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Rho-kinase inhibitors show promise in pulmonary hypertension.

Abstract
In pulmonary arterial hypertension, it is necessary to obtain a vasodilation that is selective for the pulmonary circulation. Ras human orthologue (Rho)/Rho-kinase-mediated Ca2+ sensitisation plays a central role in mediating the sustained vasoconstriction and increased vasoreactivity in the rat hypoxic model of pulmonary hypertension. Rho-kinase inhibitors (Y-27632 and/or fasudil) have been shown to reduce pulmonary arterial pressure in three rat models of pulmonary hypertension. The first clinical study to report the effects of a Rho-kinase inhibitor in pulmonary hypertension enrolled nine patients with severe pulmonary hypertension. Fasudil hydrochloride 30 mg for 30 min i.v. caused a slight decrease in the mean pulmonary artery pressure and increase in the cardiac index but neither of these responses was significant. However, fasudil caused a significant decrease in pulmonary vascular resistance. Rho-kinase inhibitors may be useful in pulmonary hypertension, and should undergo further development for this indication.
AuthorsSheila A Doggrell
JournalExpert opinion on investigational drugs (Expert Opin Investig Drugs) Vol. 14 Issue 9 Pg. 1157-9 (Sep 2005) ISSN: 1744-7658 [Electronic] England
PMID16144499 (Publication Type: Journal Article, Review)
Chemical References
  • Intracellular Signaling Peptides and Proteins
  • Protein Kinase Inhibitors
  • Protein Serine-Threonine Kinases
  • rho-Associated Kinases
Topics
  • Animals
  • Humans
  • Hypertension, Pulmonary (drug therapy, enzymology)
  • Intracellular Signaling Peptides and Proteins
  • Protein Kinase Inhibitors (chemistry, pharmacology, therapeutic use)
  • Protein Serine-Threonine Kinases (antagonists & inhibitors, metabolism)
  • rho-Associated Kinases

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