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general/gaba-transaminase-inhibitors

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GABA transaminase inhibitor

FieldValue
ImageVigabatrin.svg
ImageClassskin-invert-image
CaptionVigabatrin (Sabril; γ-vinyl-GABA), a selective and irreversible GABA-T inhibitor used as an anticonvulsant.
Width200px
SynonymsGABA-T inhibitor; GABA metabolism inhibitor; GABA degradation inhibitor
UseEpilepsy
Mechanism_of_actionGABA transaminase inhibition
Biological_targetGABA transaminase (GABA-T)
Chemical_classGABA analogues and others
Drugs.com

| Drugs.com =

A GABA transaminase inhibitor is a drug that acts as an inhibitor of the enzyme GABA transaminase (GABA-T), which metabolizes the major inhibitory neurotransmitter γ-aminobutyric acid (GABA). Inhibition of GABA-T reduces the degradation of GABA, leading to increased neuronal GABA concentrations. Examples of GABA-T inhibitors include valproic acid, vigabatrin, phenylethylidenehydrazine (PEH) (a metabolite of phenelzine), ethanolamine-O-sulfate (EOS), and L-cycloserine, among others. Certain GABA-T inhibitors, like vigabatrin, are used clinically as anticonvulsants.

References

References

  1. (February 1993). "Vigabatrin". Ann Pharmacother.
  2. (August 2003). "GABA transporters and GABA-transaminase as drug targets". Curr Drug Targets CNS Neurol Disord.
  3. (1979). "GABA—Biochemistry and CNS Functions".
  4. (1979). "Valproic acid. Review of a new antiepileptic drug". Archives of Neurology.
  5. (April 2008). "Treatment of epilepsy: the GABA-transaminase inhibitor, vigabatrin, induces neuronal plasticity in the mouse retina". Eur. J. Neurosci..
  6. (1990). "Chronic toxicity studies with vigabatrin, a GABA-transaminase inhibitor". Toxicologic Pathology.
  7. (1994). "Amine Oxidases: Function and Dysfunction".
  8. (1986). "L-cycloserine: Behavioural and biochemical effects after single and repeated administration to mice, rats and cats". Neuropharmacology.
  9. (February 2003). "Novel mechanisms of action of three antiepileptic drugs, vigabatrin, tiagabine, and topiramate". Neurochem Res.
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