Gallamine triethiodide selectively blocks voltage-gated potassium channels in Ranvier nodes.
The effects of gallamine on ionic currents in single intact Ranvier nodes of the toad Xenopus were investigated. The following fully reversible effects were observed: 1. With a test concentration of 1 mmol/l the current-voltage relation of steady-state potassium currents, IK ss exhibited a complete block of IK ss up to about V = 110 mV; with stronger depolarisations the block was incomplete. The peak sodium currents, in contrast, were not affected. 2. At the same test concentration the potassium permeability constant PK was reduced by 92% from its normal value, while the sodium permeability constant PNa decreased by only 8%. 3. Concentration-response relations of the block of PK yielded an apparent dissociation constant of 30 micromol/l and a steepness parameter of unity. Patch-clamp experiments on cloned Kv1.1, Kv1.2, Kv1.3 and Kv3.1 channels yielded apparent dissociation constants of 86, 19, >>100 and 121 micromol/l, respectively. Our findings show that gallamine is particularly well suited for separating potassium and sodium currents in axonal current ensembles. They also strongly suggest that potassium currents in Ranvier nodes of Xenopus are mainly carried by an ensemble of Kv1.1 and 1.2 channels.
Hinck
D
D
Department of Physiology and Biophysics, University of California, Irvine 92697-4560, USA.
Wulff
H
H
Koppenhöfer
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E
D000818:Animals; D004305:Dose-Response Relationship, Drug; D004594:Electrophysiology; D005703:Gallamine Triethiodide / Q000494:pharmacology*; D008956:Models, Chemical; D003473:Neuromuscular Nondepolarizing Agents / Q000494:pharmacology*; D009474:Neurons / Q000502:physiology; D018408:Patch-Clamp Techniques; D011188:Potassium / Q000378:metabolism; D024642:Potassium Channels, Voltage-Gated / Q000378:metabolism*; D011901:Ranvier's Nodes / Q000187:drug effects*; D012964:Sodium / Q000378:metabolism; D013997:Time Factors; D014981:Xenopus
D003473:Neuromuscular Nondepolarizing Agents; D024642:Potassium Channels, Voltage-Gated; D012964:Sodium; D005703:Gallamine Triethiodide; D011188:Potassium