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[The "trap"--a modification of the block of neuronal nicotinic cholinoceptors].

Authors
  • Kurennyĭ, D E
  • Derkach, V A
  • Gmiro, V E
  • Skok, V I
Type
Published Article
Journal
Neir̆ofiziologiia = Neurophysiology
Publication Date
Jan 01, 1988
Volume
20
Issue
6
Pages
826–829
Identifiers
PMID: 3249610
Source
Medline
License
Unknown

Abstract

The effect of IEM-1742, a pentaethonium derivative, on the currents induced by iontophoretic applications of acetylcholine was studied in rat superior cervical ganglion neurons using patch-clamp method in the whole-cell modification. Blocking action increased with membrane hyperpolarization and was removed by strong membrane depolarization. Apparent dissociation constant for the receptor-blocker reaction was found to be (2.9 +/- 0.6) 10(-6) M (n = 6) at -50 mV and 20-23 degrees C. IEM-1742 blocks the nicotinic acetylcholine receptor in its activated form. The dissociation of IEM-1742 from the receptor was drastically accelerated during its activation by agonist (trap-block). Trapped receptor was not released from the blocker only by membrane depolarization to the level at which any blocking effect is absent. The data obtained show that IEM-1742 in rat sympathetic ganglion neurons acts in the potential-dependent manner and displays a trap-effect.

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