Gene and Protein Information
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

GPCR3 | BALGR | biogenic amine receptor-like GPCR

Database Links
Specialist databases
GPCRdb	gpr61_human (Hs), gpr61_mouse (Mm)
Other databases
Alphafold	Q9BZJ8 (Hs), Q8C010 (Mm)
ChEMBL Target	CHEMBL4523918 (Hs)
Ensembl Gene	ENSG00000156097 (Hs), ENSMUSG00000046793 (Mm), ENSRNOG00000019738 (Rn)
Entrez Gene	83873 (Hs), 229714 (Mm), 310780 (Rn)
Human Protein Atlas	ENSG00000156097 (Hs)
KEGG Gene	hsa:83873 (Hs), mmu:229714 (Mm), rno:310780 (Rn)
OMIM	606916 (Hs)
Pharos	Q9BZJ8 (Hs)
RefSeq Nucleotide	NM_031936 (Hs), NM_175470 (Mm), NM_001107715 (Rn)
RefSeq Protein	NP_114142 (Hs), NP_780679 (Mm), NP_001101185 (Rn)
UniProtKB	Q9BZJ8 (Hs), Q8C010 (Mm)
Wikipedia	GPR61 (Hs)

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols	View all chemical structures	Click column headers to sort
Ligand Sp. Action Value Parameter Reference compound 1 [PMID: 37741852] Hs Inverse agonist 8.0 pIC50 2 ⤷ pIC50 8.0 (IC50 1x10-8 M) [2] Description: Determined using a cAMP assay in cells overexpressing hGPR61

Antagonist Comments

Although no endogenous ligands have been identified, 5-(nonyloxy)tryptamine has been reported to be a low affinity inverse agonist [4].

Primary Transduction Mechanisms
Comments:  Possibly Gs-coupled. The receptor displays constitutive activity that is abolished by deletion of the N-terminal 25 amino acids [5].
References:  5

Tissue Distribution
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:  3

Expression Datasets
Show »« Hide 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] There should be a chart of expression data here, you may need to enable JavaScript!

Physiological Consequences of Altering Gene Expression

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:  3

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
Type:  Naturally occurring SNP Species:  Human Amino acid change:  L218P Comment on frequency:  Low frequency (<10% in all tested populations) SNP accession:  rs75311269

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 [5].