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Gene and Protein Information | ||||||
class A G protein-coupled receptor | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 7 | 422 | 22q13.2 | MCHR1 | melanin concentrating hormone receptor 1 | 10,43 |
Mouse | 7 | 353 | 15 E1 | Mchr1 | melanin-concentrating hormone receptor 1 | 42 |
Rat | 7 | 353 | 7q34 | Mchr1 | melanin-concentrating hormone receptor 1 | 48 |
Gene and Protein Information Comments | ||||||
MCHR1 genes have been identified in Xenopus [40], goldfish [59], flounder [81], zebrafish [52] and shark [58]. |
Previous and Unofficial Names |
GPR24 | MCH1R | G protein-coupled receptor 24 | MCH receptor 1 | somatostatin receptor-like protein |
Database Links | |
Specialist databases | |
GPCRdb | mchr1_human (Hs), mchr1_mouse (Mm), mchr1_rat (Rn) |
Other databases | |
Alphafold | Q99705 (Hs), Q8JZL2 (Mm), P97639 (Rn) |
ChEMBL Target | CHEMBL344 (Hs), CHEMBL4730 (Mm), CHEMBL1075228 (Rn) |
Ensembl Gene | ENSG00000128285 (Hs), ENSMUSG00000050164 (Mm), ENSRNOG00000018895 (Rn) |
Entrez Gene | 2847 (Hs), 207911 (Mm), 83567 (Rn) |
Human Protein Atlas | ENSG00000128285 (Hs) |
KEGG Gene | hsa:2847 (Hs), mmu:207911 (Mm), rno:83567 (Rn) |
OMIM | 601751 (Hs) |
Pharos | Q99705 (Hs) |
RefSeq Nucleotide | NM_005297 (Hs), NM_145132 (Mm), NM_031758 (Rn) |
RefSeq Protein | NP_005288 (Hs), NP_660114 (Mm), NP_113946 (Rn) |
UniProtKB | Q99705 (Hs), Q8JZL2 (Mm), P97639 (Rn) |
Wikipedia | MCHR1 (Hs) |
Associated Proteins | |||||||||||||||||||||
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Associated Protein Comments | |||||||||||||||||||||
MIZIP (ZMYND19; Q96E35) colocalizes with MCH1 receptor in HEK293 cells when the proteins are coexpressed using a yeast two-hybrid system [12]. The interaction occurs at the C-terminus of the receptor. Neurochondrin (NCDN; Q9UBB6) and periplakin (PPL; O60437) both inhibit GTPγS binding, GIRK activity and Ca2+ mobilisation in HEK293 cells when the proteins are coexpressed using a yeast two-hybrid system [26,62]. Again, the interactions occur at the C-terminus of the receptor. In cotransfected HEK293 cells RGS8 (P57771) inhibits Gi/o and Gq-dependent Ca2+ mobilisation via an interaction within the third cytoplasmic loop [55]. In similar experiments RGS2 (P41220) inhibits Gq-dependent Ca2+ mobilisation [56]. |
Natural/Endogenous Ligands |
melanin-concentrating hormone {Sp: Human, Mouse, Rat} |
Download all structure-activity data for this target as a CSV file
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Ligand rank potency: melanin-concentrating hormone > MCH (salmon) |
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Allosteric Modulators | |||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||
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Primary Transduction Mechanisms | |
Transducer | Effector/Response |
Gs family Gi/Go family Gq/G11 family |
Adenylyl cyclase inhibition Phospholipase C stimulation |
References: 33,67,72-73 |
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Functional Assay Comments | ||||||||||
Calcium accumulation and mobilisation and downstream ERK phosphorylation have been reported using goldfish [32], Xenopus tropicalis [40] and flounder [81] MCH1 receptors. |
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Phenotypes, Alleles and Disease Models | Mouse data from MGI | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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General Comments |
In humans, MCH2 shares a similar distribution pattern as MCH1. However no role is ascribed yet to MCH2 due both to the lack of expression in rodents and the lack of selective antagonists. |
1. Adamantidis A, Salvert D, Goutagny R, Lakaye B, Gervasoni D, Grisar T, Luppi PH, Fort P. (2008) Sleep architecture of the melanin-concentrating hormone receptor 1-knockout mice. Eur J Neurosci, 27 (7): 1793-800. [PMID:18380672]
2. Adams AC, Domouzoglou EM, Chee MJ, Segal-Lieberman G, Pissios P, Maratos-Flier E. (2011) Ablation of the hypothalamic neuropeptide melanin concentrating hormone is associated with behavioral abnormalities that reflect impaired olfactory integration. Behav Brain Res, 224 (1): 195-200. [PMID:21669232]
3. Ahnaou A, Dautzenberg FM, Huysmans H, Steckler T, Drinkenburg WH. (2011) Contribution of melanin-concentrating hormone (MCH1) receptor to thermoregulation and sleep stabilization: evidence from MCH1 (-/-) mice. Behav Brain Res, 218 (1): 42-50. [PMID:21074567]
4. AstraZeneca. AZ13483342. Accessed on 16/09/2014. Modified on 16/09/2014. astrazeneca.com, http://openinnovation.astrazeneca.com/what-we-offer/compound/az13483342/
5. 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. Br J Pharmacol, 133 (3): 371-8. [PMID:11375253]
6. Audinot V, Zuana OD, Fabry N, Ouvry C, Nosjean O, Henlin JM, Fauchère JL, Boutin JA. (2009) S38151 [p-guanidinobenzoyl-[Des-Gly(10)]-MCH(7-17)] is a potent and selective antagonist at the MCH(1) receptor and has anti-feeding properties in vivo. Peptides, 30 (11): 1997-2007. [PMID:19619599]
7. Bednarek MA, Hreniuk DL, Tan C, Palyha OC, MacNeil DJ, Van der Ploeg LH, Howard AD, Feighner SD. (2002) Synthesis and biological evaluation in vitro of selective, high affinity peptide antagonists of human melanin-concentrating hormone action at human melanin-concentrating hormone receptor 1. Biochemistry, 41 (20): 6383-90. [PMID:12009900]
8. Benedetto L, Rodriguez-Servetti Z, Lagos P, D'Almeida V, Monti JM, Torterolo P. (2013) Microinjection of melanin concentrating hormone into the lateral preoptic area promotes non-REM sleep in the rat. Peptides, 39: 11-5. [PMID:23123302]
9. Berbari NF, Johnson AD, Lewis JS, Askwith CC, Mykytyn K. (2008) Identification of ciliary localization sequences within the third intracellular loop of G protein-coupled receptors. Mol Biol Cell, 19 (4): 1540-7. [PMID:18256283]
10. Borowsky B, Durkin MM, Ogozalek K, Marzabadi MR, DeLeon J, Lagu B, Heurich R, Lichtblau H, Shaposhnik Z, Daniewska I, Blackburn TP, Branchek TA, Gerald C, Vaysse PJ, Forray C. (2002) Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor antagonist. Nat Med, 8: 825-830. [PMID:12118247]
11. 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]
12. Bächner D, Kreienkamp H, Weise C, Buck F, Richter D. (1999) Identification of melanin concentrating hormone (MCH) as the natural ligand for the orphan somatostatin-like receptor 1 (SLC-1). FEBS Lett, 457 (3): 522-4. [PMID:10471841]
13. Bächner D, Kreienkamp HJ, Richter D. (2002) MIZIP, a highly conserved, vertebrate specific melanin-concentrating hormone receptor 1 interacting zinc-finger protein. FEBS Lett, 526 (1-3): 124-8. [PMID:12208518]
14. Chaki S, Funakoshi T, Hirota-Okuno S, Nishiguchi M, Shimazaki T, Iijima M, Grottick AJ, Kanuma K, Omodera K, Sekiguchi Y, Okuyama S, Tran TA, Semple G, 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]
15. Chambers J, Ames RS, Bergsma D, Muir A, Fitzgerald LR, Hervieu G, Dytko GM, Foley JJ, Martin J, Liu WS et al.. (1999) Melanin-concentrating hormone is the cognate ligand for the orphan G-protein-coupled receptor SLC-1. Nature, 400 (6741): 261-5. [PMID:10421367]
16. Chen Y, Hu C, Hsu CK, Zhang Q, Bi C, Asnicar M, Hsiung HM, Fox N, Slieker LJ, Yang DD et al.. (2002) Targeted disruption of the melanin-concentrating hormone receptor-1 results in hyperphagia and resistance to diet-induced obesity. Endocrinology, 143 (7): 2469-77. [PMID:12072376]
17. Chung S, Hopf FW, Nagasaki H, Li CY, Belluzzi JD, Bonci A, Civelli O. (2009) The melanin-concentrating hormone system modulates cocaine reward. Proc Natl Acad Sci USA, 106 (16): 6772-7. [PMID:19342492]
18. Chung S, Liao XH, Di Cosmo C, Van Sande J, Wang Z, Refetoff S, Civelli O. (2012) Disruption of the melanin-concentrating hormone receptor 1 (MCH1R) affects thyroid function. Endocrinology, 153 (12): 6145-54. [PMID:23024261]
19. Cippitelli A, Karlsson C, Shaw JL, Thorsell A, Gehlert DR, Heilig M. (2010) Suppression of alcohol self-administration and reinstatement of alcohol seeking by melanin-concentrating hormone receptor 1 (MCH1-R) antagonism in Wistar rats. Psychopharmacology (Berl.), 211 (4): 367-75. [PMID:20628734]
20. Conductier G, Brau F, Viola A, Langlet F, Ramkumar N, Dehouck B, Lemaire T, Chapot R, Lucas L, Rovère C et al.. (2013) Melanin-concentrating hormone regulates beat frequency of ependymal cilia and ventricular volume. Nat Neurosci, 16 (7): 845-7. [PMID:23708141]
21. Conductier G, Martin AO, Risold PY, Jego S, Lavoie R, Lafont C, Mollard P, Adamantidis A, Nahon JL. (2013) Control of ventricular ciliary beating by the melanin concentrating hormone-expressing neurons of the lateral hypothalamus: a functional imaging survey. Front Endocrinol (Lausanne), 4: 182. [PMID:24324458]
22. Cotta-Grand N, Rovère C, Guyon A, Cervantes A, Brau F, Nahon JL. (2009) Melanin-concentrating hormone induces neurite outgrowth in human neuroblastoma SH-SY5Y cells through p53 and MAPKinase signaling pathways. Peptides, 30 (11): 2014-24. [PMID:19540893]
23. David DJ, Klemenhagen KC, Holick KA, Saxe MD, Mendez I, Santarelli L, Craig D, Zong H, Swanson C, Hegde LG, Ping XI, Dong D, Marzabadi MR, Gerald C, Hen R. (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. J Pharmacol Exp Ther,: -. [PMID:17237257]
24. Duncan EA, Rider TR, Jandacek RJ, Clegg DJ, Benoit SC, Tso P, Woods SC. (2006) The regulation of alcohol intake by melanin-concentrating hormone in rats. Pharmacol Biochem Behav, 85 (4): 728-35. [PMID:17188345]
25. Fox BM, Natero R, Richard K, Connors R, Roveto PM, Beckmann H, Haller K, Golde J, Xiao SH, Kayser F. (2011) Novel pyrrolidine melanin-concentrating hormone receptor 1 antagonists with reduced hERG inhibition. Bioorg Med Chem Lett, 21 (8): 2460-7. [PMID:21414780]
26. Francke F, Ward RJ, Jenkins L, Kellett E, Richter D, Milligan G, Bächner D. (2006) Interaction of neurochondrin with the melanin-concentrating hormone receptor 1 interferes with G protein-coupled signal transduction but not agonist-mediated internalization. J Biol Chem, 281 (43): 32496-507. [PMID:16945926]
27. Frezzotti R, Caporossi A. (1990) Pathogenesis of posterior capsular opacification. Part I. Epidemiological and clinico-statistical data. J Cataract Refract Surg, 16 (3): 347-52. [PMID:2355323]
28. Georgescu D, Sears RM, Hommel JD, Barrot M, Bolaños CA, Marsh DJ, Bednarek MA, Bibb JA, Maratos-Flier E, Nestler EJ et al.. (2005) The hypothalamic neuropeptide melanin-concentrating hormone acts in the nucleus accumbens to modulate feeding behavior and forced-swim performance. J Neurosci, 25 (11): 2933-40. [PMID:15772353]
29. Geuzaine A, Tyhon A, Grisar T, Brabant C, Lakaye B, Tirelli E. (2014) Amphetamine reward in food restricted mice lacking the melanin-concentrating hormone receptor-1. Behav Brain Res, 262: 14-20. [PMID:24412349]
30. Giordanetto F, Karlsson O, Lindberg J, Larsson LO, Linusson A, Evertsson E, Morgan DG, Inghardt T. (2007) Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists. Bioorg Med Chem Lett, 17 (15): 4232-41. [PMID:17532215]
31. Guo T, Gu H, Hobbs DW, Busler DE, Rokosz LL. (2007) Discovery of tetralin ureas as potent melanin concentrating hormone 1 receptor antagonists. Bioorg Med Chem Lett, 17 (6): 1718-21. [PMID:17251014]
32. Hamamoto A, Mizusawa K, Takahashi A, Saito Y. (2011) Signalling pathway of goldfish melanin-concentrating hormone receptors 1 and 2. Regul Pept, 169 (1-3): 6-12. [PMID:21539863]
33. Hawes BE, Kil E, Green B, O'Neill K, Fried S, Graziano MP. (2000) The melanin-concentrating hormone receptor couples to multiple G proteins to activate diverse intracellular signaling pathways. Endocrinology, 141 (12): 4524-32. [PMID:11108264]
34. 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]
35. Hervieu GJ, Cluderay JE, Harrison D, Meakin J, Maycox P, Nasir S, Leslie RA. (2000) The distribution of the mRNA and protein products of the melanin-concentrating hormone (MCH) receptor gene, slc-1, in the central nervous system of the rat. Eur J Neurosci, 12 (4): 1194-216. [PMID:10762350]
36. Hill J, Duckworth M, Murdock P, Rennie G, Sabido-David C, Ames RS, Szekeres P, Wilson S, Bergsma DJ, Gloger IS et al.. (2001) Molecular cloning and functional characterization of MCH2, a novel human MCH receptor. J Biol Chem, 276 (23): 20125-9. [PMID:11274220]
37. Jego S, Glasgow SD, Herrera CG, Ekstrand M, Reed SJ, Boyce R, Friedman J, Burdakov D, Adamantidis AR. (2013) Optogenetic identification of a rapid eye movement sleep modulatory circuit in the hypothalamus. Nat Neurosci, 16 (11): 1637-43. [PMID:24056699]
38. Karagiannis AK, Ziogas DC, Gras-Miralles B, Geiger BM, Nagel J, Trebicka E, Najarian R, Cherayil BJ, Kokkotou E. (2013) Increased susceptibility of melanin-concentrating hormone-deficient mice to infection with Salmonella enterica serovar Typhimurium. Infect Immun, 81 (1): 166-72. [PMID:23115043]
39. Kasai S, Kamata M, Masada S, Kunitomo J, Kamaura M, Okawa T, Takami K, Ogino H, Nakano Y, Ashina S et al.. (2012) Synthesis, structure-activity relationship, and pharmacological studies of novel melanin-concentrating hormone receptor 1 antagonists 3-aminomethylquinolines: reducing human ether-a-go-go-related gene (hERG) associated liabilities. J Med Chem, 55 (9): 4336-51. [PMID:22490048]
40. Kobayashi Y, Hamamoto A, Hirayama T, Saito Y. (2015) Molecular cloning, expression, and signaling pathway of four melanin-concentrating hormone receptors from Xenopus tropicalis. Gen Comp Endocrinol, 212: 114-23. [PMID:24662390]
41. Kokkotou E, Espinoza DO, Torres D, Karagiannides I, Kosteletos S, Savidge T, O'Brien M, Pothoulakis C. (2009) Melanin-concentrating hormone (MCH) modulates C difficile toxin A-mediated enteritis in mice. Gut, 58 (1): 34-40. [PMID:18824554]
42. Kokkotou EG, Tritos NA, Mastaitis JW, Slieker L, Maratos-Flier E. (2001) Melanin-concentrating hormone receptor is a target of leptin action in the mouse brain. Endocrinology, 142 (2): 680-6. [PMID:11159839]
43. Kolakowski Jr LF, Jung BP, Nguyen T, Johnson MP, Lynch KR, Cheng R, Heng HH, George SR, O'Dowd BF. (1996) Characterization of a human gene related to genes encoding somatostatin receptors. FEBS Lett, 398 (2-3): 253-8. [PMID:8977118]
44. Konadhode RR, Pelluru D, Blanco-Centurion C, Zayachkivsky A, Liu M, Uhde T, Glen Jr WB, van den Pol AN, Mulholland PJ, Shiromani PJ. (2013) Optogenetic stimulation of MCH neurons increases sleep. J Neurosci, 33 (25): 10257-63. [PMID:23785141]
45. Kowalski TJ, Farley C, Cohen-Williams ME, Varty G, Spar BD. (2004) Melanin-concentrating hormone-1 receptor antagonism decreases feeding by reducing meal size. Eur J Pharmacol, 497 (1): 41-7. [PMID:15321733]
46. Lagos P, Monti JM, Jantos H, Torterolo P. (2012) Microinjection of the melanin-concentrating hormone into the lateral basal forebrain increases REM sleep and reduces wakefulness in the rat. Life Sci, 90 (23-24): 895-9. [PMID:22579511]
47. Lagos P, Torterolo P, Jantos H, Chase MH, Monti JM. (2009) Effects on sleep of melanin-concentrating hormone (MCH) microinjections into the dorsal raphe nucleus. Brain Res, 1265: 103-10. [PMID:19230831]
48. Lakaye B, Minet A, Zorzi W, Grisar T. (1998) Cloning of the rat brain cDNA encoding for the SLC-1 G protein-coupled receptor reveals the presence of an intron in the gene. Biochim Biophys Acta, 1401: 216-220. [PMID:9531978]
49. Lalonde R, Qian S. (2007) Exploratory activity, motor coordination, and spatial learning in Mchr1 knockout mice. Behav Brain Res, 178: 293-304. [PMID:17270288]
50. Lembo PM, Grazzini E, Cao J, Hubatsch DA, Pelletier M, Hoffert C, St-Onge S, Pou C, Labrecque J, Groblewski T et al.. (1999) The receptor for the orexigenic peptide melanin-concentrating hormone is a G-protein-coupled receptor. Nat Cell Biol, 1 (5): 267-71. [PMID:10559938]
51. Lim CJ, Kim SH, Lee BH, Oh KS, Yi KY. (2012) 4-arylphthalazin-1(2H)-one derivatives as potent antagonists of the melanin concentrating hormone receptor 1 (MCH-R1). Bioorg Med Chem Lett, 22 (1): 427-30. [PMID:22137790]
52. Logan DW, Bryson-Richardson RJ, Pagán KE, Taylor MS, Currie PD, Jackson IJ. (2003) The structure and evolution of the melanocortin and MCH receptors in fish and mammals. Genomics, 81 (2): 184-91. [PMID:12620396]
53. Lynch JK, Freeman JC, Judd AS, Iyengar R, Mulhern M, Zhao G, Napier JJ, Wodka D, Brodjian S, Dayton BD et al.. (2006) Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety. J Med Chem, 49 (22): 6569-84. [PMID:17064075]
54. Marsh DJ, Weingarth DT, Novi DE, Chen HY, Trumbauer ME, Chen AS, Guan XM, Jiang MM, Feng Y, Camacho RE et al.. (2002) Melanin-concentrating hormone 1 receptor-deficient mice are lean, hyperactive, and hyperphagic and have altered metabolism. Proc Natl Acad Sci USA, 99 (5): 3240-5. [PMID:11867747]
55. Miyamoto-Matsubara M, Chung S, Saito Y. (2010) Functional interaction of regulator of G protein signaling-2 with melanin-concentrating hormone receptor 1. Ann N Y Acad Sci, 1200: 112-9. [PMID:20633139]
56. Miyamoto-Matsubara M, Saitoh O, Maruyama K, Aizaki Y, Saito Y. (2008) Regulation of melanin-concentrating hormone receptor 1 signaling by RGS8 with the receptor third intracellular loop. Cell Signal, 20 (11): 2084-94. [PMID:18760349]
57. Miyoshi K, Kasahara K, Miyazaki I, Asanuma M. (2009) Lithium treatment elongates primary cilia in the mouse brain and in cultured cells. Biochem Biophys Res Commun, 388 (4): 757-62. [PMID:19703416]
58. Mizusawa K, Amiya N, Yamaguchi Y, Takabe S, Amano M, Breves JP, Fox BK, Grau EG, Hyodo S, Takahashi A. (2012) Identification of mRNAs coding for mammalian-type melanin-concentrating hormone and its receptors in the scalloped hammerhead shark Sphyrna lewini. Gen Comp Endocrinol, 179 (1): 78-87. [PMID:22884735]
59. Mizusawa K, Saito Y, Wang Z, Kobayashi Y, Matsuda K, Takahashi A. (2009) Molecular cloning and expression of two melanin-concentrating hormone receptors in goldfish. Peptides, 30 (11): 1990-6. [PMID:19397943]
60. Morganstern I, Chang GQ, Chen YW, Barson JR, Zhiyu Y, Hoebel BG, Leibowitz SF. (2010) Role of melanin-concentrating hormone in the control of ethanol consumption: Region-specific effects revealed by expression and injection studies. Physiol Behav, 101 (4): 428-37. [PMID:20670637]
61. Mori M, Harada M, Terao Y, Sugo T, Watanabe T, Shimomura Y, Abe M, Shintani Y, Onda H, Nishimura O et al.. (2001) Cloning of a novel G protein-coupled receptor, SLT, a subtype of the melanin-concentrating hormone receptor. Biochem Biophys Res Commun, 283 (5): 1013-8. [PMID:11355873]
62. Murdoch H, Feng GJ, Bächner D, Ormiston L, White JH, Richter D, Milligan G. (2005) Periplakin interferes with G protein activation by the melanin-concentrating hormone receptor-1 by binding to the proximal segment of the receptor C-terminal tail. J Biol Chem, 280 (9): 8208-20. [PMID:15590649]
63. Nagasaki H, Chung S, Dooley CT, Wang Z, Li C, Saito Y, Clark SD, Houghten RA, Civelli O. (2009) The pharmacological properties of a novel MCH1 receptor antagonist isolated from combinatorial libraries. Eur J Pharmacol, 602 (2-3): 194-202. [PMID:19041642]
64. Nagel JM, Geiger BM, Karagiannis AK, Gras-Miralles B, Horst D, Najarian RM, Ziogas DC, Chen X, Kokkotou E. (2012) Reduced intestinal tumorigenesis in APCmin mice lacking melanin-concentrating hormone. PLoS ONE, 7 (7): e41914. [PMID:22848656]
65. Pachoud B, Adamantidis A, Ravassard P, Luppi PH, Grisar T, Lakaye B, Salin PA. (2010) Major impairments of glutamatergic transmission and long-term synaptic plasticity in the hippocampus of mice lacking the melanin-concentrating hormone receptor-1. J Neurophysiol, 104 (3): 1417-25. [PMID:20592115]
66. Pissios P, Ozcan U, Kokkotou E, Okada T, Liew CW, Liu S, Peters JN, Dahlgren G, Karamchandani J, Kudva YC et al.. (2007) Melanin concentrating hormone is a novel regulator of islet function and growth. Diabetes, 56 (2): 311-9. [PMID:17259374]
67. Pissios P, Trombly DJ, Tzameli I, Maratos-Flier E. (2003) Melanin-concentrating hormone receptor 1 activates extracellular signal-regulated kinase and synergizes with G(s)-coupled pathways. Endocrinology, 144 (8): 3514-23. [PMID:12865333]
68. Qu D, Ludwig DS, Gammeltoft S, Piper M, Pelleymounter MA, Cullen MJ, Mathes WF, Przypek R, Kanarek R, Maratos-Flier E. (1996) A role for melanin-concentrating hormone in the central regulation of feeding behaviour. Nature, 380 (6571): 243-7. [PMID:8637571]
69. Rossi M, Choi SJ, O'Shea D, Miyoshi T, Ghatei MA, Bloom SR. (1997) Melanin-concentrating hormone acutely stimulates feeding, but chronic administration has no effect on body weight. Endocrinology, 138 (1): 351-5. [PMID:8977423]
70. Sailer AW, Sano H, Zeng Z, McDonald TP, Pan J, Pong SS, Feighner SD, Tan CP, Fukami T, Iwaasa H et al.. (2001) Identification and characterization of a second melanin-concentrating hormone receptor, MCH-2R. Proc Natl Acad Sci USA, 98 (13): 7564-9. [PMID:11404457]
71. Saito Y, Cheng M, Leslie FM, Civelli O. (2001) Expression of the melanin-concentrating hormone (MCH) receptor mRNA in the rat brain. J Comp Neurol, 435 (1): 26-40. [PMID:11370009]
72. Saito Y, Nothacker HP, Wang Z, Lin SH, Leslie F, Civelli O. (1999) Molecular characterization of the melanin-concentrating-hormone receptor. Nature, 400 (6741): 265-9. [PMID:10421368]
73. Saito Y, Wang Z, Hagino-Yamagishi K, Civelli O, Kawashima S, Maruyama K. (2001) Endogenous melanin-concentrating hormone receptor SLC-1 in human melanoma SK-MEL-37 cells. Biochem Biophys Res Commun, 289 (1): 44-50. [PMID:11708774]
74. Sakurai T, Ogawa K, Ishihara Y, Kasai S, Nakayama M. (2014) The MCH(1) receptor, an anti-obesity target, is allosterically inhibited by 8-methylquinoline derivatives possessing subnanomolar binding and long residence times. Br J Pharmacol, 171 (5): 1287-98. [PMID:24670150]
75. Sears RM, Liu RJ, Narayanan NS, Sharf R, Yeckel MF, Laubach M, Aghajanian GK, DiLeone RJ. (2010) Regulation of nucleus accumbens activity by the hypothalamic neuropeptide melanin-concentrating hormone. J Neurosci, 30 (24): 8263-73. [PMID:20554878]
76. Shearman LP, Camacho RE, Sloan Stribling D, Zhou D, Bednarek MA, Hreniuk DL, Feighner SD, Tan CP, Howard AD, Van der Ploeg LH et al.. (2003) Chronic MCH-1 receptor modulation alters appetite, body weight and adiposity in rats. Eur J Pharmacol, 475 (1-3): 37-47. [PMID:12954357]
77. Shimomura Y, Mori M, Sugo T, Ishibashi Y, Abe M, Kurokawa T, Onda H, Nishimura O, Sumino Y, Fujino M. (1999) Isolation and identification of melanin-concentrating hormone as the endogenous ligand of the SLC-1 receptor. Biochem Biophys Res Commun, 261: 622-626. [PMID:10441476]
78. 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, 31 (6): 1135-45. [PMID:16205780]
79. Suply T, Della Zuana O, Audinot V, Rodriguez M, Beauverger P, Duhault J, Canet E, Galizzi JP, Nahon JL, Levens N et al.. (2001) SLC-1 receptor mediates effect of melanin-concentrating hormone on feeding behavior in rat: a structure-activity study. J Pharmacol Exp Ther, 299 (1): 137-46. [PMID:11561073]
80. Suzuki T, Kameda M, Ando M, Miyazoe H, Sekino E, Ito S, Masutani K, Kamijo K, Takezawa A, Moriya M et al.. (2009) Discovery of novel diarylketoxime derivatives as selective and orally active melanin-concentrating hormone 1 receptor antagonists. Bioorg Med Chem Lett, 19 (18): 5339-45. [PMID:19683441]
81. Takahashi A, Kosugi T, Kobayashi Y, Yamanome T, Schiöth HB, Kawauchi H. (2007) The melanin-concentrating hormone receptor 2 (MCH-R2) mediates the effect of MCH to control body color for background adaptation in the barfin flounder. Gen Comp Endocrinol, 151 (2): 210-9. [PMID:17324419]
82. Takekawa S, Asami A, Ishihara Y, Terauchi J, Kato K, Shimomura Y, Mori M, Murakoshi H, Kato K, Suzuki N et al.. (2002) T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist. Eur J Pharmacol, 438 (3): 129-35. [PMID:11909603]
83. Tavares FX, Al-Barazanji KA, Bishop MJ, Britt CS, Carlton DL, Cooper JP, Feldman PL, Garrido DM, Goetz AS, Grizzle MK et al.. (2006) 6-(4-chlorophenyl)-3-substituted-thieno[3,2-d]pyrimidin-4(3H)-one-based melanin-concentrating hormone receptor 1 antagonist. J Med Chem, 49 (24): 7108-18. [PMID:17125263]
84. Tsunematsu T, Ueno T, Tabuchi S, Inutsuka A, Tanaka KF, Hasuwa H, Kilduff TS, Terao A, Yamanaka A. (2014) Optogenetic manipulation of activity and temporally controlled cell-specific ablation reveal a role for MCH neurons in sleep/wake regulation. J Neurosci, 34 (20): 6896-909. [PMID:24828644]
85. Tyhon A, Lakaye B, Adamantidis A, Tirelli E. (2008) Amphetamine- and cocaine-induced conditioned place preference and concomitant psychomotor sensitization in mice with genetically inactivated melanin-concentrating hormone MCH(1) receptor. Eur J Pharmacol, 599 (1-3): 72-80. [PMID:18848539]
86. Verlaet M, Adamantidis A, Coumans B, Chanas G, Zorzi W, Heinen E, Grisar T, Lakaye B. (2002) Human immune cells express ppMCH mRNA and functional MCHR1 receptor. FEBS Lett, 527 (1-3): 205-10. [PMID:12220661]
87. Wang S, Behan J, O'Neill K, Weig B, Fried S, Laz T, Bayne M, Gustafson E, Hawes BE. (2001) Identification and pharmacological characterization of a novel human melanin-concentrating hormone receptor, mch-r2. J Biol Chem, 276 (37): 34664-70. [PMID:11459838]
88. Willie JT, Sinton CM, Maratos-Flier E, Yanagisawa M. (2008) Abnormal response of melanin-concentrating hormone deficient mice to fasting: hyperactivity and rapid eye movement sleep suppression. Neuroscience, 156 (4): 819-29. [PMID:18809470]
89. Witty DR, Bateson J, Hervieu GJ, Al-Barazanji K, Jeffrey P, Hamprecht D, Haynes A, Johnson CN, Muir AI, O'Hanlon PJ et al.. (2006) Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849. Bioorg Med Chem Lett, 16 (18): 4872-8. [PMID:16839763]
90. Wu M, Dumalska I, Morozova E, van den Pol A, Alreja M. (2009) Melanin-concentrating hormone directly inhibits GnRH neurons and blocks kisspeptin activation, linking energy balance to reproduction. Proc Natl Acad Sci USA, 106 (40): 17217-22. [PMID:19805188]
91. Ziogas DC, Gras-Miralles B, Mustafa S, Geiger BM, Najarian RM, Nagel JM, Flier SN, Popov Y, Tseng YH, Kokkotou E. (2013) Anti-melanin-concentrating hormone treatment attenuates chronic experimental colitis and fibrosis. Am J Physiol Gastrointest Liver Physiol, 304 (10): G876-84. [PMID:23538494]