Recent Patents on CNS Drug Discovery

Vincenzo Di Marzo
Istituto di Chimica Biomolecolare (I.C.B.)
Consiglio Nazionale delle Ricerche (C.N.R.)
Via Campi Flegrei 34
Pozzuoli, Napoli 80078


An Update on GABA Analogs for CNS Drug Discovery

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

Affiliation: Medicinal ChemistryResearch Laboratory, Pharmacy Group, Birla Institute of Technology&Science, Pilani-333031, India;

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


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.

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Article Details

Page: [113 - 118]
Pages: 6
DOI: 10.2174/157488906775245291