Melanin-concentrating hormone receptor

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 humans.

Clinical significance

Antagonists might be useful in the treatment of obesity and anxiety and depression. An agonist might have possible utility as a treatment for osteoporosis and insomnia

Research is ongoing for antagonists affecting MCH receptors R1 and R2.

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. doi:10.2165/00023210-200620100-00002. PMID 16999451. S2CID 32524553.
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.
Monti JM, Torterolo P, Lagos P (August 2013). "Melanin-concentrating hormone control of sleep-wake behavior". Sleep Med Rev. 17 (4): 293–8. doi:10.1016/j.smrv.2012.10.002. PMID 23477948.
Saito Y, Maruyama K (2006). "Identification of melanin-concentrating hormone receptor and its impact on drug discovery". Journal of Experimental Zoology Part A: Comparative Experimental Biology. 305 (9): 761–8. Bibcode:2006JEZA..305..761S. 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

"Melanin-Concentrating Hormone Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived from the original on 2016-03-03. Retrieved 2007-10-25.
melanin-concentrating+hormone+receptor at the U.S. National Library of Medicine Medical Subject Headings (MeSH)
MCHR1+protein,+human at the U.S. National Library of Medicine Medical Subject Headings (MeSH)
MCHR2+protein,+human at the U.S. National Library of Medicine Medical Subject Headings (MeSH)

Cell surface receptor: G protein-coupled receptors

Class A: Rhodopsin-like

Neurotransmitter

Adrenergic	α1 (A B D) α2 (A B C) β1 β2 β3
Purinergic	Adenosine (A1 A2A A2B A3) P2Y (1 2 4 5 6 8 9 10 11 12 13 14)
Serotonin	(all but 5-HT3) 5-HT1 (A B D E F) 5-HT2 (A B C) 5-HT (4 5A 6 7)
Other	Acetylcholine (M1 M2 M3 M4 M5) Dopamine D1 D2 D3 D4 D5 GHB receptor Histamine H1 H2 H3 H4 Melatonin (1A 1B 1C) TAAR (1 2 5 6 8 9)

Metabolites and
signaling molecules

Eicosanoid	CysLT (1 2) LTB4 1 2 FPRL1 OXE Prostaglandin DP (1 2), EP (1 2 3 4), FP Prostacyclin Thromboxane
Other	Bile acid Cannabinoid (CB1 CB2, GPR (18 55 119)) EBI2 Estrogen Free fatty acid (1 2 3 4) Hydroxycarboxylic acids 1 2 3 Lysophosphatidic acid (1 2 3 4 5 6) Lysophospholipid (1 2 3 4 5 6 7 8) Oxoglutarate PAF Sphingosine-1-phosphate (1 2 3 4 5) Succinate

Peptide

Neuropeptide

B/W (1
2)
FF (1
2)
S
Y (1
2
4
5)
Neuromedin (B
U (1
2))
Neurotensin (1
2)

Other

Anaphylatoxin (C3a
C5a (1
2))
Angiotensin (1
2)
Apelin
Bombesin
- BRS3
- GRPR
- NMBR)
- Bradykinin (B1
- B2)
Chemokine
Cholecystokinin (A
B)
Endothelin
- A
- B
Formyl peptide (1
2
3)
FSH
Galanin (1
2
3)
Gonadotropin-releasing hormone (1
2)
Ghrelin
Kisspeptin
Luteinizing hormone/choriogonadotropin
MAS (1
1L
D
E
F
G
X1
X2
X3
X4)
Melanocortin (1
2
3
4
5)
MCHR (1
2)
Motilin
Opioid (Delta
Kappa
Mu
Nociceptin & Zeta, but not Sigma)
Orexin (1
2)
Oxytocin
Prokineticin (1
2)
Prolactin-releasing peptide
Relaxin (1
2
3
4)
Somatostatin (1
2
3
4
5)
Tachykinin (1
2
3)
Thyrotropin
Thyrotropin-releasing hormone
Urotensin-II
Vasopressin (1A
1B
2)

Miscellaneous

Taste, bitter	TAS2R 1 3 4 5 7 8 9 10 13 14 16 19 20 30 31 38 39 40 41 42 43 45 46 50 60 Vomeronasal receptor type 1
Orphan	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 78 81 82 83 84 85 87 88 92 101 103 109A 109B 119 120 132 135 137B 139 141 142 146 148 149 150 151 152 153 160 161 162 171 173 174 176 177 182 183)
Other	Adrenomedullin Olfactory Opsin (3 4 5 1LW 1MW 1SW RGR RRH) Protease-activated (1 2 3 4) SREB (1 2 3)

Class B: Secretin-like

Adhesion	ADGRB Brain-specific angiogenesis inhibitor 1 2 3 ADGRC Cadherin 1 2 3 ADGRE EMR 1 2 3 CD97 ADGRG 1 2 3 4 5 6 7 ADGRL Latrophilin 1 2 3 ELTD1
Orphan	GPR (56 64 97 98 110 111 112 113 114 115 116 123 124 125 126 128 133 143 144 155 157)
Other	Calcitonin CALCRL Corticotropin-releasing hormone (1 2) Glucagon (GR GIPR GLP1R GLP2R) Growth-hormone-releasing hormone PACAPR1 GPR Methuselah-like proteins Parathyroid hormone (1 2) Secretin Vasoactive intestinal peptide (1 2)

Class C: Metabotropic glutamate / pheromone

Taste, sweet	TAS1R 1 2 3 Vomeronasal receptor, type 2
Other	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)

Class F: Frizzled & Smoothened

Frizzled	Frizzled (1 2 3 4 5 6 7 8 9 10)
Smoothened	Smoothened

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Categories:

Clinical significance

See also

References

External links