一种潜在的白三烯B4拮抗剂SM-9064的药理学特征

Pharmacological profiles of a potential LTB4-antagonist, SM-9064.

作者信息

Namiki M, Igarashi Y, Sakamoto K, Nakamura T, Koga Y

出版信息

Biochem Biophys Res Commun. 1986 Jul 31;138(2):540-6. doi: 10.1016/s0006-291x(86)80530-7.

Abstract

Antagonistic activity against leukotriene B4 (LTB4) and other pharmacological activities of SM-9064 were studied in vitro and in vivo. It inhibited the chemotaxis of rat polymorphonuclear leukocytes (PMNLs) induced by LTB4 (IC50 = 1.3 X 10(-7) M, not by other chemoattractants. Its agonistic activity was much less than that of LTB4. It suppressed the Arthus reaction-induced inflammation in mice with the dose of 5 mg/kg, i.p. or 10 mg/kg, p.o. These results suggest that SM-9064 is a candidate of LTB4 antagonists, which is effective in some type of inflammation.

摘要

在体外和体内研究了SM - 9064对白三烯B4（LTB4）的拮抗活性及其他药理活性。它抑制LTB4诱导的大鼠多形核白细胞（PMNLs）的趋化作用（IC50 = 1.3×10⁻⁷ M），而对其他趋化因子无此作用。其激动活性远低于LTB4。以5 mg/kg腹腔注射或10 mg/kg口服剂量可抑制小鼠的阿瑟斯反应诱导的炎症。这些结果表明，SM - 9064是LTB4拮抗剂的候选药物，对某些类型的炎症有效。