产品描述:
MK-571 is a cysteinyl leukotriene 1 (CysLT1) receptor antagonist (Ki = 2.1 nM in a radioligand binding assay using isolated human lung membranes).{1501} It inhibits contractions induced by leukotriene D4 (LTD4; Item No. 20310) or LTE4 (Item No. 20410) in histamine-primed isolated guinea pig trachea (pA2s = 9.4 and 9.1, respectively), but does not inhibit contractions induced by LTC4 (Item No. 20210) in histamine-primed isolated guinea pig trachea when used at a concentration of 190 nM. MK-571 (100 nM) inhibits LTD4-induced calcium mobilization in COS-7 monkey kidney cells expressing the human CysLT1 receptor in a reporter assay.{7174} MK-571 (5 mg/kg) improves tissue damping and elasticity, markers of lung function, and decreases IL-4 and IL-5 levels in bronchoalveolar lavage fluid (BALF) in a mouse model of ovalbumin-induced asthma.{64814}