Fasitibant chloride (MEN16132 free base) is a powerful and specific nonpeptide antagonist of the bradykinin B2 receptor (B2R). This compound effectively reduces joint pain and mitigates joint edema in a rat model of Carrageenan-induced arthritis.

Fasitibant chloride (MEN16132 free base; 1 μM; pre-treatment 30 min before BK) produces a consistent reduction of the FGF-2 expression (BK induced) and decrement of BK induced-FGFR-1 phosphorylation[2]. Fasitibant chloride inhibits the phosphorylation of FRSα, ERK1/2, STAT3 (BK induced; 1 μM; for 15 min), except AKT in HUVEC[2]. Cell Viability Assay[2]Cell Line: human umbilical vein endothelial cells (HUVEC) Concentration: 1 μM Incubation Time: Pre-treatment 30 min before Bradykinin (BK; 1 μM; for 24 h) Result: Produced a consistent reduction of the FGF-2 expression (BK induced) and decrement of BK induced-FGFR-1 phosphorylation (without affecting FGFR-2 activity).

Fasitibant chloride (MEN16132 free base; 100 μg per knee; injection into the knee; 30 min before λ-carrageenan) inhibits about 40-45% on the carrageenan-induced joint pain and knee joint oedema[1]. Animal Model: Male Wistar rats weighing 250-300 g[1]Dosage: 100 μg per knee Administration: Injection into the knee; 30 min before λ-carrageenan Result: Inhibited about 40-45% on the carrageenan-induced joint pain and knee joint oedema. Reduced the neutrophil infiltration in the synovium by about 60% and the release of prostaglandins by about 30%.