2. Signaling Pathways
  3. GPCR/G Protein
  4. GPR6

GPR6

G Protein-Coupled Receptor 6

GPR6 is an orphan G protein-coupled receptor that has been associated with the cannabinoid family because of its recognition of a sub-set of cannabinoid ligands. GPR6 is highly expressed in human striatum and hypothalamus. GPR6 has been suggested as a possible target for the treatment of several neurodegenerative diseases. Experimental evidence shows that depletion of GPR6 causes both dopamine increase and cAMP decrease in the striatal tissues which are accompanied by improved movement. Knockout of GPR6 in a Parkinson’s disease mice model results in a decrease of the involuntary movements that characterize this disease. In fact, several patents claim the use of pyrazine derivatives as GPR6 inverse agonists for treating Parkinson’s disease symptoms and other dyskinesia syndromes. GPR6 is also involved in other neurological disorders such as Huntington’s and Alzheimer’s Disease. Moreover, instrumental learning has been shown to be impaired in GPR6 knockout mice models.

GPR6 Related Products (4):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-134661A
    Solangepras
    		99.70%
    CVN424 is an orally active and selective GPR6 inverse agonist with a Ki of 9.4 nM and an EC50 of 38 nM. CVN424 is brain-penetrant and has the potential for Parkinson disease research.
    Solangepras
  • HY-134661
    (S)-CVN424
    		99.16%
    (S)-CVN424 is a potent G-Protein-Coupled Receptor 6 (GPR6) modulator. (S)-CVN424 has the potential for a variety of neurological and psychiatric disorders research, including Parkinson's disease.
    (S)-CVN424
  • HY-182011
    GPR6 inverse agonist 2
    		Agonist
    GPR6 inverse agonist 2 (Compound 575) is a selective GPR6 inverse agonist, with IC50 values of < 0.1 μM and 1~30 μM against GPR6 and GPR3, respectively. GPR6 inverse agonist 2 exhibits preliminary cardiac safety, with an IC50 of 21.71 μM for hERG. GPR6 inverse agonist 2 can be used in the research of movement disorders such as Parkinson's disease.
    GPR6 inverse agonist 2
  • HY-181349
    GPR6 inverse agonist 1
    		Agonist
    GPR6 inverse agonist 1 (Compound 101) is a selective GPR6 inverse agonist with an IC50 < 100 nM. GPR6 inverse agonist 1 is applicable to research related to Parkinson's disease and Huntington's disease.
    GPR6 inverse agonist 1