Characterization of responses to cromakalim and pinacidil in smooth and cardiac muscle by use of selective antagonists

British Journal of Pharmacology
G A McPherson, J A Angus

Abstract

1. In dog isolated coronary artery (precontracted with endothelin, 10 nM) cromakalim (0.1-30 microM) and pinacidil (1-30 microM) produced concentration-dependent vasorelaxant responses. The effects of these compounds could be blocked by glibenclamide (3 microM), phentolamine (30 microM) or alinidine (30 microM) to a similar extent, indicating that both agents alter vascular tone through the same mechanism in this preparation. 2. The ability of the antagonists glibenclamide, phentolamine and alinidine to block the response to cromakalim in a number of smooth muscle types from the guniea-pig was determined. Cromakalim (0.1-30 microM) produced concentration-dependent relaxant responses in thoracic aorta (precontracted with endothelin, 30 nM), ileum (precontracted with K+, 25 mM) and trachea (spontaneously contracted). Responses to cromakalim in all tissues could be blocked by the three antagonists. However, significantly higher concentrations of the antagonists were required to block responses in the thoracic aorta than in the ileum or trachea. Given that the rank order of potency of the antagonists was similar in all tissues (i.e. glibenclamide greater than phentolamine = alinidine), this result may suggest vascular K+ channels o...Continue Reading

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Citations

Nov 1, 1992·Medicinal Research Reviews·K S Atwal
Nov 3, 2006·European Journal of Nutrition·Arif-ullah Khan, Anwarul Hassan Gilani
Apr 7, 1992·European Journal of Pharmacology·R A Lefebvre, J Horacek
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Feb 5, 2003·Progress in Biophysics and Molecular Biology·Susumu Seino, Takashi Miki
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Aug 1, 1993·Pharmacology & Toxicology·S Mellemkjaer, F Nielsen-Kudsk
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