Document Detail


Cardiac effects of a selective rho-associated kinase inhibitor, Y-27632, assessed in canine isolated, blood-perfused heart preparations.
MedLine Citation:
PMID:  11949893     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Chronotropic, inotropic and coronary effects of Y-27632 ((+)-(R)-trans-4-(1-aminoethyl)-N-(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.
Authors:
Atsushi Sugiyama; Yutaka Yatomi; Akira Takahara; Yoshioki Satoh; Keitaro Hashimoto
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Japanese journal of pharmacology     Volume:  88     ISSN:  0021-5198     ISO Abbreviation:  Jpn. J. Pharmacol.     Publication Date:  2002 Mar 
Date Detail:
Created Date:  2002-04-12     Completed Date:  2002-10-04     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  2983305R     Medline TA:  Jpn J Pharmacol     Country:  Japan    
Other Details:
Languages:  eng     Pagination:  359-61     Citation Subset:  IM    
Affiliation:
Department of Pharmacology, Yamanashi Medical University, Nakakoma-gun, Japan. atsushis@res.yamanashi-med.ac.jp
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MeSH Terms
Descriptor/Qualifier:
Amides / pharmacology*
Animals
Coronary Circulation / drug effects
Cross Circulation
Dogs
Enzyme Inhibitors / pharmacology*
Female
Heart / drug effects*
Heart Rate / drug effects
Intracellular Signaling Peptides and Proteins
Male
Myocardial Contraction / drug effects
Perfusion
Protein-Serine-Threonine Kinases / antagonists & inhibitors*
Pyridines / pharmacology*
Sinoatrial Node / drug effects
Vasodilation / drug effects
rho-Associated Kinases
Chemical
Reg. No./Substance:
0/Amides; 0/Enzyme Inhibitors; 0/Intracellular Signaling Peptides and Proteins; 0/Pyridines; 138381-45-0/Y 27632; EC 2.7.11.1/Protein-Serine-Threonine Kinases; EC 2.7.11.1/rho-Associated Kinases

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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