生物活性 | |||
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描述 | SSR240612 is a novel non-peptide antagonist of the bradykinin B1 receptor, with 500-1,000 fold selectivity for B1 over B2. It could inhibit the binding of peptide [3H]Lys0-des-Arg9-BK to bradykinin B1 receptor with Ki values of 0.48 and 0.73 nM for human fibroblast MRC5 and human embryonic kidney cells expressing recombinant human B1 receptor, respectively. SSR240612 antagonized Lys0-desAr9-BK both in vitro and in vivo. It inhibited Lys0-desAr9-BK-induced inositol monophosphate formation in MRC5 with an IC50 of 1.9 nM. Administration of SSR240612 at dose of 3 and 10 mg/kg p.o., or 0.3 and 1 mg/kg i.p., inhibited desAr9-BK-induced paw edema in mice[1]. Oral administration of SSR240612 at dose of 10mg/kg once daily for 7 days reversed low state inflammation in adipose tissue and plasma fatty acids changes associated with insulin resistance in glucose-fed rats[2]. | ||
作用机制 | SSR240612 is a competitive inhibitor of bradykinin B1 receptor.[1] |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.26mL 0.25mL 0.13mL |
6.30mL 1.26mL 0.63mL |
12.60mL 2.52mL 1.26mL |
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