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Peptides. 2006 Nov;27(11):2967-75. Epub 2006 Aug 17.

Effect of novel selective non-peptide kinin B(1) receptor antagonists on mouse pleurisy induced by carrageenan.

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  • 1Department of Pharmacology, Centre of Biological Sciences, Universidade Federal de Santa Catarina, Campus Universit├írio, Trindade, 88049-900 Florian├│polis, SC, Brazil.


Two novel selective non-peptide kinin B(1) receptor antagonists, the benzodiazepine antagonist and SSR240612, were evaluated in carrageenan-induced mouse pleurisy. The peptide R-715 (0.5 mg/kg, i.p.) and the non-peptide benzodiazepine (3 mg/kg, i.p.) antagonists significantly decreased cellular migration (predominantly neutrophils), without altering plasma exudation. SSR240612 (1 mg/kg, i.p.) diminished total cells and neutrophils, besides exudation. Oral administration of SSR240612 (10 mg/kg) also reduced total cell and neutrophil counts. Only the benzodiazepine antagonist inhibited the lung myeloperoxidase activity. No tested antagonist significantly altered the lung and pleural TNFalpha and IL-1beta production. We provide interesting evidence on the anti-inflammatory in vivo effects of non-peptide B(1) receptor antagonists.

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