BPS/IUPHAR Guide to Pharmacology | GRAC GPCR FAMILIES | Melanin-concentrating hormone receptors

Melanin-concentrating hormone receptors

More information on this family may be found on the IUPHAR-DB family and introduction pages.

Melanin-concentrating hormone (MCH) receptors (provisional nomenclature, [5]) are activated by an endogenous nonadecameric cyclic peptide identical in humans and rats (DFDMLRCMLGRVYRPCWQV) generated from a precursor (ENSG00000183395), which also produces neuropeptide EI and neuropeptide GE.

Unless otherwise stated all data refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Receptors

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Chung, S; Parks, GS; Lee, C; Civelli, O. (2011) Recent updates on the melanin-concentrating hormone (MCH) and its receptor system: lessons from MCH1R antagonists. J. Mol. Neurosci., 43 (1): 115-21. [PMID:20582487]

Chung, S; Saito, Y; Civelli, O. (2009) MCH receptors/gene structure-in vivo expression. Peptides, 30 (11): 1985-9. [PMID:19647772]

Eberle, AN; Mild, G; Zumsteg, U. (2010) Cellular models for the study of the pharmacology and signaling of melanin-concentrating hormone receptors. J. Recept. Signal Transduct. Res., 30 (6): 385-402. [PMID:21083507]

Foord, S. M., Bonner, T. I., Neubig, R. R., Rosser, E. M., Pin, J. P., Davenport, A. P., Spedding, M. and Harmar, A. J. (2005) International Union of Pharmacology. XLVI. G protein-coupled receptor list. Pharmacol Rev, 57: 279-288. [PMID:15914470]

Gao, XB. (2009) Electrophysiological effects of MCH on neurons in the hypothalamus. Peptides, 30 (11): 2025-30. [PMID:19463877]

Kemp, EH; Weetman, AP. (2009) Melanin-concentrating hormone and melanin-concentrating hormone receptors in mammalian skin physiopathology. Peptides, 30 (11): 2071-5. [PMID:19442695]

Lakaye, B; Coumans, B; Harray, S; Grisar, T. (2009) Melanin-concentrating hormone and immune function. Peptides, 30 (11): 2076-80. [PMID:19450627]

Luthin, DR. (2007) Anti-obesity effects of small molecule melanin-concentrating hormone receptor 1 (MCHR1) antagonists. Life Sci., 81 (6): 423-40. [PMID:17655875]

Pissios, P. (2009) Animals models of MCH function and what they can tell us about its role in energy balance. Peptides, 30 (11): 2040-4. [PMID:19447150]

Pissios, P., Bradley, R. L. and Maratos-Flier, E. (2006) The multiple roles of MCH in regulating energy balance and other biological functions. Endocr. Rev., 27: 606-620. [PMID:16788162]

Rokosz, LL; Hobbs, DW. (2006) Biological examination of melanin concentrating hormone receptor 1: multi-tasking from the hypothalamus. Drug News Perspect., 19 (5): 273-86. [PMID:16941049]

Saito, Y. and Nagasaki, H. (2008) The melanin-concentrating hormone system and its physiological functions. Results Probl. Cell Differ., 46: 159-179. [PMID:18227983]

Shimazaki, T; Yoshimizu, T; Chaki, S. (2006) Melanin-concentrating hormone MCH1 receptor antagonists: a potential new approach to the treatment of depression and anxiety disorders. CNS Drugs, 20 (10): 801-11. [PMID:16999451]

References Show »« Hide

1. Audinot, V., Lahaye, C., Suply, T., Beauverger, P., Rodriguez, M., Galizzi, J. P., Fauchere, J. L. and Boutin, J. A. (2001) [125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor. Br J Pharmacol, 133: 371-378. [PMID:11375253]

2. Borowsky, B., Durkin, M. M., Ogozalek, K., Marzabadi, M. R., DeLeon, J., Lagu, B., Heurich, R., Lichtblau, H., Shaposhnik, Z., Daniewska, I., Blackburn, T. P., Branchek, T. A., Gerald, C., Vaysse, P. J. and Forray, C. (2002) Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor antagonist. Nat Med, 8: 825-830. [PMID:12118247]

3. Burgaud, JL; Poosti, R; Fehrentz, JA; Martinez, J; Nahon, JL. (1997) Melanin-concentrating hormone binding sites in human SVK14 keratinocytes. Biochem. Biophys. Res. Commun., 241 (3): 622-9. [PMID:9434758]

4. Chaki, S., Funakoshi, T., Hirota-Okuno, S., Nishiguchi, M., Shimazaki, T., Iijima, M., Grottick, A. J., Kanuma, K., Omodera, K., Sekiguchi, Y., Okuyama, S., Tran, T. A., Semple, G. and Thomsen, W. (2005) Anxiolytic- and antidepressant-like profile of ATC0065 and ATC0175: nonpeptidic and orally active melanin-concentrating hormone receptor 1 antagonists. J Pharmacol Exp Ther, 313: 831-839. [PMID:15677346]

5. Foord, S. M., Bonner, T. I., Neubig, R. R., Rosser, E. M., Pin, J. P., Davenport, A. P., Spedding, M. and Harmar, A. J. (2005) International Union of Pharmacology. XLVI. G protein-coupled receptor list. Pharmacol Rev, 57: 279-288. [PMID:15914470]

6. Hertzog, DL; Al-Barazanji, KA; Bigham, EC; Bishop, MJ; Britt, CS; Carlton, DL; Cooper, JP; Daniels, AJ; Garrido, DM; Goetz, AS; et al.. (2006) The discovery and optimization of pyrimidinone-containing MCH R1 antagonists. Bioorg. Med. Chem. Lett., 16 (18): 4723-7. [PMID:16870432]

7. Hill, J., Duckworth, M., Murdock, P., Rennie, G., Sabido-David, C., Ames, R. S., Szekeres, P., Wilson, S., Bergsma, D. J., Gloger, I. S., Levy, D. S., Chambers, J. K. and Muir, A. I. (2001) Molecular cloning and functional characterization of MCH2, a novel human MCH receptor. J Biol Chem, 276: 20125-20129. [PMID:11274220]

8. Mori, M., Harada, M., Terao, Y., Sugo, T., Watanabe, T., Shimomura, Y., Abe, M., Shintani, Y., Onda, H., Nishimura, O. and Fujino, M. (2001) Cloning of a novel G protein-coupled receptor, SLT, a subtype of the melanin-concentrating hormone receptor. Biochem Biophys Res Commun, 283: 1013-1018. [PMID:11355873]

9. Rodriguez, M., Beauverger, P., Naime, I., Rique, H., Ouvry, C., Souchaud, S., Dromaint, S., Nagel, N., Suply, T., Audinot, V., Boutin, J. A. and Galizzi, J. P. (2001) Cloning and molecular characterization of the novel human melanin-concentrating hormone receptor MCH2. Mol Pharmacol, 60: 632-639. [PMID:11562423]

10. Takekawa, S., Asami, A., Ishihara, Y., Terauchi, J., Kato, K., Shimomura, Y., Mori, M., Murakoshi, H., Kato, K., Suzuki, N., Nishimura, O. and Fujino, M. (2002) T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist. Eur J Pharmacol, 438: 129-135. [PMID:11909603]

11. Tan, C. P., Sano, H., Iwaasa, H., Pan, J., Sailer, A. W., Hreniuk, D. L., Feighner, S. D., Palyha, O. C., Pong, S. S., Figueroa, D. J., Austin, C. P., Jiang, M. M., Yu, H., Ito, J., Ito, M., Ito, M., Guan, X. M., MacNeil, D. J., Kanatani, A., Van der Ploeg, L. H. and Howard, A. D. (2002) Melanin-concentrating hormone receptor subtypes 1 and 2: species-specific gene expression. Genomics, 79: 785-792. [PMID:12036292]