氨甲吖啶类药物向细胞内的转运。

Transport of AMSA drugs into cells.

作者信息

Darkin S, Ralph R K

出版信息

FEBS Lett. 1985 Oct 14;190(2):349-53. doi: 10.1016/0014-5793(85)81317-x.

Abstract

The uptake and efflux of radioactive 4'-(9-acridinylamino)methanesulphon-m-anisidide (mAMSA) and its inactive congener 4'-(9-acridinylamino)methanesulphon-o-anisidide (oAMSA) by PY815 mastocytoma cells were investigated. Both drugs were readily taken up by intact cells although only mAMSA caused DNA scission and is actively cytotoxic to PY815 cells. The microsomal enzyme inhibitors cimetidine or SKF525A increased drug uptake and decreased drug efflux suggesting that drug metabolism could explain the different activities of oAMSA and mAMSA.

摘要

研究了PY815肥大细胞瘤细胞对放射性4'-(9-吖啶基氨基)甲磺基间茴香胺（mAMSA）及其无活性类似物4'-(9-吖啶基氨基)甲磺基邻茴香胺（oAMSA）的摄取和流出。两种药物都很容易被完整细胞摄取，尽管只有mAMSA会导致DNA断裂，并且对PY815细胞具有活性细胞毒性。微粒体酶抑制剂西咪替丁或SKF525A增加了药物摄取并减少了药物流出，这表明药物代谢可以解释oAMSA和mAMSA的不同活性。