Akinori Ueno, Hiroaki Naraba and Sachiko Oh-ishi (*)
Department of Pharmacology, School of Pharmaceutical Sciences, Kitasato
University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan
(*) To whom correspondence should be addressed.
Abstract: A novel non-peptide bradykinin B2-receptor agonist,
FR190997 (8-[2,6-dichloro-3-[N-[(E)-4-(N-methylcarbamoyl) cinnamidoacetyl]-N-methylamino]
benzyloxy]-2-methyl-4-(2-pyridylmethoxy) quinoline), induced dose-dependent
and longer-lasting swelling than bradykinin in the mouse paw. The swelling,
peaking around 30 min, was suppressed dose-dependently by intraperitoneal
administration of FR173657, a novel non-peptide B2-receptor antagonist.
A known B2-antagonist, Hoe 140, also significantly suppressed this edema.
The result indicates that the novel B2-agonist FR190997, being more stable
than bradykinin, could induce plasma exudation locally in mice via the B2-receptor
as a substitute for bradykinin.
Keywords: Bradykinin B2-receptor agonist, FR190997, Mouse paw edema