1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. GPR139


G Protein-Coupled Receptor 139

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.

GPR139 Related Products (6):

Cat. No. Product Name Effect Purity
  • HY-19838
    Agonist 99.38%
    JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB).
  • HY-132228
    Agonist 99.63%
    Zelatriazin (TAK-041; NBI-1065846) is a potent and selective GPR139 agonist with an EC50 of 22 nM. Zelatriazin has the potential for the research of negative symptoms associated with schizophrenia.
  • HY-128057
    Antagonist ≥99.0%
    NCRW0005-F05 is a potent GPR139 antagonist with an IC50 value of 0.21 μM. NCRW0005-F05 can be used to research diabetes, obesity and Parkinson's disease.
  • HY-101777
    TC-O 9311
    Agonist 99.70%
    TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM.
  • HY-119168
    Antagonist 99.69%
    LP-471756 is a potent GPR139 antagonist with an IC50 value of 640 nM. LP-471756 inhibits LP-360924-stimulated cAMP production.
  • HY-149651
    GPR139 agonist-2
    GPR139 agonist-2 (compound 20a) is a potent GPR139 agonist with an EC50 of 24.7 nM. GPR139 agonist-2 rescues the social interaction deficits and alleviates cognitive deficits in murine schizophrenia models. GPR139 agonist-2 has the potential for antischizophrenia drug research.