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

3‐Substituted GABA analogs with central nervous system activity: A review Gabapentin and Pregabalin are both 3‐alkylated γ‐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. © 1999 John Wiley & Sons, Inc. Med Res Rev 19, 149–177, 1999. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Medicinal Research Reviews Wiley

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

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Publisher
Wiley
Copyright
Copyright © 1999 John Wiley & Sons, Inc.
ISSN
0198-6325
eISSN
1098-1128
DOI
10.1002/(SICI)1098-1128(199903)19:2<149::AID-MED3>3.3.CO;2-2
Publisher site
See Article on Publisher Site

Abstract

Gabapentin and Pregabalin are both 3‐alkylated γ‐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. © 1999 John Wiley & Sons, Inc. Med Res Rev 19, 149–177, 1999.

Journal

Medicinal Research ReviewsWiley

Published: Mar 1, 1999

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