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 (13):

By Effects:	Inhibitor (1) Agonists (5) Controls (2)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

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.

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.

HY-100013C

2-PCCA hydrochloride		99.61%
2-PCCA hydrochloride is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC₅₀ of 116 nM in HEK293 cells.

HY-167856A

RTI-122 dihydrochloride	Agonist	99.36%
RTI-122 dihydrochloride is a selective, blood-brain barrier-permeable GPR88 agonist (cAMP EC₅₀=11 nM), with EC₅₀ values of 11.5 nM and 155 nM for human and mouse GPR88, respectively ([³⁵S]GTPγS assay). By activating the GPR88 receptor to regulate the cAMP signaling pathway and G protein activity, RTI-122 dihydrochloride significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 dihydrochloride blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 dihydrochloride exhibits metabolic stability in mice (T_1/2=5.8 h) and can be used to investigate alcohol use disorder.

HY-156771

GPR88-IN-1	Inhibitor	99.17%
GPR88-IN-1 is a GPR88 inhibitor, and can be used for research of central diseases.

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.

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.

HY-167856

RTI-122	Agonist
RTI-122 is a selective, blood-brain barrier-permeable GPR88 agonist (cAMP EC₅₀=11 nM), with EC₅₀ values of 11.5 nM and 155 nM for human and mouse GPR88, respectively ([³⁵S]GTPγS assay). By activating the GPR88 receptor to regulate the cAMP signaling pathway and G protein activity, RTI-122 significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 exhibits metabolic stability in mice (T_1/2=5.8 h) and can be used to investigate alcohol use disorder.

HY-100013B1

(1S,2S)-2-PCCA hydrochloride	Control	99.65%
(1S,2S)-2-PCCA hydrochloride is a less active diastereomer of 2-PCCA. 2-PCCA is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC₅₀ of 116 nM in HEK293 cells.

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.

HY-100013B1R

(1S,2S)-2-PCCA hydrochloride (Standard)	Control
(1S,2S)-2-PCCA (hydrochloride) (Standard) is the analytical standard of (1S,2S)-2-PCCA (hydrochloride) (HY-100013B1). This product is intended for research and analytical applications. (1S,2S)-2-PCCA hydrochloride is a less active diastereomer of 2-PCCA. 2-PCCA is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC50 of 116 nM in HEK293 cells.

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.

HY-100013A1R

(1R,2R)-2-PCCA hydrochloride (Standard)
(1R,2R)-2-PCCA (hydrochloride) (Standard) is the analytical standard of (1R,2R)-2-PCCA (hydrochloride) (HY-100013A1). This product is intended for research and analytical applications. (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.

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