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.
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GPR88 Related Products (14)
Related Products (14)
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RTI-13951-33 hydrochloride
0 ImagesCat. No.: HY-112612APurity: 98.50%
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2-PCCA hydrochloride
0 ImagesCat. No.: HY-100013CPurity: 99.11%2-PCCA hydrochloride is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC50 of 116 nM in HEK293 cells.
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RTI-122 dihydrochloride
0 ImagesCat. No.: HY-167856ARTI-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 (T1/2=5.8 h) and can be used to investigate alcohol use disorder.
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2-PCCA
0 ImagesCat. No.: HY-100013CAS No.: 1984859-71-32-PCCA is a racemic form of the GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC50 of 116 nM in HEK293 cells.
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RTI-13951-33
0 ImagesCat. No.: HY-112612CAS No.: 2244884-08-8
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RTI-122
0 ImagesCat. No.: HY-167856CAS No.: 3034664-39-3RTI-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 (T1/2=5.8 h) and can be used to investigate alcohol use disorder.
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BI-9508
0 ImagesCat. No.: HY-162660CAS No.: 3082554-75-1BI-9508 is a selective and cross the blood-brain barrier GPR88 agonist. BI-9508 has the potential for the research of neurological disorders.
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(1S,2S)-2-PCCA hydrochloride (Standard)
0 ImagesCat. No.: HY-100013B1RCAS No.: 1609563-70-3(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.
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(1R,2R)-2-PCCA hydrochloride (Standard)
0 ImagesCat. No.: HY-100013A1RCAS No.: 1609563-71-4(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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