Engineering a GABA endowed with pharmacological CNS activity when given by an extracerebral route View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

2009-05

AUTHORS

Joseph Vamecq, Yves Feutelais, Pierre Maurois, Mehrez Sghaier, Emma Dichi, Michèle German-Fattal, Christine Herrenknecht, Pierre Gressens, Roméo Cecchelli, Lucie Dehouck, James P. Stables, Nicole Pages, Bernard Legendre, Pierre Bac

ABSTRACT

Gamma-aminobutyric acid (GABA) is a major inhibitory neurotransmitter physiologically active in the central nervous system (CNS), being synthesised and delivered by GABAergic neurons. It is, however, pharmacologically devoid of CNS activity when presented externally to brain because of limited blood–brain barrier diffusion and intensive breakdown by astrocyte GABA transaminase. We show herein that extracerebral administration may be, however, pharmacologically effective in controlling experimental convulsive attacks when GABA is submitted to sublimation under vacuum just before use. Though initially enigmatic because nuclear magnetic resonance (NMR) and infrared (IR) analyses identified the sublimation-derived compound to be the reference zwitterionic GABA, this observation was understood by showing that the reference and sublimated GABAs were monoclinic and tetragonal phases of GABA solid, respectively. More... »

PAGES

255-267

References to SciGraph publications

  • 2008. Regulation of Excitation by GABA Neurotransmission: Focus on Metabolism and Transport in INHIBITORY REGULATION OF EXCITATORY NEUROTRANSMISSION
  • Identifiers

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    http://scigraph.springernature.com/pub.10.1007/s00044-008-9124-1

    DOI

    http://dx.doi.org/10.1007/s00044-008-9124-1

    DIMENSIONS

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