Amelubant (BIIL 284) (BIIL 284) 是一种有效的口服长效 LTB4 受体拮抗剂，与 LTB4 受体的结合可忽略不计，在活细胞和细胞膜中的 Kis 分别为 221 nM 和 230 nM。
Amelubant (BIIL 284) is a potent, oral and long acting LTB4 receptor antagonist, negligibly binds to LTB4 receptor, with Kis of 221 nM and 230 nM in vital cells and membranes. Amelubant (BIIL 284) is a prodrug of active metabolites BIIL 260 and BIIL 315. Anti-inflammatory activity[1].
Amelubant is a prodrug of active metabolites BIIL 260 and BIIL 315, which are reversible and competitive LTB4 receptor antagonists, with Kis of 1.4, 1.1 nM and 1.7, 1.9 nM in vital cells and membranes, respectively[1].
[1]. Birke FW, et al. In vitro and in vivo pharmacological characterization of BIIL 284, a novel and potent leukotriene B(4) receptor antagonist. J Pharmacol Exp Ther. 2001 Apr;297(1):458-66.
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