Vasorelaxant properties of norbormide, a selective vasoconstrictor agent for the rat microvasculature

British Journal of Pharmacology
S BovaGabriella Cargnelli

Abstract

1. The effects of norbormide on the contractility of endothelium-deprived rat, guinea-pig, mouse, and human artery rings, and of freshly isolated smooth muscle cells of rat caudal artery were investigated. In addition, the effect of norbormide on intracellular calcium levels of A7r5 cells was evaluated. 2. In resting rat mesenteric, renal, and caudal arteries, norbormide (0.5-50 microM) induced a concentration-dependent contractile effect. In rat caudal artery, the contraction was very slowly reversible on washing, completely abolished in the absence of extracellular calcium, and antagonized by high concentrations (10-800 microM) of verapamil. The norbormide effect persisted upon removal of either extracellular Na+ or K+. The contractile effect of norbormide was observed also in single, freshly isolated smooth muscle cells from rat caudal artery. 3. In resting rat and guinea-pig aortae, guinea-pig mesenteric artery, mouse caudal artery, and human subcutaneous resistance arteries, norbormide did not induce contraction. When these vessels were contracted by 80 mM KCl, norbormide (10-100 microM) caused relaxation. Norbormide inhibited the response to Ca2+ of rat aorta incubated in 80 mM KCl/Ca2(+)-free medium. Norbormide (up to 10...Continue Reading

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Citations

Jun 12, 2003·European Journal of Pharmacology·Sergio BovaFabio Fusi
Aug 15, 2002·International Journal of Pharmaceutics·Allan Nadian, Louise Lindblom
May 7, 2003·The Journal of Steroid Biochemistry and Molecular Biology·Giuliano NeriGastone G Nussdorfer
Jul 1, 2009·Environmental Toxicology and Pharmacology·Shanthinie RavindranMalcolm Tingle
Jan 1, 2009·Environmental Toxicology and Pharmacology·Shanthinie RavindranMalcolm Tingle
Jun 15, 2005·Biochimica Et Biophysica Acta·Fernanda RicchelliSergio Bova
May 19, 2007·Biochimica Et Biophysica Acta·Alessandra ZulianFernanda Ricchelli
Oct 11, 2016·Frontiers in Pharmacology·Claudio D'AmoreSergio Bova
May 22, 2004·Journal of Pharmacological Sciences·Maura FloreaniPaola Dorigo
May 18, 2004·The Journal of Clinical Investigation·Martina J Sinnegger-BraunsJörg Striessnig
May 5, 2016·Chemistry & Biodiversity·Hans ChoiDavid Rennison
Dec 7, 2018·Molecular Diversity·Xuelian LiuZhaohai Qin
Feb 27, 2007·Bioorganic & Medicinal Chemistry·David RennisonMargaret A Brimble

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