![]()
INV-18111
Background
G protein-gated inwardly rectifying potassium (GIRK) channels, are channels distributed throughout the central nervous system as well as the heart. Pharmacological investigations of GIRK channels, along with studies in animal models, suggest that GIRK activity has an important role in physiological responses, including pain perception and memory modulation. However, the lack of selective GIRK drugs that discriminate among the different GIRK channel subtypes (brain vs. cardiac), have hampered investigations into their precise physiological relevance and therapeutic potential.
Technology Overview
A novel compound has been developed that imparts high selectivity and efficacy for activation of brain GIRK1/GIRK2 channels. This new compound, identified as GAT1508, is a small molecule drug. While providing action for GIRK1/2, it does not activate cardiac GIRK1/4 channels, making it a lead candidate for neuronal indications.
The initial use of this drug has been focused on the treatment of Post-traumatic stress disorder (PTSD). An estimated 7-8% of the US population will have PTSD at some point in their lives. There is an urgent need to address a critical lack of advancement in the psychopharmacologic treatment of this disorder. Studies conducted to date by the research team show promising results, and suggest this compound’s possible utility for this prevalent indication for which there is currently no completely effective treatment.
Benefits
- High selectivity and efficacy for activation of GIRK1/GIRK2 channels
- Avoids activation of cardiac GIRK1/GIRK4 channels
- Compound can be synthesized in minutes
- Has shown positive activity for PTSD
Applications
- PTSD
- General anxiety disorders
- Epilepsy
- Pain (chronic, neuropathic and inflammatory)
Opportunity
- License
- Partnering
- Research Collaboration
