Background

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. The research team has discovered the first α6 selective ligands. The team continues to explore indications including epilepsy, tic disorders, schizophrenia, obsessive compulsive disorders, attention deficit disorders, depression,migraine, and pain.

Technology Overview

Through a joint collaboration the inventors have synthesized and tested novel GABA A receptor ligands specific to the alpha 6 subtype (GABAAR-α6). Recent studies have implicated the α6 receptors in trigeminal orofacial pain, neuropsychiatric disorders with sensori-motor gating deficits, depression, and migraine.

Stage of Development

The group has observed promising results in animal models for several of these indications, and the lead compounds show a lack of cytotoxicity, improved metabolic stability, and increased brain concentrations, rendering them potential candidates for treatment of CNS disorders.

Benefits

Specific – The novel compounds are specific for the α6 GABAA subtypes
Non-Sedating – Avoidance of the α1-subtype aids in preventing sedative effects
Metabolically stable – Deuteration of the methoxy group of aryl-pyrazoloquinolinones improves metabolic stability and bioavailability
Safer/Less addictive – Compounds which are silent or nearly silent at the α1-and α5-subtype should demonstrate no tolerance and less addictive effects.

Opportunity

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.

Novel GABAAR-α6 Subtype Selective Ligands for Pain and CNS Disorders

Patents

IP Status

Seeking