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Effect of YM-254890, a specific Galphaq/11 inhibitor, on experimental peripheral arterial disease in rats.

Abstract
The protective effect of YM-254890, a specific Galphaq/11 inhibitor, on laurate-induced peripheral arterial disease in rats was compared with those of prostaglandin E1 (PGE1), beraprost, and clopidogrel. YM-254890 inhibited ADP-induced ex vivo rat platelet aggregation at a dose of 3 microg/kg. Furthermore, YM-254890 strongly inhibited phenylephrine-, serotonin- and endothelin-1-induced contractions in the rat aorta, and improved dermal blood flow after the laurate injection. The intra-arterial single bolus administration of YM-254890 15 min after the laurate injection dose-dependently inhibited the progression of the lesion, with significance, at 3 microg/kg without affecting systemic blood pressure. PGE1 and beraprost, when administered before the laurate injection, were effective, but their potencies were less than that of YM-254890. Clopidogrel significantly suppressed lesion progression when administered at 30 mg/kg twice a day for 3 days, which completely inhibited platelet aggregation. These results suggest that the local administration of YM-254890 may be useful for treating peripheral arterial disease.
AuthorsToshio Uemura, Hajime Takamatsu, Tomihisa Kawasaki, Masatoshi Taniguchi, Eisaku Yamamoto, Yuichi Tomura, Wataru Uchida, Keiji Miyata
JournalEuropean journal of pharmacology (Eur J Pharmacol) Vol. 536 Issue 1-2 Pg. 154-61 (Apr 24 2006) ISSN: 0014-2999 [Print] Netherlands
PMID16566917 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Lauric Acids
  • Peptides, Cyclic
  • Platelet Aggregation Inhibitors
  • Vasodilator Agents
  • YM-254890
  • lauric acid
  • beraprost
  • Clopidogrel
  • Epoprostenol
  • GTP-Binding Protein alpha Subunits, Gq-G11
  • Ticlopidine
Topics
  • Animals
  • Aorta (drug effects, physiology)
  • Blood Flow Velocity (drug effects)
  • Blood Pressure (drug effects)
  • Clopidogrel
  • Dermis (blood supply, drug effects)
  • Dose-Response Relationship, Drug
  • Endothelium, Vascular (physiology)
  • Epoprostenol (analogs & derivatives, pharmacology)
  • GTP-Binding Protein alpha Subunits, Gq-G11 (antagonists & inhibitors)
  • Heart Rate (drug effects)
  • Hindlimb (blood supply, drug effects)
  • In Vitro Techniques
  • Lauric Acids
  • Male
  • Peptides, Cyclic (pharmacology)
  • Peripheral Vascular Diseases (chemically induced, pathology, prevention & control)
  • Platelet Aggregation (drug effects)
  • Platelet Aggregation Inhibitors (pharmacology)
  • Rats
  • Rats, Sprague-Dawley
  • Ticlopidine (analogs & derivatives, pharmacology)
  • Vasodilation (drug effects)
  • Vasodilator Agents (pharmacology)

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