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  • Title: Use-dependent block of GABA-activated chloride channels in crayfish muscle fibers by picrate.
    Author: Kaila K, Erik K, Akerman O, Voipio J.
    Journal: Comp Biochem Physiol C Comp Pharmacol Toxicol; 1984; 78(2):309-13. PubMed ID: 6149070.
    Abstract:
    In crayfish muscle fibers studied with intracellular microelectrodes the protein-binding agent, picrate (2,4,6-trinitrophenolate; 10(-5)-2 X 10(-4) M) was found to have a specific and dose-dependent inhibitory effect on the chloride conductance activated by bath-applied gamma-aminobutyric acid (GABA). A kinetic analysis showed that picrate did not interfere with GABA binding to its receptor. The blocking action of picrate was not increased by lowering the extracellular Cl- concentration which indicates that picrate is not likely to bind to the ionic selectivity site of the postsynaptic Cl- channel. In fibers first exposed to picrate (1-2 X 10(-4) M) and then, in the continuous presence of this drug, to GABA (5 X 10(-4) M), the latter induced a transient increase in the chloride conductance with an apparent rate constant of decay of about 40 sec. It is tentatively suggested that the site of action of picrate is a positively charged amino acid residue that is exposed through the action of GABA and critically involved in the chemical gating of the postsynaptic chloride channel.
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