The inner quaternary ammonium ion receptor in potassium channels of the node of Ranvier.
Quaternary ammonium ions were applied to the inside of single myelinated nerve fibers by diffusion from a cut end. The resulting block of potassium channels in the node of Ranvier was studied under voltage-clamp conditions. The results agree in almost all respects with similar studies by Armstrong of squid giant axons. With tetraethylammonium ion (TEA), pentyltriethylammonium ion (C(5)), or nonyltriethylammonium ion (C(9)) inside the node, potassium current during a depolarization begins to rise at the normal rate, reaches a peak, and then falls again. This unusual inactivation is more complete with C(9) than with TEA. Larger depolarizations give more block. Thus the block of potassium channels grows with time and voltage during a depolarization. The block reverses with repolarization, but for C(9) full reversal takes seconds at -75 mv. The reversal is faster in 120 mM KCl Ringer's and slower during a hyperpolarization to -125 mv. All of these effects contrast with the time and voltage-independent block of potassium, channels seen with external quaternary ammonium ions on the node of Ranvier. External TEA, C(5), and C(9) block without inactivation. The external quaternary ammonium ion receptor appears to be distinct from the inner one. Apparently the inner quaternary ammonium ion receptor can be reached only when the activation gate for potassium channels is open. We suggest that the inner receptor lies within the channel and that the channel is a pore with its activation gate near the axoplasmic end.
D000818:Animals; D001001:Anura; D001370:Axonal Transport / Q000187:drug effects; D001369:Axons / Q000187:drug effects; D066298:In Vitro Techniques; D007700:Kinetics; D008564:Membrane Potentials; D009186:Myelin Sheath / Q000187:drug effects*; D009413:Nerve Fibers, Myelinated / Q000187:drug effects; D009467:Neuromuscular Depolarizing Agents / Q000494:pharmacology; D011188:Potassium / Q000378:metabolism*; D000644:Quaternary Ammonium Compounds / Q000494:pharmacology*; D011894:Rana pipiens; D011901:Ranvier's Nodes / Q000187:drug effects; D011955:Receptors, Drug; D013757:Tetraethylammonium Compounds / Q000494:pharmacology
D009467:Neuromuscular Depolarizing Agents; D000644:Quaternary Ammonium Compounds; D011955:Receptors, Drug; D013757:Tetraethylammonium Compounds; D011188:Potassium