In this article, we will discuss Amsacrine (Experimental Notes-4). So, let’s get started.
A number of reports have described the metabolism of amsacrine in rats and mice.
In mouse bile, 5′- and 6′-glutathione conjugates were present in roughly equal amounts and accounted for 70% of the excreted biliary radiolabel after administration of radio-labelled amsacrine (Robertson et al., 1988). In rats, the principal biliary metabolite was
the 5′-glutathione conjugate, which accounted for 80% of the excreted radiolabel within the first 90 min and > 50% of the administered dose over 3 h (Shoemaker et al., 1982). The 6′-conjugate was also subsequently identified in rat bile (Robertson et al., 1993). In rat liver microsomes and human neutrophils, intermediate oxidation products have
been identified as N1′-methanesulfonyl-N4′-(9-acridinyl)-3′-methoxy-2′,5′-cyclohexadiene-1′,4′-diimine and 3′-methoxy-4′-(9-acridinylamino-2′,5′-cyclohexadien-1′-one (Shoemaker et al., 1984; Kettle et al., 1992).