RTI-122
/ RTI International
- LARVOL DELTA
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June 20, 2025
The GPR88 Agonist RTI-122 Reduces Alcohol-Related Motivation and Consumption.
(PubMed, Addict Biol)
- "Importantly, RTI-122 did not affect water intake in mice or sucrose self-administration in rats, indicating receptor- and reward-specific modulation of alcohol intake. These findings suggest that RTI-122, through GPR88 agonism, effectively reduces alcohol consumption and motivation across various contexts, positioning it as a promising lead for the development of new AUD treatments."
Journal • Addiction (Opioid and Alcohol)
November 03, 2023
Exploration of Novel Chemotypes as GPR88 Agonists: Design, Synthesis, and SAR Studies of (4-Substituted-phenyl)acetamides Based on the Reversed Amide Strategy
(Neuroscience 2023)
- "Although the endogenous ligand for GPR88 is yet to be discovered, extensive medicinal chemistry campaigns have uncovered highly potent and brain-penetrant agonists such as RTI-13951-33 and RTI-122...With the aim of further improving the pharmacotherapeutic properties, as well as gaining access to new chemical space, we have developed novel (4-substituted-phenyl)acetamides based agonists for GPR88 that arise from bioisosteric replacement of amide functionality of the 2-AMPP scaffold. The rational design, synthesis, SAR, and computational docking studies based on the recently elucidated cryo-EM structure of GPR88 will be presented."
Addiction (Opioid and Alcohol) • CNS Disorders • Parkinson's Disease • Psychiatry • Schizophrenia
February 08, 2023
Improvement of the Metabolic Stability of GPR88 Agonist RTI-13951-33: Design, Synthesis, and Biological Evaluation.
(PubMed, J Med Chem)
- "Notably, RTI-122 was more effective than RTI-13951-33 in attenuating the binge-like alcohol drinking behavior in the drinking-in-the-dark paradigm. Collectively, our findings suggest that RTI-122 is a promising lead compound for drug discovery research of GPR88 agonists."
Journal
October 10, 2022
Design and characterization of a highly potent, metabolically stable, and brain-penetrant GPR88 agonist RTI-122
(Neuroscience 2022)
- "Finally, RTI-122 is active in vivo and significantly attenuated alcohol drinking and reinforcement in mice and rats. This work is supported by NIH R01AA026820."
Addiction (Opioid and Alcohol) • CNS Disorders • Parkinson's Disease • Psychiatry • Schizophrenia • Substance Abuse
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