产品描述:
SSR 240612 is a selective, non-peptide antagonist of the bradykinin B1 receptor (Kis = 0.48-0.73 and 358-481 nM for B1 and B2 receptors, respectively).{45045} It inhibits the contraction of rabbit aorta and rat ileum induced by the B1 receptor agonist des-Arg9-bradykinin (des-Arg9-BK) ex vivo in a concentration-dependent manner. SSR 240612 (0.3 mg/kg) reduces tissue damage and neutrophil accumulation in a rat model of splanchnic artery occlusion/reperfusion-induced intestinal injury and inhibits des-Arg9-BK-induced paw edema in mice when administered orally at doses of 3 and 10 mg/kg or intraperitoneally at doses of 0.3 and 1 mg/kg. SSR 240612 (10 mg/kg per day) reduces fibrosis in a unilateral ureteral obstruction mouse model of kidney fibrosis.{45046} It also reduces mean arterial blood pressure in two rat models of hypertension when administered at doses of 5 and 10 mg/kg and reduces plasma glucose and insulin levels in a glucose-fed rat model of insulin resistance when administered at a dose of 10 mg/kg per day.{45047,45048} SSR 240612 also exhibits analgesic properties in several rodent models of hyperalgesia.{45045}