Alpha 6-GABAAR-Selective Modulators for Oral Neuropathic Pain and CNS Disorders 



Orofacial pain, neuropsychiatric disorders, migraine, CNS disorders. 

Target Problems

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. 

Key Benefits

  • Functionally selective – The novel compounds are functionally selective for the α6GABAARsubtypes 
  • Non-Sedating – Avoidance of the α1-subtype aids in preventing sedative and other psychomotor-impairing effects.  
  • Metabolically stable – Deuteration of the methoxy group of aryl-pyrazoloquinolinones improves metabolic stability and optimizes bioavailability. 
  • Safer/Less addictive – Compounds that are silent or nearly silent at the α1-and α5- receptor subtypes should demonstrate limited tolerance and less addictive effects.  


Through collaboration, inventors have synthesized and tested novel non-benzodiazepine GABAA receptor ligands functionally selective to the alpha 6 subtype (α6GABAAR). The team continues to explore indications including schizophrenia and migraine.  

Intellectual Property


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