Recent studies have implicated the α6GABAARs as the valid target in trigeminal orofacial pain, neuropsychiatric disorders with sensori-motor gating deficits, depression, and migraine. Promising results were found in animal models for several of these indications, and the lead compounds show a lack of cytotoxicity, improved metabolic stability, an excellent bioavailability after oral administration, and appropriate brain concentrations, rendering them potential candidates for treatment of CNS disorders.
Many GABAergic drugs on the market today offer little subtype selectivity and thus exhibit undesired side effects (sedation, ataxia, amnesia, tolerance, and addiction). There has been a lack of new drugs developed for CNS disorders, while the social, clinical, and economic need remains.
Through a joint collaboration, the inventors have synthesized and tested novel non-benzodiazepine GABAA receptor ligands functionally selective to the alpha 6 subtype (α6GABAAR).
We believe our team has discovered the first α6GABAAR selective ligands. The team continues to explore indications including epilepsy, tic disorders, schizophrenia, obsessive compulsive disorders, attention deficit disorders, depression, migraine, and pain.
US and EP Nationalized Applications PCT/US2016/035761.
This technology is part of an active and ongoing research program and is seeking partners for development of the final product. It is available for developmental research support/licensing under either exclusive or non-exclusive terms.