摘要
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 investigate the effects of two kinds of pyridazinone derivatives:6 (α,α diphenylacetylpiperazinyl)phenyl 5 methyl 4,5 dihydro 3 (2H) pyridazinone(PMDP) and 6 (α phenylacetylpiperaziny) phenyl 5 methyl 4,5 dihydro 3(2H) pyridazinone (PMDP) on tumor necrosis factor(TNF) release from mouse peritoneal macrophages.METHODS In vitro cell cytotoxic assays were used for tumor necrosis factor.RESULTS It was found that DMDP and PMDP significantly inhibited TNF release from mouse peritoneal macrophages.At the concentration from 10 -6 ～10 -4 mol·L -1 ,the inhibitory effects were presented by DMDP in a dose dependent manner.TNF release was entirely inhibited by DMDP at 10 -4 mol·L -1 .At the concentration from 10 -8 ～10 -6 mol·L -1 ,the inhibitory effects were presented by PMDP in a dose dependent manner,TNF release was entirely inhibited by PMDP at 10 -6 mol·L -1 .CONCLUSION DMDP and PMDP inhibited TNF release from mouse peritoneal macrophages.The two drugs may have effects on the prevention and treatment of cardio cerebrovascular disorders.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2001年第2期95-97,共3页
Chinese Pharmaceutical Journal
