2. Signaling Pathways
  3. GPCR/G Protein
  4. GPR88

GPR88

G Protein-Coupled Receptor 88

GPR88 is an orphan G protein-coupled receptor (GPCR) of the class A rhodopsin family. GPR88 was originally identified as a striatum-specific receptor (designated Strg/GPR88) in both human and rodents, though it is also expressed at low levels in the cerebral cortex, central extended amygdala, lateral, cortical, hypothalamus, and other brain regions.

The specific brain signaling pathways and physiologic functions of GPR88 are largely unknown because the endogenous hormone or transmitter for the receptor has not yet been identified. However, several lines of evidence suggest that GPR88 may provide an important role regulating the excitability of glutamatergic and GABAergic neurons as well as modulating responses to dopaminergic neurons, based on the particularly robust expression of GPR88 in medium spiny neurons (MSNs) in the striatum. Conversely, glutamatergic and dopaminergic depletion differentially alters Gpr88 mRNA levels in distinct MSN subpopulations, indicating neurotransmission regulates Gpr88 gene expression. Consequently, GPR88 is implicated in many behavioral functions and responses, including cognition, mood, movement control, and cued response reward learning.

GPR88 Related Products (9):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-100013A1
    (1R,2R)-2-PCCA hydrochloride
    		98.08%
    (1R,2R)-2-PCCA hydrochloride is a diastereomer of 2-PCCA, and acts as a potent GPR88 receptor agonist, with an EC50 of 3 nM in cell-free assay, and 603 nM in cell assay.
    (1R,2R)-2-PCCA hydrochloride
  • HY-100013C
    2-PCCA hydrochloride
    		99.63%
    2-PCCA hydrochloride is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC50 of 116 nM in HEK293 cells.
    2-PCCA hydrochloride
  • HY-112612A
    RTI-13951-33 hydrochloride
    		98.56%
    RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 hydrochloride reduces alcohol reinforcement and intake behaviors in rats.
    RTI-13951-33 hydrochloride
  • HY-156771
    GPR88-IN-1
    		Inhibitor 99.54%
    GPR88-IN-1 is a GPR88 inhibitor, and can be used for research of central diseases.
    GPR88-IN-1
  • HY-112612
    RTI-13951-33
    RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 reduces alcohol reinforcement and intake behaviors in rats.
    RTI-13951-33
  • HY-162660
    BI-9508
    		Agonist
    BI-9508 is a selective and cross the blood-brain barrier GPR88 agonist. BI-9508 has the potential for the research of neurological disorders.
    BI-9508
  • HY-167856
    RTI-122
    		Agonist
    RTI-122 is a brain-penetrant and potent GPR88 agonist with good metabolic stability (half-life of 5.8 h in mice) and a cAMP EC50 of 11 nM. RTI-122 can be utilized in research on excessive drinking.
    RTI-122
  • HY-156772
    GPR88 agonist 2
    		Agonist 99.57%
    GPR88 agonist 2 (compound 53) is a potent and brain-penetrantGPR88 agonist with an EC50 value of 14 µM in GPR88 cAMP functional assay.
    GPR88 agonist 2
  • HY-163096
    GPR88 agonist 3
    		Agonist
    GPR88 agonist 3 (compound 20) is a GPR88 agonist 3, with an EC50 of 204 nM. GPR88 agonist 3 can be used for psychiatric and neurodegenerative disorders research.
    GPR88 agonist 3