GPR88 Agonist

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.

2-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.

GPR88 agonist 2 (compound 53) is a potent and brain-penetrantGPR88 agonist with an EC₅₀ value of 14 µM in GPR88 cAMP functional assay.

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.

BI-9508 is a selective and cross the blood-brain barrier GPR88 agonist. BI-9508 has the potential for the research of neurological disorders.

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.