Cardiac Effects of a Selective Rho-Associated Kinase Inhibitor, Y-27632, Assessed in Canine Isolated, Blood-Perfused Heart Preparations
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Chronotropic, inotropic and coronary effects of Y-27632 ((+)-(<i>R</i>)-<i>trans</i>-4-(1-aminoethyl)-<i>N</i>-(4-pyridyl) cyclohexanecarboxamide dihydrochloride, monohydrate), a specific inhibitor of Rho-associated coiled-coil forming protein serine/threonine kinase (ROCK), were assessed using canine isolated, blood-perfused heart preparations. Y-27632 slightly enhanced sinoatrial automaticity and significantly increased coronary blood flow, while it decreased ventricular contraction. The concentrations of Y-27632 needed to cause the currently observed changes were similar to those inhibiting ROCK in a previous in vitro study. These results suggest that the constitutional ROCK in the heart mainly regulates the ventricular contractility and coronary vascular tone rather than the sinoatrial automaticity.
- The Japanese Journal of Pharmacology
The Japanese Journal of Pharmacology 88(3), 359-361, 2002-03-01
The Japanese Pharmacological Society