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目的 研究两种哒嗪酮衍生物即 :6 (α,α 二苯基乙酰哌嗪基苯基 ) 4,5 二氢 5 甲基 3 (2H) 哒嗪酮 (简称DMDP)和 6 (α 苯基乙酰哌嗪基苯基 ) 4,5 二氢 5 甲基 3 (2H) 哒嗪酮 (简称PMDP)及对照药物维拉帕米 (verapamil,Ver)对小鼠腹腔巨噬细胞体外释放肿瘤坏死因子 (tumornecrosisfactor ,TNF)的影响。方法 体外诱生TNF ,以L92 9细胞为靶细胞的细胞毒结晶紫染色法进行TNF的生物定量测定。结果 在 10 -6～ 10 -4 mol·L-1浓度范围内 ,DMDP的抑制作用呈剂量依赖性 ;浓度达 10 -4 mol·L-1时 ,可完全抑制TNF的释放。IC50 <10 -6mol·L-1。PMDP的抑制作用更强 :10 -8～ 10 -6mol·L-1时 ,该抑制作用呈剂量依赖性 ;10 -6mol·L-1时 ,即可完全抑制TNF的释放。IC50 <10 -8mol·L-1。结论 DMDP ,PMDP及Ver对小鼠腹腔巨噬细胞体外释放TNF具有显著的抑制作用。
OBJECTIVE To study the effect of two pyridazinone derivatives, namely, 6 (α, α diphenylacetylpiperazinophenyl) 4,5 dihydro 5 methyl 3 (2H) pyridazinone 4,5-dihydro-5-methyl-3 (2H) pyridazinone (abbreviated as PMDP) and verapamil (Ver) as control drug on peritoneal macrophages in vitro release of tumor necrosis Effect of tumor necrosis factor (TNF). Methods Tumor necrosis factor (TNF) was induced in vitro. The biological quantitative determination of TNF was performed by cytotoxic violet staining of L92 9 cells. Results The inhibitory effect of DMDP in a concentration range of 10 -6 ~ 10 -4 mol·L -1 was dose-dependent. When the concentration was 10 -4 mol·L -1, the release of TNF was completely inhibited. IC50 <10 -6 mol·L-1. The inhibitory effect of PMDP was stronger: 10 -8 ~ 10 -6 mol·L-1, the dose-dependent inhibition; 10 -6 mol·L-1, can completely inhibit the release of TNF. IC50 <10 -8 mol·L-1. Conclusion DMDP, PMDP and Ver have a significant inhibitory effect on the in vitro release of TNF by mouse peritoneal macrophages.