Effects of khellin on contractile responses and 45Ca2+ movements in rat isolated aorta

Journal of Pharmacy and Pharmacology - Tập 43 Số 1 - Trang 46-48 - 1991
Amalia Úbeda1, Teresa Tejerina2, Juan Tamargo2, Angel Villar3
1Department of Pharmacology, Laboratory of Pharmacognosy and Pharmacodynamics, School of Pharmacy, Blasco [bañez 13, 46010 Valencia, Spain
2Department of Pharmacology, School of Medicine, Universidad Complutense, 28040, Madrid, Spain
3Department of Pharmacology, School of Pharmacy, Universidad Complutense, 28040 Madrid, Spain

Tóm tắt

Abstract The effects of khellin on contractile responses and 45Ca2+ flux have been studied in rat isolated aortae. Khellin (10−5- 3.2 times 10−4M) produced a concentration-dependent inhibition of noradrenaline (10−6 M) and high K+ (80 mM)-induced contractions. At 3.2 times 10−4 M, khellin increased cAMP levels and reduced 45Ca2+ influx in resting tissues and in tissues stimulated by noradrenaline (10−5 M) and high K+ without affecting basal 45Ca2+ efflux or noradrenaline induced 45Ca2+ efflux. It is concluded that in rat isolated aorta, khellin caused a non-specific inhibition of Ca2+ influx but may also exhibit intracellular actions, thus decreasing the availability of Ca2+ required for activation. One or more of these mechanisms may be related to an increase in intracellular cAMP levels.

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