Ca(2+) entry blocking and contractility promoting actions of norbormide in single rat caudal artery myocytes

British Journal of Pharmacology
Fabio FusiSergio Bova

Abstract

1 Aim of the present study was to investigate the effects of norbormide, a selective vasoconstrictor agent of the rat peripheral vessels, on the whole-cell voltage-dependent L-type Ca(2+) current (I(Ca(L))) of freshly isolated smooth muscle cells from the rat caudal artery, using either the conventional or the amphotericin B-perforated whole-cell patch-clamp method. 2 Norbormide decreased L-type Ca(2+) current in a concentration- and voltage-dependent manner, without modifying the threshold and the maximum of the current-voltage relationship. Norbormide-induced I(Ca(L)) inhibition was reversible upon wash-out. 3 Norbormide both shifted the voltage dependence of the steady-state inactivation curve to more negative potentials by about 16 mV, without affecting the activation curve, and decreased the slope of inactivation. Norbormide, however, did not modify both the activation and the inactivation kinetics of the I(Ca(L)). 4 Norbormide decreased I(Ca(L)) progressively during repetitive step depolarizations, with inhibition depending on the stimulation frequency (use-dependent block) as well as on the holding potential. 5 Addition of 50 micro M norbormide caused the contraction of all freshly isolated cells and also of those impale...Continue Reading

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Citations

Jun 12, 2003·European Journal of Pharmacology·Sergio BovaFabio Fusi
May 7, 2003·The Journal of Steroid Biochemistry and Molecular Biology·Giuliano NeriGastone G Nussdorfer
Oct 11, 2016·Frontiers in Pharmacology·Claudio D'AmoreSergio Bova
Jun 15, 2005·Biochimica Et Biophysica Acta·Fernanda RicchelliSergio Bova
Jan 25, 2005·The Journal of Pharmacology and Experimental Therapeutics·Fabio FusiSimona Saponara
Nov 20, 2009·The Journal of Pharmacology and Experimental Therapeutics·Fabio FusiSimona Saponara
May 5, 2016·Chemistry & Biodiversity·Hans ChoiDavid Rennison
Feb 27, 2007·Bioorganic & Medicinal Chemistry·David RennisonMargaret A Brimble
May 19, 2007·Biochimica Et Biophysica Acta·Alessandra ZulianFernanda Ricchelli

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