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3-Substituted GABA analogs with central nervous system activity: A review

✍ Scribed by Justin S. Bryans; David J. Wustrow

Publisher
John Wiley and Sons
Year
1999
Tongue
English
Weight
177 KB
Volume
19
Category
Article
ISSN
0198-6325

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✦ Synopsis

Gabapentin and Pregabalin are both 3-alkylated ␥-amino butyric acid (GABA) analogs. Gabapentin was designed as a lipophilic GABA analog and was first synthesized as a potential anticonvulsant and was launched in 1994 as add-on therapy for the treatment of epilepsy. In this review the discovery and development of gabapentin as an anticonvulsant are discussed. During human trials and while in clinical use, it became apparent that gabapentin induced some other potentially useful therapeutic effects in chronic pain states and behavioral disorders. A review of animal and clinical data relating to these other potential therapeutic utilities is presented. Pregabalin was identified after an investigation into other 3-substituted GABA analogs. It has since been shown to have a similar pharmacological profile to gabapentin with greater potency in preclinical models of pain and epilepsy. Studies of the mechanism(s) of action of these compounds are discussed. Work towards identifying new analogs of both gabapentin and pregabalin is also reviewed.

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