Melanin-koncentrirajući hormonski receptor 1 — разлика између измена
Изглед
Садржај обрисан Садржај додат
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*[[Melanin-koncentrirajući hormone receptor]] |
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==Literatura== |
==Literatura== |
Верзија на датум 26. август 2010. у 21:15
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
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
Agonisti
- Melanin koncentrirajući hormone (MCH)
- S-36057 - modifikovani MCH 6-13 fragment zamenjen sa 3-jodotirozinom na N-terminusu putem dioksioktanoil linkera. Koristi se kao 125I radioligand za MCH1 mapiranje in vivo.[10][11]
Antagonisti
- ATC-0065
- ATC-0175[12]
- GW-803,430[13]
- NGD-4715
- SNAP-7941[14]
- SNAP-94847[15]
- T-226,296[16]
Vidi isto
Literatura
- ^ а б „Entrez Gene: MCHR1 melanin-concentrating hormone receptor 1”.
- ^ 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. Непознати параметар
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игнорисан (помоћ) - ^ 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.
- ^ 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. Непознати параметар
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игнорисан (помоћ) - ^ 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.
- ^ 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. Непознати параметар
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игнорисан (помоћ) - ^ 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. Непознати параметар
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игнорисан (помоћ) - ^ 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. Непознати параметар
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игнорисан (помоћ) - ^ 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.
- ^ 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 1572795
. PMID 11375253. doi:10.1038/sj.bjp.0704085. Непознати параметар
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игнорисан (помоћ) - ^ 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. Непознати параметар
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игнорисан (помоћ) - ^ 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.
- ^ 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. Непознати параметар
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игнорисан (помоћ) - ^ 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. Непознати параметар
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игнорисан (помоћ) - ^ {{cite journal |author=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 |month=April |pmid=17237257 |doi=10.1124/jpet.106.109678 |url=}}
- ^ 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. Непознати параметар
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