Renal transport and disposition of Na‐2‐mercaptoethane sulfonate disulfide (Dimesna) in the rat

FEBS Letters

Uehara, N.¹  Ormstad, K.¹ 

[1] Department of Forensic Medicine, Karolinska Institutet, PO Box 60400, S-104 01 Stockholm, Sweden

关键词: Kidney;    Mercaptoethane sulfonate;    Glutathione;    Transport;   

DOI  :  10.1016/0014-5793(82)80767-9

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

The transport and reduction of dimesna (NA-2-mercaptoethane sulfonate disulfide) was studied in vitro using isolated, perfused rat kidney, and isolated renal epithelial cells. Cellular uptake of dimesna was found to be dependent on an active transport mechanism working across the luminal brush border, with an app. K _m of ∼22 μM and V _max ∼1.4 nmol. 10⁶ cells⁻¹.min⁻¹. Among other low molecular thiols or disulfides reduced glutathione was the only one to exert competitive inhibition. γ-GT-activity or cellular GSH status had no influence on renal uptake of dimesna, but the intracellular reduction rate was dependent on access to reduced glutathione as a cofactor.

【 授权许可】

Unknown