Penitrem A as a tool for understanding the role of large conductance Ca(2+)/voltage-sensitive K(+) channels in vascular function.

The Journal of Pharmacology and Experimental Therapeutics
Shinichi AsanoGregory M Dick

Abstract

Large conductance, Ca(2+)/voltage-sensitive K(+) channels (BK channels) are well characterized, but their physiological roles, often determined through pharmacological manipulation, are less clear. Iberiotoxin is considered the "gold standard" antagonist, but cost and membrane-impermeability limit its usefulness. Economical and membrane-permeable alternatives could facilitate the study of BK channels. Thus, we characterized the effect of penitrem A, a tremorigenic mycotoxin, on BK channels and demonstrate its utility for studying vascular function in vitro and in vivo. Whole-cell currents from human embryonic kidney 293 cells transfected with hSlo α or α + β1 were blocked >95% by penitrem A (IC(50) 6.4 versus 64.4 nM; p < 0.05). Furthermore, penitrem A inhibited BK channels in inside-out and cell-attached patches, whereas iberiotoxin could not. Inhibitory effects of penitrem A on whole-cell K(+) currents were equivalent to iberiotoxin in canine coronary smooth muscle cells. As for specificity, penitrem A had no effect on native delayed rectifier K(+) currents, cloned voltage-dependent Kv1.5 channels, or native ATP-dependent K(ATP) current. Penitrem A enhanced the sensitivity to K(+)-induced contraction in canine coronary arteri...Continue Reading

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Citations

Jan 31, 2014·Channels·Trey S RottgenGregory M Dick
Nov 26, 2014·Journal of Psycholinguistic Research·Noam Chomsky
Jul 6, 2014·American Journal of Physiology. Regulatory, Integrative and Comparative Physiology·Georgi V Petkov
Jan 8, 2019·Applied Microbiology and Biotechnology·László KozákIstván Molnár
Feb 6, 2017·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Barry D KyleAndrew P Braun
Mar 19, 2021·PloS One·Mieczysława Irena BoguśMartyna Boguś-Sobocińska

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