Shin J S, Lee J J, Kim Y, Lee C K, Yun Y P, Lee M K
College of Pharmacy, Chungbhuk National University, Cheongju, Republic of Korea.
Biol Pharm Bull. 2001 Jan;24(1):103-5. doi: 10.1248/bpb.24.103.
The inhibitory effects of ethaverine on dopamine content in PC12 cells were investigated. Ethaverine decreased dopamine content in a concentration-dependent manner in PC12 cells and showed 33.6% inhibition of dopamine content at a concentration of 1.0 microM for 24-48 h. The IC50 value of ethaverine was 1.4 microM. Dopamine content was lowered at 6h and reached a minimal level at 12h after exposure to ethaverine at 2.0 microM. The decreased dopamine level was maintained up to 48 h and then recovered to the control level at about 72 h. Tyrosine hydroxylase (TH) was inhibited at 6 h following treatment with ethaverine in PC12 cells and the activity was maintained at a reduced level up to 36 h (12-22% inhibition at 2.0 microM). These results indicate that ethaverine leads to a decrease in dopamine content by inhibition of TH activity.
研究了依他维林对PC12细胞中多巴胺含量的抑制作用。依他维林在PC12细胞中以浓度依赖性方式降低多巴胺含量，在1.0微摩尔浓度下作用24 - 48小时，对多巴胺含量的抑制率为33.6%。依他维林的IC50值为1.4微摩尔。在暴露于2.0微摩尔依他维林后，多巴胺含量在6小时降低，12小时达到最低水平。多巴胺水平降低持续至48小时，然后在约72小时恢复到对照水平。在PC12细胞中用依他维林处理6小时后酪氨酸羟化酶（TH）受到抑制，其活性在长达36小时内维持在降低水平（在2.0微摩尔时抑制12 - 22%）。这些结果表明依他维林通过抑制TH活性导致多巴胺含量降低。
