Description
| Description | FR167344 free base is an orally active and nonpeptide antagonist of bradykinin receptor B2. FR167344 free base displays a high-affinity binding to the B2 receptor (IC50: 65 nM). It has no binding affinity for the B1 receptor. |
| Targets&IC50 | Bradykinin receptor B2:65 nM |
| In vitro | FR167344 shows no stimulatory effects on PI hydrolysis. FR167344 inhibits the B2 receptor-mediated phosphatidylinositol (PI) hydrolysis and produces a concentration-dependent rightward shift in the dose-response curve to bradykinin, in competitive experiments using membranes prepared from Chinese hamster ovary cells expressing the bradykinin receptor subtypes. 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 [1]. |
| In vivo | FR167344 (p.o.; 2h; carrageenin injection) inhibits carrageenin-induced paw oedema in rats (ID50: 2.7 mg/kg). FR167344 (p.o.) inhibits kaolin-induced writhing in mice (ID50: 2.8 mg/kg in 10 min writhing and 4.2 mg/kg in 15 min writhing). FR167344(p.o.) inhibits caerulein-induced pancreatic oedema (ID50: 13.8 mg/kg) and it also increases in amylase and lipase of blood samples (ID50: 10.3 and 7.4 mg/kg, respectively, in rats) [2]. |
| Molecular Weight |
673.38 |
| Formula | C30H28BrCl2N5O4 |
| CAS No. | 215258-13-2 |
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
