Melanin-concentrating hormone receptor

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melanin-concentrating hormone receptor 1
Identifiers
Symbol	MCHR1
Alt. Symbols	GPR24
Entrez	2847
HUGO	4479
OMIM	601751
RefSeq	NM_005297
UniProt	Q99705
Other data
Locus	Chr. 22 q13.3

melanin-concentrating hormone receptor 2
Identifiers
Symbol	MCHR2
Alt. Symbols	GPR145
Entrez	84539
HUGO	20867
OMIM	606111
RefSeq	NM_032503
UniProt	Q969V1
Other data
Locus	Chr. 6 q16

Two Melanin-concentrating hormone receptors (MCHR) have recently been characterized: MCH-R1 and MCH-R2. These two receptors share approximately 38% homology.

MCH-R1 is expressed in all mammals.
MCH-R2 is only found in some primates and carnivores including dogs, ferrets and man.

Clinical significance

Antagonists might be useful in the treatment of obesity^[1]^[2] and anxiety and depression.^[3] An agonist might have possible utility as a treatment for osteoporosis.^[4]

Research is ongoing for antagonists affecting MCH receptors R1 and R2.^[5]^[6]

References

↑ Handlon AL, Zhou H (2006). "Melanin-concentrating hormone-1 receptor antagonists for the treatment of obesity". J. Med. Chem. 49 (14): 4017–22. doi:10.1021/jm058239j. PMID 16821761.
↑ Luthin DR (2007). "Anti-obesity effects of small molecule melanin-concentrating hormone receptor 1 (MCHR1) antagonists". Life Sci. 81 (6): 423–40. doi:10.1016/j.lfs.2007.05.029. PMID 17655875.
↑ 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.
↑ Bohlooly-Y M, Mahlapuu M, Andersén H, Astrand A, Hjorth S, Svensson L, Törnell J, Snaith MR, Morgan DG, Ohlsson C (2004). "Osteoporosis in MCHR1-deficient mice". Biochem. Biophys. Res. Commun. 318 (4): 964–9. doi:10.1016/j.bbrc.2004.04.122. PMID 15147966.
↑ Saito Y, Maruyama K (2006). "Identification of melanin-concentrating hormone receptor and its impact on drug discovery". J. Exp. Zoolog. Part A Comp. Exp. Biol. 305 (9): 761–8. doi:10.1002/jez.a.311. PMID 16902961.
↑ McBriar MD (2006). "Recent advances in the discovery of melanin-concentrating hormone receptor antagonists". Current opinion in drug discovery & development 9 (4): 496–508. PMID 16889232.

External links

v • d • e Transmembrane receptor: G protein-coupled receptors
Class A: Rhodopsin like	Acetylcholine (M1, M2, M3, M4, M5) - Adrenergic (α1 (A, B, D), α2 (A, B, C), β1, β2, β3) - Adrenomedullin - Anaphylatoxin (C3a, C5a) - Angiotensin (1, 2) - Apelin - Bile acid - Bombesin (BRS3, GRPR, NMBR) - Bradykinin (B1, B2) - Cannabinoid (CB1, CB2) - Chemokine - Cholecystokinin (A, B) - Dopamine (D1, D2, D3, D4, D5) - Eicosanoid (CysLT (1, 2), LTB4 (1, 2), FPRL1, OXE, Prostaglandin ((DP (1, 2), EP (1, 2, 3, 4), PGF, Prostacyclin, Thromboxane) - EBI2 - Endothelin (A, B) - Estrogen - Formyl peptide (1, L1, L2) - Free fatty acid (1, 2, 3, 4) - FSH - Galanin (1, 2, 3) - Gonadotropin-releasing hormone (1, 2) - GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 79, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172, 173, 174, 176, 182) - Ghrelin - Histamine (H1, H2, H3, H4) - Kisspeptin - Luteinizing hormone/choriogonadotropin - Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) - MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) - Melanocortin (1, 2, 3, 4, 5) - MCHR (1, 2) - Melatonin (1A, 1B)- Motilin - Neuromedin (B, U (1, 2)) - Neuropeptide (B/W (1, 2), FF (1, 2), S, Y (1, 2, 4, 5)) - Neurotensin (1, 2) - Opioid (Delta, Kappa, Mu, Nociceptin, but not Sigma) - Olfactory - Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) - Orexin (1, 2) - Oxytocin - Oxoglutarate - PAF - Prokineticin (1, 2) - Prolactin-releasing peptide - Protease-activated (1, 2, 3, 4) - Purinergics (Adenosine (A1, A2a, A2b, A3), P2Y, (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)) - Relaxin (1, 2, 3, 4) - Somatostatin (1, 2, 3, 4, 5) - Serotonin, all but 5-HT3 (5-HT1 (A, B, D, E, F), 5-HT2 (A, B, C), 5-HT (4, 5A, 6, 7)) - SREB - Succinate - TAAR (1, 2, 3, 5, 6, 8, 9) - Tachykinin (1, 2, 3) - Thyrotropin - Thyrotropin-releasing hormone - Urotensin-II - Vasopressin (1A, 1B, 2)
Class B: Secretin like	Brain-specific angiogenesis inhibitor (1, 2, 3) - Cadherin (1, 2, 3) - Calcitonin - CD97 - Corticotropin-releasing hormone (1, 2) - EMR (1, 2, 3) - Glucagon (GR, GIPR, GLP1R, GLP2R) - Growth hormone releasing hormone - PACAPR1- GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157) - Latrophilin (1, 2, 3, ELTD1) - Parathyroid hormone (1, 2) - Secretin - Vasoactive intestinal peptide (1, 2)
Class C: Metabotropic glutamate / pheromone	Calcium-sensing receptor - GABA B (1, 2) - Glutamate receptor (Metabotropic glutamate (1, 2, 3, 4, 5, 6, 7, 8)) - GPRC6A - GPR (156, 158, 179) - RAIG (1, 2, 3, 4) - Taste receptors (TAS1R (1, 2, 3) TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50))
Frizzled / Smoothened	Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) - Smoothened