FR167344 free base |
カタログ番号GC31926 |
FR167344 遊離塩基は、経口で活性な非ペプチド ブラジキニン受容体 B2 アンタゴニストです。
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Cas No.: 215258-13-2
Sample solution is provided at 25 µL, 10mM.
FR167344 free base is an orally active, nonpeptide bradykinin receptor B2 antagonist. FR167344 free base shows a high affinity binding to the B2 receptor with an IC50 value of 65 nM and no binding affinity for the B1 receptor.
In competitive experiments using membranes prepared from Chinese hamster ovary cells expressing the bradykinin receptor subtypes, FR167344 shows a high affinity binding to the B2 receptor with IC50 values of 65 nM, and no binding affinity for the B1 receptor. FR167344 inhibits the B2 receptor-mediated phosphatidylinositol (PI) hydrolysis and produces a concentration-dependent rightward shift in the dose-response curve to bradykinin. This shift is accompanied by a progressive reduction of maximal response. Estimated pA2 values for the antagonism of bradykinin induced PI hydrolysis by FR167344 is 8.0. FR167344 shows no stimulatory effects on PI hydrolysis[1].
Oral administration of FR167344 inhibits carrageenin-induced paw oedema in rats with an ID50 of 2.7 mg/kg at 2h after carrageenin injection. Oral administration of FR167344 inhibits kaolin-induced writhing in mice with an ID50 of 2.8 mg/kg in 10 min writhing and 4.2 mg/kg in 15 min writhing. Oral administration of FR167344 inhibits caerulein-induced pancreatic oedema with an ID50 of 13.8 mg/kg as well as increases in amylase and lipase of blood samples with ID50 of 10.3 and 7.4 mg/kg, respectively, in rats[2].
[1]. Aramori I, et al. Novel subtype-selective nonpeptide bradykinin receptor antagonists FR167344 and FR173657. Mol Pharmacol. 1997 Feb;51(2):171-6. [2]. Asano M, et al. Effects of a nonpeptide bradykinin B2 receptor antagonist, FR167344, on different in vivoanimal models of inflammation.Br J Pharmacol. 1997 Dec;122(7):1436-40.
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