Bioorganic & medicinal chemistry

Synthesis and evaluation of novel heteroaromatic substrates of GABA aminotransferase

DD Hawker, RB Silverman

Index: Hawker, Dustin D.; Silverman, Richard B. Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 19 p. 5763 - 5773

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Citation Number: 12

Abstract

Two principal neurotransmitters are involved in the regulation of mammalian neuronal activity, namely, γ-aminobutyric acid (GABA), an inhibitory neurotransmitter, and l-glutamic acid, an excitatory neurotransmitter. Low GABA levels in the brain have been implicated in epilepsy and several other neurological diseases. Because of GABA's poor ability to cross the blood–brain barrier (BBB), a successful strategy to raise brain GABA concentrations is ...