Melanin-concentrating hormone receptor 1

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Melanin-concentrating hormone receptor 1
Identifiers
Symbols MCHR1 ; GPR24; MCH-1R; MCH1R; SLC-1; SLC1
External IDs OMIM601751 MGI2180756 HomoloGene21097 IUPHAR: MCH1 ChEMBL: 344 GeneCards: MCHR1 Gene
RNA expression pattern
PBB GE MCHR1 221354 s at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez 2847 207911
Ensembl ENSG00000128285 ENSMUSG00000050164
UniProt Q99705 Q8JZL2
RefSeq (mRNA) NM_005297 NM_145132
RefSeq (protein) NP_005288 NP_660114
Location (UCSC) Chr 22:
41.07 – 41.08 Mb
Chr 15:
81.24 – 81.24 Mb
PubMed search [1] [2]

Melanin-concentrating hormone receptor 1, also known as MCH1, is one of the human melanin-concentrating hormone receptors.[1]

The protein encoded by this gene, a member of the G protein-coupled receptor family 1, is an integral plasma membrane protein which binds melanin-concentrating hormone. The encoded protein can inhibit cAMP accumulation and stimulate intracellular calcium flux, and is probably involved in the neuronal regulation of food consumption. Although structurally similar to somatostatin receptors, this protein does not seem to bind somatostatin.[1]

Function[edit]

MCH1 is thought to have a number of functions including in the regulation of appetite,[2][3] and in stress, anxiety and depression.[4][5][6][7][8][9]

Selective Ligands[edit]

Agonists[edit]

Antagonists[edit]

See also[edit]

References[edit]

  1. ^ a b "Entrez Gene: MCHR1 melanin-concentrating hormone receptor 1". 
  2. ^ Luthin DR (July 2007). "Anti-obesity effects of small molecule melanin-concentrating hormone receptor 1 (MCHR1) antagonists". Life Sciences 81 (6): 423–440. doi:10.1016/j.lfs.2007.05.029. PMID 17655875. 
  3. ^ Rivera G, Bocanegra-García V, Galiano S, Cirauqui N, Ceras J, Pérez S, Aldana I, Monge A (2008). "Melanin-concentrating hormone receptor 1 antagonists: a new perspective for the pharmacologic treatment of obesity". Current Medicinal Chemistry 15 (10): 1025–1043. doi:10.2174/092986708784049621. PMID 18393860. 
  4. ^ Hervieu G (August 2003). "Melanin-concentrating hormone functions in the nervous system: food intake and stress". Expert Opinion on Therapeutic Targets 7 (4): 495–511. doi:10.1517/14728222.7.4.495. PMID 12885269. 
  5. ^ 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. doi:10.2165/00023210-200620100-00002. PMID 16999451. 
  6. ^ Hervieu GJ (April 2006). "Further insights into the neurobiology of melanin-concentrating hormone in energy and mood balances". Expert Opinion on Therapeutic Targets 10 (2): 211–229. doi:10.1517/14728222.10.2.211. PMID 16548771. 
  7. ^ Smith DG, Davis RJ, Rorick-Kehn L, Morin M, Witkin JM, McKinzie DL, Nomikos GG, Gehlert DR (June 2006). "Melanin-concentrating hormone-1 receptor modulates neuroendocrine, behavioral, and corticolimbic neurochemical stress responses in mice". Neuropsychopharmacology 31 (6): 1135–45. doi:10.1038/sj.npp.1300913. PMID 16205780. 
  8. ^ Roy M, David N, Cueva M, Giorgetti M (January 2007). "A study of the involvement of melanin-concentrating hormone receptor 1 (MCHR1) in murine models of depression". Biological Psychiatry 61 (2): 174–180. doi:10.1016/j.biopsych.2006.03.076. PMID 16934771. 
  9. ^ Saito Y, Nagasaki H (2008). "The melanin-concentrating hormone system and its physiological functions". Results and Problems in Cell Differentiation. Results and Problems in Cell Differentiation 46: 159–179. doi:10.1007/400_2007_052. ISBN 978-3-540-78350-3. PMID 18227983. 
  10. ^ Audinot V, Lahaye C, Suply T, Beauverger P, Rodriguez M, Galizzi JP, Fauchère JL, Boutin JA (June 2001). "[125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor". British Journal of Pharmacology 133 (3): 371–378. doi:10.1038/sj.bjp.0704085. PMC 1572795. PMID 11375253. 
  11. ^ Able SL, Ivarsson M, Fish RL, Clarke TL, McCourt C, Duckworth JM, Napier C, Katugampola SD (June 2009). "Localisation of melanin-concentrating hormone receptor 1 in rat brain and evidence that sleep parameters are not altered despite high central receptor occupancy". European Journal of Pharmacology 616 (1–3): 101–106. doi:10.1016/j.ejphar.2009.06.009. PMID 19540226. 
  12. ^ Chaki S, Yamaguchi J, Yamada H, Thomsen W, Tran TA, Semple G, Sekiguchi Y (2005). "ATC0175: an orally active melanin-concentrating hormone receptor 1 antagonist for the potential treatment of depression and anxiety". CNS Drug Reviews 11 (4): 341–352. doi:10.1111/j.1527-3458.2005.tb00052.x. PMID 16614734. 
  13. ^ Gehlert DR, Rasmussen K, Shaw J, Li X, Ardayfio P, Craft L, Coskun T, Zhang HY, Chen Y, Witkin JM (May 2009). "Preclinical evaluation of melanin-concentrating hormone receptor 1 antagonism for the treatment of obesity and depression". The Journal of Pharmacology and Experimental Therapeutics 329 (2): 429–438. doi:10.1124/jpet.108.143362. PMID 19182070. 
  14. ^ Doggrell SA (June 2003). "Does the melanin-concentrating hormone antagonist SNAP-7941 deserve 3As?". Expert Opinion on Investigational Drugs 12 (6): 1035–1038. doi:10.1517/13543784.12.6.1035. PMID 12783607. 
  15. ^ David DJ, Klemenhagen KC, Holick KA, Saxe MD, Mendez I, Santarelli L, Craig DA, Zhong H, Swanson CJ, Hegde LG, Ping XI, Dong D, Marzabadi MR, Gerald CP, Hen R (April 2007). "Efficacy of the MCHR1 antagonist N-[3-(1-{[4-(3,4-difluorophenoxy)phenyl]methyl}(4-piperidyl))-4-methylphenyl]-2-methylpropanamide (SNAP 94847) in mouse models of anxiety and depression following acute and chronic administration is independent of hippocampal neurogenesis". The Journal of Pharmacology and Experimental Therapeutics 321 (1): 237–48. doi:10.1124/jpet.106.109678. PMID 17237257. 
  16. ^ Takekawa S, Asami A, Ishihara Y, Terauchi J, Kato K, Shimomura Y, Mori M, Murakoshi H, Kato K, Suzuki N, Nishimura O, Fujino M (March 2002). "T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist". European Journal of Pharmacology 438 (3): 129–135. doi:10.1016/S0014-2999(02)01314-6. PMID 11909603. 

External links[edit]

Further reading[edit]

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