The effect of S-(+)-boldine on the alpha 1-adrenoceptor of the guinea-pig aorta

British Journal of Pharmacology
S ChuliáC Advenier

Abstract

1. The cardiovascular activity of S-(+)-boldine, an aporphine alkaloid structurally related to papaverine, was determined. The work includes functional studies on guinea-pig isolated aorta contracted with noradrenaline, caffeine, KCl or Ca2+, and on guinea-pig trachea contracted with acetylcholine or histamine. 2. S-(+)-boldine inhibited in a concentration-dependent manner the contractile response evoked by noradrenaline (10 microM) in guinea-pig aorta (IC50 = 1.4 +/- 0.2 microM) while the KCl depolarizing solution (60 mM)- or the Ca2+ (1 mM)-induced contractions were only partially affected by boldine up to 300 microM. In contrast, papaverine relaxed noradrenaline (NA), KCl or Ca2+ induced contractions showing similar IC50 values in all cases. S-(+)-boldine had a greater potency on the contraction elicited by NA whereas papaverine acted in a non-selective manner. 3. S-(+)-boldine was found to be an alpha 1-adrenoceptor blocking agent in guinea-pig aorta as revealed by its competitive antagonism of noradrenaline-induced vasoconstriction (pA2 = 5.64 +/- 0.08), and its potency was compared with that of prazosin (pA2 = 8.56 +/- 0.24), a known potent alpha 1-adrenoceptor antagonist. In contrast, papaverine caused rightward shifts o...Continue Reading

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Citations

Sep 27, 2003·European Journal of Pharmacology·Hisatoshi Tsuchida, Yasushi Ohizumi
Aug 1, 1997·British Journal of Pharmacology·J CortijoR C Small
Oct 14, 2005·Chemico-biological Interactions·Peter O'BrienHernán Speisky
Apr 16, 1998·Japanese Journal of Pharmacology·J J KangW M Fu
Dec 14, 2011·Experimental Biology and Medicine·Yeh-Siang LauMohd Rais Mustafa

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