Melanin-koncentrirajući hormonski receptor 1

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Melanin-koncentrirajući hormonski receptor 1
Identifikatori
Simboli MCHR1; GPR24; MCH1R; MGC32129; SLC1
Vanjski ID OMIM601751 MGI2180756 HomoloGene21097 IUPHAR: MCH1 GeneCards: MCHR1 Gene
Pregled RNK izražavanja
PBB GE MCHR1 221354 s at tn.png
podaci
Ortolozi
Vrsta Čovek Miš
Entrez 2847 207911
Ensembl ENSG00000128285 ENSMUSG00000050164
UniProt Q99705 Q3UY93
RefSeq (mRNA) NM_005297 NM_145132
RefSeq (protein) NP_005288 NP_660114
Lokacija (UCSC) Chr 22:
39.41 - 39.41 Mb
Chr 15:
81.06 - 81.07 Mb
PubMed pretraga [1] [2]

Melanin-koncentrirajući hormonski receptor 1, takođe poznat kao MCH1, je jedan od ljudskih melanin-koncentrirajućih hormonskih receptora.[1]

Protein kodiran ovim genom je član G protein-spregnuti receptor familije 1. On je integralni protein membrane plazme koji vezuje melanin-koncentrirajući hormon. Ovaj receptor može da inhibira cAMP akumulaciju, i da stimuliše intracelularni kalcijum fluks. Smatra se da on učestvuje u neuronalnoj regulaciju konzumacije hrane. Mada je strukturno sličan sa somatostatin receptorima, ovaj protein ne vezuje somatostatin.[1]

Funkcija[уреди]

MCH1 ima brojne funkcije, u koje se ubrajaju regulacija apetita,[2][3] kao i posredovanje stresa, strepnje i depresije.[4][5][6][7][8][9]

Selektivni Ligandi[уреди]

Agonisti[уреди]

Antagonisti[уреди]

Vidi još[уреди]

Literatura[уреди]

  1. 1,0 1,1 „Entrez Gene: MCHR1 melanin-concentrating hormone receptor 1”. 
  2. ^ Luthin DR (2007). „Anti-obesity effects of small molecule melanin-concentrating hormone receptor 1 (MCHR1) antagonists”. Life Sciences. 81 (6): 423—40. PMID 17655875. doi:10.1016/j.lfs.2007.05.029. 
  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—43. PMID 18393860. doi:10.2174/092986708784049621. 
  4. ^ Hervieu G (2003). „Melanin-concentrating hormone functions in the nervous system: food intake and stress”. Expert Opinion on Therapeutic Targets. 7 (4): 495—511. PMID 12885269. doi:10.1517/14728222.7.4.495. 
  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. PMID 16999451. 
  6. ^ Hervieu GJ (2006). „Further insights into the neurobiology of melanin-concentrating hormone in energy and mood balances”. Expert Opinion on Therapeutic Targets. 10 (2): 211—29. PMID 16548771. doi:10.1517/14728222.10.2.211. 
  7. ^ Smith DG, Davis RJ, Rorick-Kehn L, Morin M, Witkin JM, McKinzie DL, Nomikos GG, Gehlert DR (2006). „Melanin-concentrating hormone-1 receptor modulates neuroendocrine, behavioral, and corticolimbic neurochemical stress responses in mice”. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 31 (6): 1135—45. PMID 16205780. doi:10.1038/sj.npp.1300913. 
  8. ^ Roy M, David N, Cueva M, Giorgetti M (2007). „A study of the involvement of melanin-concentrating hormone receptor 1 (MCHR1) in murine models of depression”. Biological Psychiatry. 61 (2): 174—80. PMID 16934771. doi:10.1016/j.biopsych.2006.03.076. 
  9. ^ Saito Y, Nagasaki H (2008). „The melanin-concentrating hormone system and its physiological functions”. Results and Problems in Cell Differentiation. 46: 159—79. PMID 18227983. doi:10.1007/400_2007_052. 
  10. ^ Audinot V, Lahaye C, Suply T, Beauverger P, Rodriguez M, Galizzi JP, Fauchère JL, Boutin JA (2001). „[125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor”. British Journal of Pharmacology. 133 (3): 371—8. PMC 1572795Слободан приступ. PMID 11375253. doi:10.1038/sj.bjp.0704085. 
  11. ^ Able SL, Ivarsson M, Fish RL, Clarke TL, McCourt C, Duckworth JM, Napier C, Katugampola SD (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—6. PMID 19540226. doi:10.1016/j.ejphar.2009.06.009. 
  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—52. PMID 16614734. 
  13. ^ Gehlert DR, Rasmussen K, Shaw J, Li X, Ardayfio P, Craft L, Coskun T, Zhang HY, Chen Y, Witkin JM (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—38. PMID 19182070. doi:10.1124/jpet.108.143362. 
  14. ^ Doggrell SA (2003). „Does the melanin-concentrating hormone antagonist SNAP-7941 deserve 3As?”. Expert Opinion on Investigational Drugs. 12 (6): 1035—8. PMID 12783607. doi:10.1517/13543784.12.6.1035. 
  15. ^ {{cite journal |vauthors=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 |title=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 |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=321 |issue=1 |pages=237–48 |year=2007 |pmid=17237257 |doi=10.1124/jpet.106.109678 |url=}}
  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 (2002). „T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist”. European Journal of Pharmacology. 438 (3): 129—35. PMID 11909603. doi:10.1016/S0014-2999(02)01314-6. 

Dodatna literatura[уреди]

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  • Saito Y; Nothacker HP; Wang Z; et al. (1999). „Molecular characterization of the melanin-concentrating-hormone receptor.”. Nature. 400 (6741): 265—9. PMID 10421368. doi:10.1038/22321. 
  • Shimomura Y; Mori M; Sugo T; et al. (1999). „Isolation and identification of melanin-concentrating hormone as the endogenous ligand of the SLC-1 receptor.”. Biochem. Biophys. Res. Commun. 261 (3): 622—6. PMID 10441476. doi:10.1006/bbrc.1999.1104. 
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