The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4, 4-bis (3-methyl-2-thienyl)-3-butenyl]-3- …

KE Andersen, C Braestrup, FC Groenwald…

Index: Andersen, Knud Erik; Braestrup, Claus; Groenwald, Frederik C.; Joergensen, Anker S.; Nielsen, Erik B.; et al. Journal of Medicinal Chemistry, 1993 , vol. 36, # 12 p. 1716 - 1725

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Citation Number: 121

Abstract

Introduction y-Aminobutyric acid (GABA) is recognized as the principal inhibitory neurotransmitter in the mammalian central nervous system (CNS). lv2 It has been estimated that approximately 40% of synapses in the CNS are GABA'ergic. 3 Attenuation of GABA'ergic neurotransmission has been postulated as being involved in the pathophysiology of several CNS disorders in humans, for example anxiety, pain, and epilepsy.-As a result, much ...