Effects of the K+ channel blockers paspalitrem-C and paxilline on mammalian smooth muscle

European Journal of Pharmacology
F P DeFariasG Suarez-Kurtz

Abstract

The tremorgenic alkaloids, paxilline and paspalitrem-C (0.1-10 microM), increased the spontaneous contractility of guinea-pig and rat urinary bladder, and rat duodenum, and induced tension in guinea-pig trachea. These effects are ascribed to blockade of high-conductance, Ca(2+)-activated K+ (BKCa) channels. Paxilline potentiated the charybdotoxin-induced stimulation of guinea-pig detrusor muscle; this is consistent with the alkaloid's ability to allosterically enhance the binding of charybdotoxin to smooth muscle membranes (Knaus et al., 1994). Paspalitrem-C and paxilline did not affect the myogenic activity of isolated portal vein from guinea-pig, which is insensitive to charybdotoxin, or of that from rat which is stimulated by charybdotoxin. Paxilline and paspalitrem-C also differed from charybdotoxin in that the alkaloids did not consistently elicit tension in guinea-pig aortic rings. These discrepancies are attributed to differences in relative potency, sites and/or mechanisms of action of the indole alkaloids vs. peptidyl blockers of the BKCa channel.

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Citations

Jan 10, 2002·European Journal of Pharmacology·R Vianna-JorgeG Suarez-Kurtz
Nov 22, 1997·European Journal of Pharmacology·G Suarez-KurtzG J Kaczorowski
Feb 10, 2000·European Journal of Pharmacology·E J MolinariM Gopalakrishnan
Aug 17, 2012·American Journal of Physiology. Renal Physiology·Tanchun WangRobert S Moreland
Jan 22, 2010·PloS One·Wendy L ImlachJulie E Dalziel
Feb 12, 2008·Mycological Research·Sanjay SaikiaBarry Scott
Jan 29, 2005·British Journal of Pharmacology·Ticiana Camila Mora, Guilherme Suarez-Kurtz
Jul 27, 1999·Current Opinion in Chemical Biology·G J Kaczorowski, M L Garcia
Sep 28, 2000·The Journal of Pharmacy and Pharmacology·M S MukerjiH Huddart
Jul 6, 2014·American Journal of Physiology. Regulatory, Integrative and Comparative Physiology·Georgi V Petkov
Dec 20, 2013·American Journal of Physiology. Cell Physiology·Kiril L HristovGeorgi V Petkov
Aug 31, 2013·Journal of Animal Science·J E DalzielS C Finch
May 30, 2019·Toxins·Priyanka ReddySimone Rochfort

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