An Update on GABA Analogs for CNS Drug Discovery

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

Document Type: Research Article


Affiliations: Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science, Pilani-333031, India;

Publication date: January 1, 2006

More about this publication?
  • Recent Patents on CNS Drug Discovery publishes review articles on recent patents in the field of CNS drug discovery e.g. novel bioactive compounds, analogs & targets. A selection of important and recent patents on CNS drug discovery is also included in the journal. The journal is essential reading for all researchers involved in CNS drug design and discovery.
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