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You are here:Home-Inhibitors & Agonists-GPCR-GPR139

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GPR139 (G protein-coupled receptor 139) is a protein that in humans is encoded by the GPR139 gene. GPR139 is an orphan G-protein–coupled receptor expressed in the central nervous system.

The expression pattern of GPR139 has primarily been studied on the mRNA level and showed expression mainly in the central nervous system.

GPR139 is an orphan receptor identified from bioinformatics analysis of the human genome. GPR139 is thus a potential target for the treatment of Parkinson’s disease, obesity, eating disorders, and/or diabetes.

The GPR139 is expressed specifically in the brain in areas of relevance for motor control. GPR139 function and signal transduction pathways are elusive, and results in the literature are even contradictory. GPR139 agonists dose-dependently protect primary dopaminergic (DA) neurons against MPP+ toxicity.

Cat. No. Product Name CAS No. Information
H3367

JNJ-63533054

 		1802326-66-4

JNJ-63533054 (JNJ63533054) is a potent, selective GPR139 agonist that specifically activates human GPR139 in the calcium mobilization with EC50 of 16 nM; shows similar potency for rat and mouse GPR139 receptor (rat EC50 =63 nM, mouse EC50=28 nM); decreases spontaneous locomotor activity in rats; shows no cross-reactivity in a panel of 50 known GPCRs, ion channels, and transporters, and displays suitable pharmacokinetic properties for in vivo studies; CNS-penetrable and orally bioavailable.
H3366

GPR139 agonist AC4

 		1147746-85-7

GPR139 agonist AC4 is a novel small molecule GPR139 receptor agonist with EC50 of 220 nM in calcium mobilization assay in CHO-GPR139 cells.

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