Stilbamidine dihydrochloride

Stilbamidine dihydrochloride is a diamidine compound derived from Stilbene and used chiefly in the form of its crystalline isethionate salt in treating various fungal infections.

The high-affinity pentamidine transporter (HAPT1) is inhibited by Propamidine but displays only low affinity to Stilbamidine dihydrochloride. adenosine-sensitive pentamidine transporter (ASPT1), in contrast, is strongly inhibited by Stilbamidine dihydrochloride, and Propamidine. [³H]pentamidine uptake is determined in the presence of various concentrations of adenosine (IC₅₀=1.2 μM) or melarsen oxide (IC₅₀=0.7 μM), as well as in the presence of 250 μM adenosine and increasing concentrations of hypoxanthine, Propamidine (IC₅₀=6.1 μM) and Stilbamidine dihydrochloride (IC₅₀=110 μM)^[1]. The two diamidine compounds, Stilbamidine dihydrochloride 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^[2].

References:
[1]. De Koning HP. Uptake of pentamidine in Trypanosoma brucei brucei is mediated by three distinct transporters: implications for cross-resistance with arsenicals. Mol Pharmacol. 2001 Mar;59(3):586-92.
[2]. BREWER AE.et al. Multiple myeloma treated with stilbamidine and pentamidine. Br Med J. 1948 Dec 4;2(4587):978-82.