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FR167344 free base

CAS No. : 215258-13-2

MCE 站：FR167344 free base

产品活性：FR167344 free base是有口服活性，非多肽的缓激肽受体B2 (bradykinin receptor B2) 拮抗剂，对B2有高亲和力，IC₅₀值为65 nM，对B1受体没有结合力。

研究领域：GPCR/G Protein

作用靶点：Bradykinin Receptor

In Vitro: 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.

In Vivo: 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.

相关产品：Bradykinin  |  Icatibant  |  [Des-Arg9]-Bradykinin acetate  |  ELN-441958  |  Lys-[Des-Arg9]Bradykinin TFA  |  Bradykinin (2-9)  |  Bradykinin (1-5)  |  Bradykinin (1-6)  |  Retrobradykinin  |  [Hyp3]-Bradykinin  |  Bradykinin (1-3)  |  Bradykinin (1-7)

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