RTI-122 / RTI International - LARVOL DELTA

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)

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

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

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