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编 号：F120069
分子式：C26H23ClN6O2S
分子量：519.02
分子式：C26H23ClN6O2S
分子量：519.02
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CAS No: 132418-35-0
产品详情
生物活性：
Setipafant is a platelet-activating factor (PAF) antagonist.
体内研究：
Animals are separated into six groups: U4, controls; S, sham operated animals undergoing laparotomy; I4 and I9, ligation of the mesenteric vessels in the last ileal loop; IT4 and IT9, same procedure together with treatment with Setipafant (50 mg/kg) orally before and after surgery and intraperitoneally during surgery.Animals are killed at day 4 in groups U4, S, I4 and IT4 and at day 9 in groups I9 and IT9, with histological studies and mediator measurements taken. Macroscopic and histological lesions of intestinal wall in groups I4, I9, IT4 and IT9 are similar to those of human neonatal necrotizing enterocolitis and do not vary according to the absence or the presence of Setipafant (BN 50727) treatment. Peritoneal bands are significantly reduced in treated groups IT4 and IT9 as compared with untreated ones I4 and I9. Mucosal PAF levels in the terminal ileum are higher in group I4 than in groups U4 or I9. In the upper loop, mucosal PAF levels are comparable in all groups. An increase in stool PAF levels is observed only in group I9, whereas values comparable to those observed in controls are detected in other groups. Pretreatment of the animals with one or other of the structurally unrelated PAF receptor antagonists, BN 52021 (10 mg/kg, i.p.) or BN 50727 (1 mg/kg, i.p.) significantly reduces Dexamethasone-induced gastric damage. In these animals neither petechiae nor erosions are observed.
Setipafant is a platelet-activating factor (PAF) antagonist.
体内研究：
Animals are separated into six groups: U4, controls; S, sham operated animals undergoing laparotomy; I4 and I9, ligation of the mesenteric vessels in the last ileal loop; IT4 and IT9, same procedure together with treatment with Setipafant (50 mg/kg) orally before and after surgery and intraperitoneally during surgery.Animals are killed at day 4 in groups U4, S, I4 and IT4 and at day 9 in groups I9 and IT9, with histological studies and mediator measurements taken. Macroscopic and histological lesions of intestinal wall in groups I4, I9, IT4 and IT9 are similar to those of human neonatal necrotizing enterocolitis and do not vary according to the absence or the presence of Setipafant (BN 50727) treatment. Peritoneal bands are significantly reduced in treated groups IT4 and IT9 as compared with untreated ones I4 and I9. Mucosal PAF levels in the terminal ileum are higher in group I4 than in groups U4 or I9. In the upper loop, mucosal PAF levels are comparable in all groups. An increase in stool PAF levels is observed only in group I9, whereas values comparable to those observed in controls are detected in other groups. Pretreatment of the animals with one or other of the structurally unrelated PAF receptor antagonists, BN 52021 (10 mg/kg, i.p.) or BN 50727 (1 mg/kg, i.p.) significantly reduces Dexamethasone-induced gastric damage. In these animals neither petechiae nor erosions are observed.
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