The Blockade of Open Channel of Acetylcholine Receptor is Responsible for Selective Blockade of Nicotinic Transmission

  • Vladimir I. Skok


Hexamethonium, a selective ganglionic blocker, at its lowest effective concentration exhibits the open-channel blockade of nicotinic acetylcholine (ACh) receptors in sympathetic ganglion neurones, with no signs of their competitive blockade. This is evidenced by the facts that 1) hexamethonium shortens in a voltage-dependent manner the apparent mean channel lifetime estimated from the excitatory postsynaptic current (EPSC) decay and from the ACh noise analysis as well as from the analysis of single channel activity, and 2) the hexamethonium-induced reduction of the ACh current amplitude is enhanced by the preliminary opening of the ACh-gated channels.

The rate constants that characterize binding of hexamethonium, pirilenum and some other selective ganglionic blockers to an open ACh-gated channel correlates with their ganglion-blocking activities, in contrast to what is observed in the effects of competitive ganglionic blockers tubocurarine and trimethaphan. This observation suggests that selective ganglionic blockade produced by some compounds is due to an open-channel blockade while in other cases it is due to a competitive mechanism. The selective blockade of open channel can be observed in different types of synapses. It is suggested that the site in the ACh-gated open channel that binds selective blockers normally binds Ca2+ ions.


Open Channel Sympathetic Ganglion Selective Blockade Single Channel Activity Nicotinic AChR 
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Copyright information

© Plenum Press, New York 1987

Authors and Affiliations

  • Vladimir I. Skok
    • 1
  1. 1.Department of the Autonomic Nervous System PhysiologyBogomoletz Institute of PhysiologyKiev-24USSR

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