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Contrary to its effects on the
Volume 270,
Number 23,
Issue of June 9, pp. 13799-13806, 1995
©1995 by The American Society for Biochemistry and Molecular Biology, Inc.
-aminobutyric acid type A
receptor, picrotoxin antagonism of the
1 subunit of the human
glycine receptor is shown to be competitive, not use-dependent, and
nonselective between the picrotoxin components, picrotin, and
picrotoxinin. Competitive antagonism and non-use dependence are
consistent with picrotoxin binding to a site in the extracellular
domain. The mutations Arg Leu or Arg
Gln at residue 271
of the glycine receptor
1 subunit, which are both associated with
human startle disease, have previously been demonstrated to disrupt the
transduction process between agonist binding and channel activation. We
show here that these mutations also transform picrotoxin from an
allosterically acting competitive antagonist to an allosteric
potentiator at low (0.01-3 µM) concentrations and to
a noncompetitive antagonist at higher (
3 µM)
concentrations. This demonstrates that arginine 271 is involved in the
transduction process between picrotoxin binding and its mechanism of
action. Thus, the allosteric transduction pathways of both agonists and
antagonists converge at a common residue prior to the activation gate
of the channel, suggesting that this residue may act as an integration
point for information from various extracellular ligand binding sites.
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