Hydroxy-and amino-substituted piperidinecarboxylic acids as. gamma.-aminobutyric acid agonists and uptake inhibitors

…, E Falch, P Krogsgaard-Larsen

Index: Jacobsen; Labouta; Schaumburg; Falch; Krogsgaard-Larsen Journal of Medicinal Chemistry, 1982 , vol. 25, # 10 p. 1157 - 1162

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Citation Number: 22

Abstract

(3RS, 4SR)-3-hydroxypiperidine-4-carboxylic acid (14), related to the specific GABA agonist piperidine-4-carboxylic acid (isonipecotic acid), has been synthesized. The structures of 4, 10, 14, 18, and 20 have been established by 270-MHz'H NMR spectroscopic analyses. The affinity of the compounds for the GABA receptors and for the neuronal (synaptosomal) GABA uptake system in vitro has been measured. Compound 14 interacts selectively with the ...