Format

Send to

Choose Destination
Perspect Medicin Chem. 2010 Aug 3;4:23-31.

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

Author information

1
Durham Veterans Affairs Medical Center and Duke University School of Medicine Durham, NC, USA.

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.

KEYWORDS:

GABA; GABA esters; central pain

PMID:
20703328
PMCID:
PMC2918363

Supplemental Content

Full text links

Icon for PubMed Central
Loading ...
Support Center