Pharmacological evaluation of a selective bradykinin B₁ antagonist in a canine model of arthritis

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• 作者：B. A. Duclos ; C. A. Rugg ; J. White ; J. T. Ross ; M. Darling ; D. Huczek ; J. Curry ; S. Alexander-Bowman ; A. Townley ; D. Garcia-Tapia ; C. Chio and S. Kamerling
• 刊名：Journal of Veterinary Pharmacology and Therapeutics
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：40
• 期：1
• 页码：70-76
• 全文大小：438K
• ISSN：1365-2885

文摘

The effects of a selective bradykinin 1 receptor antagonist, compound A, were evaluated in a canine model of acute inflammatory model of arthritis. Despite detection of the B₁ receptor in canine type B synoviocytes using a fluorescent ligand, oral administration of compound A (9 and 27 mg/kg) did not improve weight bearing of dogs injected intra-articularly with IL-1β in a force plate analysis. Analysis of the synovial fluid of IL-1β-treated dogs indicated high levels of bradykinin postchallenge. Excellent exposure, coupled with evidence of the presence of the B₁ receptor during an acute inflammatory model of pain, indicates an inability of the receptor to mediate inflammatory pain in canines.