GABA discovery

Nonbenzodiazepine Benzodiazepine Receptor Ligands. The simultaneous discovery of the molecular target for the BZs, the GABA /BZ receptor complex, by two teams of workers (34,35) resulted ia the identification of a number of atypical or anxioselective anxiolytics that, whereas not having the BZ pharmacophore, interacted direcdy with the central BZ receptor. The anxioselective nature of such agents was considered to be... 

The story of the discovery of pregabalin (2) began in 1991, when Silverman and Taylor published a paper on the anticonvulsant effect of 3-alkyl GABA analogs (Silverman et ah, 1991). Out of this collection of compounds, 3-isobutyl GABA stood out as the most active analog in the series, which protected mice from seizures induced by corneal electroshock. 

GABA is the most comprehensively studied inhibitory neurotransmitter, and there are many reviews of its biochemistry and pharmacology. The reason for this great interest is the discovery that the most popular drugs of the 1970-1980s, the benzodiazepine tranquilizers or anxiolytics, as well as the previously popular barbiturates, act on the GABAergic neuronal system. 

P. J. Whiting (2003). GABA-A receptor subtypes in the brain a paradigm for CNS drug discovery Drug Discov. Today 8 445-450. 

Tiagabine is a derivative of nipecotic acid and was "rationally designed" as an inhibitor of GABA uptake (as opposed to discovery through random... 

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