Recently we have designed a series of subtype selective GABA(A)-ergic ligands that are active as nonsedating anxiolytics in rodents and primates. These GABAergic/BzR agonists are nearly silent at a1 and a5�2?2 subtypes; consequently, tolerance does not develop to the anxiolytic, anticonvulsant, or antihyper-algesic effects. Based on available literature these agents will exhibit little or no abuse potential in contrast to the well known tranquilizers (Valium, Xanax and Librium). Because they do not develop tolerance and do not cause amnesia, ataxia nor sedation, they are targeted for treatment of neuropathic and inflammatory pain. Also, another series of ligands has been synthesized that target a5�2?2 subtypes while staying silent at a1 which can used to target treatment of schizophrenia. Analogs of the lead compound can be synthesized and quickly screening using transiently transfected cells assayed with an automated-patchclamp instrument. Again, these non toxic agents do not develop tolerance.

Synthesis of benzodiazepines active against neuropathic pain as well as schizophrenia

245th National Meeting (2013)

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