Orally active and potent inhibitors of gamma-aminobutyric acid uptake.

  title={Orally active and potent inhibitors of gamma-aminobutyric acid uptake.},
  author={Feda' E Ali and William E. Bondinell and P A Dandridge and James Frazee and Emlyn B. Garvey and G R Girard and Christina Kaiser and Thomas W. Ku and John Lafferty and George I. Moonsammy},
  journal={Journal of medicinal chemistry},
  volume={28 5},
3-Pyrrolidineacetic acid (1a), certain piperidinecarboxylic acids--i.e., 3-piperidinecarboxylic acid (2a), 1,2,5,6-tetrahydro-3-pyridinecarboxylic acid (3a), and cis-4-hydroxy-3-piperidinecarboxylic acid (4a)--cis-3-aminocyclohexanecarboxylic acid (5a, cis-3-ACHC), and gamma-aminobutyric acid (6a, GABA) itself are among the most potent inhibitors of [3H]GABA uptake by neurons and glia in vitro. These hydrophilic amino acids, however, do not readily enter the central nervous system in… CONTINUE READING
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