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Target not currently curated in GtoImmuPdb

Target id: 110

Nomenclature: GPR61

Family: Class A Orphans

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 451 1p13.3 GPR61 G protein-coupled receptor 61 1
Mouse 7 449 3 F2.3 Gpr61 G protein-coupled receptor 61
Rat 7 449 2q34 Gpr61 G protein-coupled receptor 61
Previous and Unofficial Names Click here for help
GPCR3 | BALGR | biogenic amine receptor-like GPCR
Database Links Click here for help
Specialist databases
GPCRDB gpr61_human (Hs), gpr61_mouse (Mm)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
RefSeq Nucleotide
RefSeq Protein
Antagonist Comments
Although no endogenous ligands have been identified, 5-(nonyloxy)tryptamine has been reported to be a low affinity inverse agonist [3].
Primary Transduction Mechanisms Click here for help
Comments:  Possibly Gs-coupled. The receptor displays constitutive activity that is abolished by deletion of the N-terminal 25 amino acids [4].
References:  4
Tissue Distribution Click here for help
Brain, testes
Species:  Human
Technique:  Semi-quantitative PCR
References:  1
Cerebral cortex, occipital pole, frontal lobe, temporal lobe, amygdala, hippocampus (lower expression in putamen and caudate nucleus)
Species:  Human
Technique:  Northern blot
References:  1
Dentate gyrus, hippocampus, cerebral cortex (moderate to weak expression in hypothalamus, central amygdala, nucleus accumbens and nucleus tractus solitarius)
Species:  Mouse
Technique:  RT-PCR
References:  2
Expression Datasets Click here for help

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Physiological Consequences of Altering Gene Expression Click here for help
GPR61 deficient mice exhibit obesity associated with hyperphagia. Significantly lower mRNA levels of pro-opiomelanocortin and brain-derived neurotropic factor mRNAs in hypothalamus compared to wild type. Phenotype displayed: hyperphagia, increased visceral fat pad weight, increased liver weight and triglyceride content, increased plasma leptin and insulin levels.
Species:  Mouse
Tissue:  Live, adipose, plasma
Technique:  Targeted gene disruption
References:  2
Gene Expression and Pathophysiology Comments
Mouse models of GPR61 disruption indicate a role for the receptor in regulation of appetite and body weight, indicating that the receptor may be a therapeutic target for obesity and eating disorders.
Biologically Significant Variants Click here for help
Type:  Naturally occurring SNP
Species:  Human
Amino acid change:  L218P
Comment on frequency:  Low frequency (<10% in all tested populations)
SNP accession: 
General Comments
Site-directed mutagenesis studies suggest a possible role for the N-terminal 25 amino acids of the receptor in constitutive activity and for membrane translocation of the receptor [4].


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1. Cikos S, Gregor P, Koppel J. (2001) Cloning of a novel biogenic amine receptor-like G protein-coupled receptor expressed in human brain. Biochim Biophys Acta, 1521 (1-3): 66-72. [PMID:11690637]

2. Nambu H, Fukushima M, Hikichi H, Inoue T, Nagano N, Tahara Y, Nambu T, Ito J, Ogawa Y, Ozaki S et al.. (2011) Characterization of metabolic phenotypes of mice lacking GPR61, an orphan G-protein coupled receptor. Life Sci, 89 (21-22): 765-72. [PMID:21971119]

3. Takeda S, Okada T, Okamura M, Haga T, Isoyama-Tanaka J, Kuwahara H, Minamino N. (2004) The receptor-Galpha fusion protein as a tool for ligand screening: a model study using a nociceptin receptor-Galphai2 fusion protein. J Biochem, 135 (5): 597-604. [PMID:15173198]

4. Toyooka M, Tujii T, Takeda S. (2009) The N-terminal domain of GPR61, an orphan G-protein-coupled receptor, is essential for its constitutive activity. J Neurosci Res, 87 (6): 1329-33. [PMID:19025769]


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