Nomenclature: MCH2 receptor

Family: Melanin-concentrating hormone receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates. 

Contents

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 340 6q16.3 MCHR2 melanin-concentrating hormone receptor 2 1,4,6-7
Previous and Unofficial Names
S643b
GPR145
gpr 145
MCHR2
MCH-2R
SLT
GPRv17
MCH2
MCH2R
G protein-coupled receptor 145
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
GPCRDB
GeneCards
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
OMIM
PharmGKB Gene
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
Natural/Endogenous Ligands
melanin-concentrating hormone {Sp: Human, Mouse, Rat}
Rank order of potency (Human)
melanin-concentrating hormone (PMCH, P20382) = MCH (salmon)  [4]
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[Phe13,Tyr19]MCH Hs Full agonist 8.4 – 9.2 pIC50 8-9
pIC50 8.4 – 9.2 [8-9]
melanin-concentrating hormone {Sp: Human, Mouse, Rat} Hs Full agonist 8.2 – 9.2 pIC50 8
pIC50 8.2 – 9.2 [8]
Ac-hMCH-(6-16)-NH2 Hs Full agonist 8.4 – 8.8 pIC50 2
pIC50 8.4 – 8.8 [2]
MCH (salmon) Hs Full agonist 6.2 – 7.1 pIC50 8-9
pIC50 6.2 – 7.1 [8-9]
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[Ava9,10,Ava14,15]-Ac-hMCH6-16-NH2 Hs Antagonist 7.3 pIC50 2
pIC50 7.3 [2]
ATC0065 Hs Antagonist 5.8 – 5.9 pIC50 3
pIC50 5.8 – 5.9 [3]
Primary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Adenylate cyclase inhibition
Phospholipase C stimulation
References:  8
Tissue Distribution
Brain; frontal lobe, temporal lobe, occipital lobe, precentral gyrus, pons, hippocampus, amygdala, putamen, and the caudate nucleus, with relatively high levels in the cerebral cortex > thalamus, corpus callosum, and medulla oblongata.

Hypothalamus, adipocytes, pituitary, and pancreas.
Species:  Human
Technique:  RT-PCR, Northern hybridization and RNA dot array blot hybridization.
References:  1
Brain; arcuate nucleus and ventral medial hypothalamus.
Species:  Human
Technique:  Northern Blot and in situ hybridization.
References:  8
Brain (cortex, occipital lobe, frontal lobe, temporal lobe, parietal lobe, paracentral gyrus, cerebellum, amygdala, hippocampus, accumbens nucleus, thalamus).
Species:  Human
Technique:  Northern and dot blot.
References:  9
Brain > adipose tissue > prostate, lymphocytes, intestine. Cingulate gyrus > nucleus accumbens > medial frontal gyrus > superior frontal gyrus.
Species:  Human
Technique:  Quantitative RT-PCR.
References:  4
Brain (temporal lobe, cerebral cortex > hippocampus, parietal lobe, amygdala, corpus callosum, occipital lobe, frontal lobe, caudate nucleus) > tetis.
Species:  Human
Technique:  Quantitative RT-PCR.
References:  6-7
Hypothalamus (paraventricular nucleus (magnocellular part), dorsomedial, ventromedial, and arcuate nucleus), olfactory pathway, nucleus of the solitary tract.

Thyroid, kidney, lung, testis.
Species:  Mouse
Technique:  in situ hybridization.
References:  5
Functional Assays
Measurement of inositol phosphate turnover.
Species:  Human
Tissue: 
Response measured:  Stimulation of inositol phosphate turnover.
References:  8
Measurement of IP3 production in CHO cells transfected with the human NCH2 receptors.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of IP3 production.
References:  8-9
Measurement of intracellular Ca2+ levels in CHO cells transfected with the human MCH2 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Increase in intracellular Ca2+.
References:  7-9
Measurement of intracellular Ca2+ levels in HEK 293 cells transfected with the human MCH2 receptor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Increase in intracellular Ca2+.
References:  4,8
Measurement of cellular extrusion of protons in HEK 293 cells transfected with the human MHC2 receptor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Increase in cellular extrusion of protons.
References:  4
Available Assays
DiscoveRx PathHunter® eXpress MCHR2 U2OS β-Arrestin GPCR Assay (Cat no. 93-0691E3CP5M)
PathHunter® U2OS MCHR2 β-Arrestin Cell Line (Cat no. 93-0691C3)
more info

REFERENCES

1. An S, Cutler G, Zhao JJ, Huang SG, Tian H, Li W, Liang L, Rich M, Bakleh A, Du J, Chen JL, Dai K. (2001) Identification and characterization of a melanin-concentrating hormone receptor. Proc Natl Acad Sci U S A98: 7576-7581. [PMID:11416225]

2. 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. Biochemistry41: 6383-6390. [PMID:12009900]

3. 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 Ther313: 831-839. [PMID:15677346]

4. Hill J, Duckworth M, Murdock P, Rennie G, Sabido-David C, Ames RS, Szekeres P, Wilson S, Bergsma DJ, Gloger IS, Levy DS, Chambers JK, Muir AI. (2001) Molecular cloning and functional characterization of MCH2, a novel human MCH receptor. J Biol Chem276: 20125-20129. [PMID:11274220]

5. 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. Endocrinology142: 680-686. [PMID:11159839]

6. Mori M, Harada M, Terao Y, Sugo T, Watanabe T, Shimomura Y, Abe M, Shintani Y, Onda H, Nishimura O, Fujino M. (2001) Cloning of a novel G protein-coupled receptor, SLT, a subtype of the melanin-concentrating hormone receptor. Biochem Biophys Res Commun283: 1013-1018. [PMID:11355873]

7. Rodriguez M, Beauverger P, Naime I, Rique H, Ouvry C, Souchaud S, Dromaint S, Nagel N, Suply T, Audinot V, Boutin JA, Galizzi JP. (2001) Cloning and molecular characterization of the novel human melanin-concentrating hormone receptor MCH2. Mol Pharmacol60: 632-639. [PMID:11562423]

8. Sailer AW, Sano H, Zeng Z, McDonald TP, Pan J, Pong SS, Feighner SD, Tan CP, Fukami T, Iwaasa H, Hreniuk DL, Morin NR, Sadowski SJ, Ito M, Ito M, Bansal A, Ky B, Figueroa DJ, Jiang Q, Austin CP, MacNeil DJ, Ishihara A, Ihara M, Kanatani A, Van der Ploeg LH, Howard AD, Liu Q. (2001) Identification and characterization of a second melanin-concentrating hormone receptor, MCH-2R. Proc Natl Acad Sci U S A98: 7564-7569. [PMID:11404457]

9. 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 Chem276: 34664-34670. [PMID:11459838]

To cite this database page, please use the following:

Valérie Audinot, Jean A. Boutin.
Melanin-concentrating hormone receptors: MCH2 receptor. Last modified on 31/07/2010. Accessed on 24/10/2014. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=281.

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