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. 1987 Mar;7(1):97–103. doi: 10.1007/BF00734993

Multiple mechanisms of antagonism ofγ-aminobutyric acid (GABA) responses

N Akaike 1, T Yakushiji 1, N Tokutomi 1, D O Carpenter 1,✉
PMCID: PMC11567227  PMID: 3594520

Abstract

  1. Gamma-aminobutyric acid (GABA) is one of the most important neurotransmitters in the brain. In an effort to understand the operation of the GABA receptor-ionophore complex, the antagonism of GABA responses by four substances was studied in bullfrog dorsal root ganglion cells by concentration-clamp and internal-perfusion techniques.

  2. Two antagonists (bicuculline and Zn2+) were competitive; two (picrotoxin and penicillin) were noncompetitive. However, significant changes in the kinetics of activation and inactivation were produced by the antagonists, including those that were competitive.

  3. The causes of these changes may be important clues to the structure and operation of the GABA receptor-ionophore complex.

Key words: γ-aminobutyric acid (GABA), dorsal root ganglion neurons, internal perfusion, GABA antagonists

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