH induce hyperphagia and mild obesity in wild-type mice, but not in Mch1r-/- mice [1].
  • Mice carrying a null mutation of the MCHR1 gene display anxiolytic-like behavior across a battery different behavioral paradigms commonly used to assess fear and anxiety responses in rodents: open field, elevated plus maze, social interaction, and stress-induced hyperthermia [2].
  • Administration of the adrenergic antagonist metoprolol completely reversed the tachycardia seen in MCHR1(-/-) mice, suggesting an increased sympathetic tone [3].

Psychiatry related information on Mchr1

  • We conclude that MCH1R is a physiologically relevant MCH receptor in mice that plays a role in energy homeostasis through multiple actions on locomotor activity, metabolism, appetite, and neuroendocrine function [1].
  • This work identifies a novel hypothalamic-AcSh circuit that influences appetitive behavior and mediates the antidepressant activity of MCH1R antagonists [4].
  • CONCLUSION: Taken together, we suggest that antagonism of the MCHR1 receptor may provide a novel approach for the treatment of affective disorders, including depression, with a potentially increased efficacy in women [5].
  • I have focused particularly on recent data concerning transgenic mice and the ongoing development of MC/MCH receptor antagonists/agonists that may represent promising drugs to treat human eating disorders on both sides of the energy balance (anorexia, obesity) [6].

High impact information on Mchr1


Chemical compound and disease context of Mchr1


Biological context of Mchr1


Anatomical context of Mchr1

  • In summary, we show that MCHR1 can modulate stress- and anxiety-like behaviors and suggest that this may be due to changes in serotonergic transmission in forebrain regions [2].
  • Baseline dialysate 5-HT levels were significantly lower in MCHR1 knockout mice as compared with wild-type controls (9.53+/-0.24 fmol for wild types vs 6.91+/-0.36 fmol for knockouts) in the prefrontal cortex (PFC), one of the main target structures of the serotonergic system and one that is highly associated with the control of emotional processes [2].
  • With a high-fat diet, body fat mass is significantly lower in both male (4.7 +/- 0.6 g vs. 9.6 +/- 1.2 g) and female (3.9 +/- 0.2 vs. 5.8 +/- 0.5 g) MCHR1-/- mice than that of the wild-type control (P < 0.01), but the lean mass remains constant [15].
  • Potential signaling pathways mediating MCH-R1 action in adipocytes were investigated [13].
  • The rodent MCH receptor (MCH1R) is highly expressed in the nucleus accumbens shell (AcSh), a region that is important in the regulation of appetitive behavior [4].

Associations of Mchr1 with chemical compounds

  • To examine the impact of MCHR1 receptor deletion on 5-HT neurotransmission, we used in vivo microdialysis in freely moving knockout and wild-type mice [2].
  • We studied the effects of intracerebroventricular (i.c.v.) administration of an MCH-1 receptor agonist (Compound A) and an MCH-1 receptor antagonist (Compound B) on feeding in satiated rats [16].
  • It is speculated that MCHR1 may contribute to the neurobiological mechanisms of conditioned cocaine-induced psychomotor effects, possibly to those underpinning sensitization, and to a lesser extent to those sub-serving acute pharmacological cocaine action [17].
  • A series of urea-based N-1-(2-aminoethyl)-indazoles was synthesized and evaluated for melanin-concentrating hormone receptor 1 (MCHr1) antagonism in both binding and functional assays [12].
  • Further delineation of the structural parameters essential for MCHr1-binding affinity of this class of nontraditional GPCR ligands resulted in the identification of compounds such as 33, 34 and 37, which demonstrate single digit nanomolar antagonism of MCHr1-mediated Ca(2+) release [18].

Other interactions of Mchr1


Analytical, diagnostic and therapeutic context of Mchr1

  • The performance of new vacuum filtration system was evaluated with MCH1 receptor binding assay and ligand washout experiments [22].
  • Both MCH and MCHR1 are expressed in mouse and human islets and in clonal beta-cell lines as assessed using quantitative real-time PCR and immunohistochemistry [23].
  • Additionally, while female and male mice carrying a null mutation of the MCHR1 gene show comparable anxiolytic-like behavior on the open field, only female knockout mice exhibit antidepressant-like behavior, when tested on the forced swim and tail suspension tests [5].


  1. Melanin-concentrating hormone 1 receptor-deficient mice are lean, hyperactive, and hyperphagic and have altered metabolism. Marsh, D.J., Weingarth, D.T., Novi, D.E., Chen, H.Y., Trumbauer, M.E., Chen, A.S., Guan, X.M., Jiang, M.M., Feng, Y., Camacho, R.E., Shen, Z., Frazier, E.G., Yu, H., Metzger, J.M., Kuca, S.J., Shearman, L.P., Gopal-Truter, S., MacNeil, D.J., Strack, A.M., MacIntyre, D.E., Van der Ploeg, L.H., Qian, S. Proc. Natl. Acad. Sci. U.S.A. (2002) [Pubmed]
  2. Genetic inactivation of melanin-concentrating hormone receptor subtype 1 (MCHR1) in mice exerts anxiolytic-like behavioral effects. Roy, M., David, N.K., Danao, J.V., Baribault, H., Tian, H., Giorgetti, M. Neuropsychopharmacology (2006) [Pubmed]
  3. Mice lacking melanin-concentrating hormone receptor 1 demonstrate increased heart rate associated with altered autonomic activity. Astrand, A., Bohlooly-Y, M., Larsdotter, S., Mahlapuu, M., Andersén, H., Tornell, J., Ohlsson, C., Snaith, M., Morgan, D.G. Am. J. Physiol. Regul. Integr. Comp. Physiol. (2004) [Pubmed]
  4. The hypothalamic neuropeptide melanin-concentrating hormone acts in the nucleus accumbens to modulate feeding behavior and forced-swim performance. Georgescu, D., Sears, R.M., Hommel, J.D., Barrot, M., Bolaños, C.A., Marsh, D.J., Bednarek, M.A., Bibb, J.A., Maratos-Flier, E., Nestler, E.J., DiLeone, R.J. J. Neurosci. (2005) [Pubmed]
  5. A study of the involvement of melanin-concentrating hormone receptor 1 (MCHR1) in murine models of depression. Roy, M., David, N., Cueva, M., Giorgetti, M. Biol. Psychiatry (2007) [Pubmed]
  6. The melanocortins and melanin-concentrating hormone in the central regulation of feeding behavior and energy homeostasis. Nahon, J.L. C. R. Biol. (2006) [Pubmed]
  7. Melanin-concentrating hormone is a critical mediator of the leptin-deficient phenotype. Segal-Lieberman, G., Bradley, R.L., Kokkotou, E., Carlson, M., Trombly, D.J., Wang, X., Bates, S., Myers, M.G., Flier, J.S., Maratos-Flier, E. Proc. Natl. Acad. Sci. U.S.A. (2003) [Pubmed]
  8. Melanin-concentrating hormone receptor 1 deficiency increases insulin sensitivity in obese leptin-deficient mice without affecting body weight. Bjursell, M., Gerdin, A.K., Ploj, K., Svensson, D., Svensson, L., Oscarsson, J., Snaith, M., Törnell, J., Bohlooly-Y, M. Diabetes (2006) [Pubmed]
  9. Leptin resistance and enhancement of feeding facilitation by melanin-concentrating hormone in mice lacking bombesin receptor subtype-3. Maekawa, F., Quah, H.M., Tanaka, K., Ohki-Hamazaki, H. Diabetes (2004) [Pubmed]
  10. Loss of heterozygosity on murine chromosome 6 in two-stage carcinogenesis: evidence for a conserved tumor suppressor gene. Zenklusen, J.C., Hodges, L.C., Conti, C.J. Oncogene (1997) [Pubmed]
  11. Identification of 2-(4-benzyloxyphenyl)-N- [1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity. Souers, A.J., Gao, J., Brune, M., Bush, E., Wodka, D., Vasudevan, A., Judd, A.S., Mulhern, M., Brodjian, S., Dayton, B., Shapiro, R., Hernandez, L.E., Marsh, K.C., Sham, H.L., Collins, C.A., Kym, P.R. J. Med. Chem. (2005) [Pubmed]
  12. Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity. Souers, A.J., Gao, J., Wodka, D., Judd, A.S., Mulhern, M.M., Napier, J.J., Brune, M.E., Bush, E.N., Brodjian, S.J., Dayton, B.D., Shapiro, R., Hernandez, L.E., Marsh, K.C., Sham, H.L., Collins, C.A., Kym, P.R. Bioorg. Med. Chem. Lett. (2005) [Pubmed]
  13. Melanin-concentrating hormone activates signaling pathways in 3T3-L1 adipocytes. Bradley, R.L., Mansfield, J.P., Maratos-Flier, E., Cheatham, B. Am. J. Physiol. Endocrinol. Metab. (2002) [Pubmed]
  14. Discovery of bicycloalkyl urea melanin concentrating hormone receptor antagonists: orally efficacious antiobesity therapeutics. McBriar, M.D., Guzik, H., Xu, R., Paruchova, J., Li, S., Palani, A., Clader, J.W., Greenlee, W.J., Hawes, B.E., Kowalski, T.J., O'Neill, K., Spar, B., Weig, B. J. Med. Chem. (2005) [Pubmed]
  15. Targeted disruption of the melanin-concentrating hormone receptor-1 results in hyperphagia and resistance to diet-induced obesity. Chen, Y., Hu, C., Hsu, C.K., Zhang, Q., Bi, C., Asnicar, M., Hsiung, H.M., Fox, N., Slieker, L.J., Yang, D.D., Heiman, M.L., Shi, Y. Endocrinology (2002) [Pubmed]
  16. Chronic MCH-1 receptor modulation alters appetite, body weight and adiposity in rats. Shearman, L.P., Camacho, R.E., Sloan Stribling, D., Zhou, D., Bednarek, M.A., Hreniuk, D.L., Feighner, S.D., Tan, C.P., Howard, A.D., Van der Ploeg, L.H., MacIntyre, D.E., Hickey, G.J., Strack, A.M. Eur. J. Pharmacol. (2003) [Pubmed]
  17. Mice lacking the melanin-concentrating hormone receptor-1 exhibit an atypical psychomotor susceptibility to cocaine and no conditioned cocaine response. Tyhon, A., Adamantidis, A., Foidart, A., Grisar, T., Lakaye, B., Tirelli, E. Behav. Brain Res. (2006) [Pubmed]
  18. Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2. Vasudevan, A., Wodka, D., Verzal, M.K., Souers, A.J., Gao, J., Brodjian, S., Fry, D., Dayton, B., Marsh, K.C., Hernandez, L.E., Ogiela, C.A., Collins, C.A., Kym, P.R. Bioorg. Med. Chem. Lett. (2004) [Pubmed]
  19. Importance of melanin-concentrating hormone receptor for the acute effects of ghrelin. Bjursell, M., Egecioglu, E., Gerdin, A.K., Svensson, L., Oscarsson, J., Morgan, D., Snaith, M., Törnell, J., Bohlooly-Y, M. Biochem. Biophys. Res. Commun. (2005) [Pubmed]
  20. Disrupting the melanin-concentrating hormone receptor 1 in mice leads to cognitive deficits and alterations of NMDA receptor function. Adamantidis, A., Thomas, E., Foidart, A., Tyhon, A., Coumans, B., Minet, A., Tirelli, E., Seutin, V., Grisar, T., Lakaye, B. Eur. J. Neurosci. (2005) [Pubmed]
  21. Relationship between the expression of differentiation-specific keratins 1 and 10 and cell proliferation in epidermal tumors. Kartasova, T., Roop, D.R., Yuspa, S.H. Mol. Carcinog. (1992) [Pubmed]
  22. Development of a vacuum filtration system for the conventional microplate washer. Lee, S. Journal of pharmacological and toxicological methods. (2006) [Pubmed]
  23. Melanin concentrating hormone is a novel regulator of islet function and growth. Pissios, P., Ozcan, U., Kokkotou, E., Okada, T., Liew, C.W., Liu, S., Peters, J.N., Dahlgren, G., Karamchandani, J., Kudva, Y.C., Kurpad, A.J., Kennedy, R.T., Maratos-Flier, E., Kulkarni, R.N. Diabetes (2007) [Pubmed]
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