title: The flickery block of ATP-dependent potassium channels of skeletal muscle by internal 4-aminopyridine.
abstract: We have examined the effects of 4-aminopyridine (4-AP) on single ATP-dependent potassium channels in patches excised from frog skeletal muscle. 4-AP applied to the internal face of the membrane caused a flickery block. We could not detect any flickery block when 10 mM 4-AP was applied to the external surface of the membrane. The reduction in mean unitary current by internal 4-AP was consistent with 1:1 binding with a Kd of 3.3 mM at 0 mV. The block was voltage-dependent, increasing with depolarization with an effective valency of 0.57. Rate constants for blocking and unblocking by 4-AP were obtained by fitting beta functions to the distribution of current amplitudes. Both rate constants were voltage-dependent. At 0 mV they were 17 mM-1 ms-1 and 61 ms-1. Simulation of the block using these rate constants produced a flickery block very similar to that observed experimentally.
authors.affiliation: Department of Physiology, University of Leicester, UK.
authors.forename: N W
authors.initials: NW
authors.lastname: Davies
authors.forename: A I
authors.initials: AI
authors.lastname: Pettit
authors.forename: R
authors.initials: R
authors.lastname: Agarwal
authors.forename: N B
authors.initials: NB
authors.lastname: Standen
mesh_terms: D015761:4-Aminopyridine / Q000494:pharmacology*; D000255:Adenosine Triphosphate / Q000494:pharmacology*; D000818:Animals; D004594:Electrophysiology; D009132:Muscles / Q000378:metabolism*; D011188:Potassium / Q000037:antagonists & inhibitors*; D015221:Potassium Channels / Q000378:metabolism* / Q000502:physiology; D011896:Rana temporaria
chemical_list: D015221:Potassium Channels; D000255:Adenosine Triphosphate; D015761:4-Aminopyridine; D011188:Potassium