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JOURNAL

Perspectives in Medicinal Chemistry

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Selected Gamma Aminobutyric Acid (GABA) Esters may Provide Analgesia for Some Central Pain Conditions

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Publication Date: 03 Aug 2010

Type: Review

Journal: Perspectives in Medicinal Chemistry

Citation: Perspectives in Medicinal Chemistry 2010:4 23-31

doi: 10.4137/PMC.S5490

Abstract

Central pain is an enigmatic, intractable condition, related to destruction of thalamic areas, resulting in likely loss of inhibitory synaptic transmission mediated by GABA. It is proposed that treatment of central pain, a localized process, may be treated by GABA supplementation, like Parkinson’s disease and depression. At physiologic pH, GABA exists as a zwitterion that is poorly permeable to the blood brain barrier (BBB). Because the pH of the cerebral spinal fluid (CSF) is acidic relative to the plasma, ion trapping may allow a GABA ester prodrug to accumulate and be hydrolyzed within the CSF. Previous investigations with ester local anesthetics may be applicable to some GABA esters since they are weak bases, hydrolyzed by esterases and cross the BBB. Potential non-toxic GABA esters are discussed. Many GABA esters were investigated in the 1980s and it is hoped that this paper may spark renewed interest in their development.


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My experience publishing in Perspectives in Medicinal Chemistry was very positive.  The submission process was very quick and easy.  I was extremely impressed by the efficiency of the editorial staff and reviewers.
Dr Peter Wostyn (PC Sint Amandus, Beernem, Belgium)
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