The inhibitory effects of N2-dansyl-l-arginine-4-t-butylpiperidine amide (TI 233) on contraction of vascular and intestinal smooth muscle
Open Access
- 1 November 1983
- journal article
- research article
- Published by Wiley in British Journal of Pharmacology
- Vol. 80 (3) , 519-525
- https://doi.org/10.1111/j.1476-5381.1983.tb10724.x
Abstract
1 Effects of N2-dansyl-l-arginine-4-t-butylpiperidine amide (TI 233) on the contractions in vascular and intestinal smooth muscles were examined. 2 High K-induced sustained contractions in the smooth muscles were inhibited by TI 233 with an IC50 of 2.1 × 10−5m for rabbit aorta and 3.6 × 10−6m for guinea-pig taenia coli in a solution containing 1.5 mm Ca. Initial transient contraction induced by K in taenia coli was less sensitive to the inhibitory effect of TI 233. When the Ca concentration in the medium was decreased to 0.3 mm, the concentration-inhibition curves for TI 233 shifted to the left in both aorta and taenia coli. Increasing the Ca concentration to 7.5 mm shifted the curve to the right in the aorta. TI 233 also inhibited the noradrenaline-induced contraction in the aorta (IC50 = 2.1 × 10−5 m). 3 In a hypoxic solution without added glucose, the inhibitory effect of TI 233 on the K-induced contraction in aorta was augmented. In the presence of high concentrations (40 mm) of glucose in hypoxia, TI 233 did not inhibit the noradrenaline-induced contraction of the aorta. Hypoxia and a high concentration of glucose also decreased the inhibitory effect of TI 233 on the K-induced contraction in taenia coli. 4 TI 233 inhibited the K-induced increase in cellular Ca content measured by a modified lanthanum method. 5 TI 233 decreased oxygen consumption and ATP content of resting and K-stimulated aorta and taenia coli. 6 It was concluded that TI 233 inhibits the vascular and intestinal smooth muscle contraction by a Ca antagonistic action and also by inhibition of aerobic metabolism.This publication has 21 references indexed in Scilit:
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