LY 255283 是白三烯 B4 (LTB4) 受体的特异性拮抗剂,抑制人外周血多形核白细胞和由钙离子载体 A23187 激活的单核细胞中 LTB(4) 的产生。
产品描述
LY 255283 is a specific antagonit of leukotriene B4 (LTB4) receptor. It inhibits the production of LTB(4) in human peripheral blood polymorphonuclear leukocytes (PMNL) and in monocytes activated by calcium ionophore A23187.
体内活性
All seven rats given only the vehicle died within 2 h of reperfusion, whereas rats treated with LY-255283 (3 or 10 mg/kg iv), a leukotriene B4 (LTB4) receptor antagonist given 10 min before reperfusion, exhibited significantly higher survival rates of 57% (4 out of 7) and 75% (6 out of 8), respectively, 2 h after reperfusion.?Rats given 1 mg/kg of LY-255283 showed no significant improvement in survival.?Splanchnic artery occlusion (SAO)-shock rats treated with LY-255283 (3 or 10 mg/kg) exhibited significantly attenuated accumulation of plasma free amino-nitrogenous compounds and of a myocardial depressant factor.?Treatment with LY-255283 (10 mg/kg) markedly (P less than 0.01) ameliorated the deficits of endothelium-dependent relaxation of isolated superior mesenteric artery (SMA) rings in untreated SAO-shock rats.?LY-255283 at 10 mg/kg significantly attenuated the increased myeloperoxidase activity in the intestinal tissue of SAO-shock rats[1].
Cas No.
117690-79-6
分子式
C19H28N4O3
分子量
360.45
别名
LY 255283
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years