Engineering a GABA endowed with pharmacological CNS activity when given by an extracerebral route - Archive ouverte HAL Access content directly
Journal Articles Medicinal Chemistry Research Year : 2009

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

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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.

Dates and versions

hal-00545967 , version 1 (13-12-2010)

Identifiers

Cite

Joseph Vamecq, Yves Feutelais, Pierre Maurois, Mehrez Sghaier, Emma Dichi, et al.. Engineering a GABA endowed with pharmacological CNS activity when given by an extracerebral route. Medicinal Chemistry Research, 2009, 18 (4), pp.255-267. ⟨10.1007/s00044-008-9124-1⟩. ⟨hal-00545967⟩
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