国产氯苯扎利的药效学研究

Studies on pharmacodynamics of domestic Lobenzarit

氯苯扎利（Ｌｏｂ，２５，５０与１００ｍｇ·ｋｇ－１）对大鼠角叉菜胶足肿胀、棉球内芽肿均无明显抑制作用。而Ｌｏｂ三种剂量与二种给药方案对佐剂性关节炎（ＡＡ）大鼠的多发性关节肿胀均有明显的防治作用，并能使ＡＡ大鼠低下的脾细胞ＣｏｎＡ增殖反应恢复正常，还能使ＡＡ大鼠腹腔巨噬细胞（ＰＭΦ）升高的ＩＬ－１水平降低。在环磷酰胺（Ｃｙ）诱导溶血素抗体生成低下或增高的小鼠模型上，Ｌｏｂ均呈现反向调节作用。Ｌｏｂ（０．００１～１００μｍｏｌ·Ｌ－１）对正常小鼠脾细胞的ＣｏｎＡ增殖反应具有低浓度促进和高浓度抑制的双向调节作用。

The pharmacodynamics of domestic lobenzarit(Lob)were.studied.The results showed that Lob(25,50and 100mg·kg-1ig)had no inhibitory effect on carrageenan eodema,cotton pellet granulomatosis in rats.Using the protocol of admininistration(+3～+12d)or(+12～+22d),Lob(25,50 and 100 mg·kg-1ig)had prophylactic or therapeutic activity during the poly-arthritis symptoms in rats with adjuvant arthritis(AA).It was also showed that not only the lower ConA-induced responses of splenocytes were restored to normal,but also the elevated IL-1 reseased from peritoneal macrophages(PMΦ)were reduced in AA rats treated with Lob.Both cyclophamide(Cy)induced diminished ad enhanced mice for hemolysin responses,Lob(25,50 and 100 mg·kg-1ig)had recovery activity.It was found that ConA-induced responses of splenocytes were enhanced by in vitro treatment with Lob(0.001～0.1μmol·L-1),but diminished by Lob(0.1～100μmol·L-1)in mice.These results suggest that domestic Lob could possess condition-depedent and dose-dependent manner of immunomodulation,which might be one of the mechanisms of its antiarthric effect.