3034664-39-3
Chemical Structure
RTI-122
- CAS No.: 3034664-39-3
- Formula:C29H34FN3O3
- Molecular Weight:491.60
InChIKey: OXODNABCLPQQDT-CEWWTIOHSA-N
SMILES: CO[C@H](C)[C@H](N)CN(C1=CC=C(C2=CC=C(C=C2)OC(C)C)C=C1)C([C@H]3[C@H](C4=CC=C(C=N4)F)C3)=O
Biological Activity: 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 (T1/2=5.8 h) and can be used to investigate alcohol use disorder[1][2].
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RTI-122 | 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 (T1/2=5.8 h) and can be used to investigate alcohol use disorder. | |||||||||||||||||||||
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References
- [1]. Rahman MT, et al. Improvement of the Metabolic Stability of GPR88 Agonist RTI-13951-33: Design, Synthesis, and Biological Evaluation. J Med Chem. 2023;66(4):2964-2978. [Content Brief]
- [2]. Lovelock DF, et al. The GPR88 Agonist RTI-122 Reduces Alcohol-Related Motivation and Consumption. Addict Biol. 2025;30(6):e70058. [Content Brief]
