Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:2.6.1.19 (GABA transaminase)
 808 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Two clinically effective anticonvulsants, phenobarbitone and diazepam, protected 5-day old chicks against picrotoxin convulsions without reducing brain GABA-transaminase activity or raising brain GABA concentration. Ethanolamine-O-sulphate and amino-oxyacetic acid, in doses which inhibited GABA-transminase by at least 63% and approximately doubled brain GABA concentration, did not significantly affect the ED50 for picrotoxin convulsions. The ED50 for picrotoxin convulsions was significantly raised by di-n-propylacetate (800 mg/kg) which inhibited GABA transaminase activity by 6% and elevated brain GABA concentration by 26%.
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PMID:Picrotoxin convulsions and GABA metabolism after injection of anticonvulsants in chicks. 99 20

1. Partially purified preparations of rat brain 4-aminobutyrate aminotransferase were inhibited in a time-dependent manner by ethanolamine O-sulphate. The inhibition was not reversed by dialysis. 2. The inhibitor formed an initial reversible complex with the enzyme (K(i)=4.4x10(-4)m) and the rate of inactivation followed pseudo-first-order kinetics (k=7.15x10(-4)s(-1)). The inclusion of 4-aminobutyrate markedly slowed the rate of inactivation. 3. Ethanolamine O-sulphate did not inhibit glutamate decarboxylase, alanine aminotransferase or aspartate aminotransferase. 4. Intracisternal injection of ethanolamine O-sulphate into rats led to rapid inactivation of 4-aminobutyrate aminotransferase in vivo.
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PMID:Active-site-directed irreversible inhibition of rat brain 4-aminobutyrate aminotransferase by ethanolamine O-sulphate in vitro and in vivo. 466 81

2-Aminoethanol (ethanolamine) was studied for effects on neurochemical assays for GABA synthesis, receptor binding, uptake and metabolism in rat brain preparations. The effects of ethanolamine were compared with those of ethanolamine O-sulphate (EOS), an inhibitor of GABA degradation. Furthermore, the effect of both compounds was compared on GABA metabolism in rat brain in vivo. In vitro, ethanolamine and EOS had no significant effect on the GABA synthesizing enzyme glutamic decarboxylase (GAD) and GABA uptake, but both drugs proved virtually equipotent to inhibit the GABA degrading enzyme GABA aminotransferase (GABA-T). EOS was a relatively potent inhibitor of GABA receptor binding, whereas ethanolamine was not effective in this regard. Following systemic administration in rats, 50% inhibition of GABA-T in the brain was achieved by 500 mg/kg ethanolamine or 2000 mg/kg EOS, respectively. As a consequence of GABA-T inhibition, GABA levels increased significantly. GAD activity remained unchanged after both treatments. The present results suggest that the recently reported enhancement of functional effects of GABA by ethanolamine may relate, at least in part, to the inhibitory effect of the compound on GABA catabolism.
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PMID:Effect of 2-aminoethanol on the synthesis, binding, uptake and metabolism of GABA. 632 73