体外研究
The high-affinity pentamidine transporter (HAPT1) is inhibited by Propamidine but displays only low affinity to Stilbamidine. adenosine-sensitive pentamidine transporter (ASPT1), in contrast, is strongly inhibited by Stilbamidine, and Propamidine. [
3
H]pentamidine uptake is determined in the presence of various concentrations of adenosine (IC
50
=1.2 μM) or melarsen oxide (IC
50
=0.7 μM), as well as in the presence of 250 μM adenosine and increasing concentrations of hypoxanthine, Propamidine (IC
50
=6.1 μM) and Stilbamidine (IC
50
=110 μM). The two diamidine compounds, Stilbamidine and Pentamidine are used to treat in multiple myeloma, a disease in which increase of the globulin content of the serum is of frequent occurrence.
编辑结构
