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Recent Patents on CNS Drug Discovery (Discontinued)


ISSN (Print): 1574-8898
ISSN (Online): 2212-3954

An Update on GABA Analogs for CNS Drug Discovery

Author(s): Perumal Yogeeswari, Jegadeesan V. Ragavendran and Dharmarajan Sriram

Volume 1, Issue 1, 2006

Page: [113 - 118] Pages: 6

DOI: 10.2174/157488906775245291


GABA (γ-aminobutyric acid) is one of the major inhibitory transmitters in the central nervous system of mammals. GABA is not transported efficiently into the brain from the bloodstream (i.e. GABA does not effectively cross the blood-brain barrier). Consequently, brain cells provide virtually all of the GABA found in the brain i.e. GABA is biosynthesized by decarboxylation of glutamic acid with pyridoxal phosphate. The implication of low GABA levels in a number of common CNS disease states and/or common medical disorders has stimulated intensive interest in preparing GABA analogs, which have superior pharmaceutical properties in comparison to GABA. Accordingly, a number of GABA analogs, with considerable pharmaceutical activity have been synthesized in the art. This review includes some of the important recent patents on novel GABA analogs and some pharmaceutical compositions there of.

Keywords: γ-Aminobutyric acid, blood brain barrier, epilepsy, depression, neuropathic pain, GABA analogs

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