Bioorganic & medicinal chemistry

Synthesis and evaluation of N-substituted nipecotic acid derivatives with an unsymmetrical bis-aromatic residue attached to a vinyl ether spacer as potential GABA …

G Quandt, G Höfner, KT Wanner

Index: Quandt, Gabriele; Hoefner, Georg; Wanner, Klaus T. Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 11 p. 3363 - 3378

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Citation Number: 12

Abstract

γ-Amino butyric acid (GABA) is the major inhibitory neurotransmitter in the mammalian central nervous system (CNS). A malfunction of the GABAergic neurotransmission is connected to several neuronal disorders like epilepsy, Alzheimer's disease, neuropathic pain, and depression. One possibility to enhance GABA levels in the synaptic cleft is to inhibit mGAT1, one of the four known plasma membrane bound GABA transporters, which ...