PMID: 7932213Jun 1, 1994Paper

On the mechanism of 4-aminopyridine action on the cloned mouse brain potassium channel mKv1.1

The Journal of Physiology
G J StephensD G Owen

Abstract

1. This study used the whole-cell patch clamp technique to investigate the mechanism of action of the K+ channel blocker 4-aminopyridine (4-AP) on the cloned K+ channel mouse Kv1.1 (mKv1.1) expressed in Chinese hamster ovary cells. 2. Cells transfected with mKv1.1 expressed a non-inactivating, delayed rectifier-type K+ current. 4-AP induced a dose-, voltage- and use-dependent block of mKv1.1. 3. 4-AP blockade of mKv1.1 was similar whether 4-AP was administered extracellularly (IC50 = 147 microM) or intracellularly (IC50 = 117 microM). 4. Inclusion of the first twenty amino acids of the N-terminus sequence of the Shaker B K+ channel ('inactivation peptide') in the patch electrode transformed mKv1.1 into a rapidly inactivating current. The time constant of decay for the modified current was dependent on the concentration of inactivation peptide, and under these conditions extracellular 4-AP had a reduced potency (IC50 values of 471 and 537 microM for 0.5 and 2 mg ml-1 inactivation peptide, respectively). 5. A permanently charged analogue of 4-AP, 4-aminopyridine methiodide (4-APMI), was found to block mKv1.1 when applied inside the cell, but was without effect when administered externally. 6. Decreasing the intracellular pH (pHi)...Continue Reading

Citations

Feb 1, 1997·British Journal of Pharmacology·M Nobile, P Vercellino
Sep 14, 2011·The Journal of Physiology·Matthew H Higgs, William J Spain
Jun 1, 1997·The Journal of General Physiology·C C ShiehG E Kirsch
Feb 14, 2006·Pharmacology & Therapeutics·Susan I V Judge, Christopher T Bever
Aug 4, 2001·Nitric Oxide : Biology and Chemistry·A Hermann, C Erxleben
Apr 19, 2018·ELife·Richard Burkett Dewell, Fabrizio Gabbiani
Jul 24, 1998·Journal of Cardiovascular Pharmacology·J W WegenerH Nawrath
Sep 16, 1998·Proceedings of the National Academy of Sciences of the United States of America·N N Urban, G Barrionuevo
Sep 24, 1998·The American Journal of Physiology·M G BergerN J Rusch
Jan 25, 2013·The Journal of Biological Chemistry·Wardah AlasmariChristopher L R Barratt
Mar 10, 2017·Journal of the Royal Society, Interface·Linford J B BriantPatrik Rorsman
Dec 9, 2020·Journal of Functional Biomaterials·Tomoki Furuseki, Yasumitsu Matsuo
Nov 1, 1996·Comparative Biochemistry and Physiology. Part C, Pharmacology, Toxicology & Endocrinology·T SugimotoH Yabu

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