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Updated: Jun 24, 2026

Bladder Smooth Muscle Strip Contractility as a Method to Evaluate Lower Urinary Tract Pharmacology
Published on: August 18, 2014
Effects of a new PAR1 antagonist, F 16618, on smooth muscle cell contraction
Arnaud Bocquet1, Robert Létienne, Sylvie Sablayrolles
1Centre de Recherche Pierre Fabre, Castres Cedex, France.
Abstract:
This study evaluated the effects of two PAR1 antagonists on vessels contracted by SFLLR. ER 121958 antagonized the SFLLR-induced contraction on rat denuded superior mesenteric artery and pig coronary artery in a non-competitive manner (IC(50) values were 22 [7.5-43.6] nM and 2.9 [2.09-4.02] nM, respectively). F 16618 inhibited the SFLLR-induced superior mesenteric arteries and coronary arteries contraction in a competitive manner (pA(2) values of 7.3 and 6.2, respectively). PAR1 antagonists do not affect vessel resting tension or haemodynamic parameters in anaesthetized rats. Thus, PAR1 antagonists could have beneficial effects against vasospasm due to vessel injury.
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