TABLE 1

Comparison of the biliary excretion of benzoic substituted isomers7to9and their fully aliphatic counterparts,6bto6d Based on observations in this paper and in McDonagh and Lightner (2007). Rapid biliary excretion means >60% of the injected dose excreted in <2 h with peak excretion <20 min after injection.


Compound

Rapid Biliary Excretion

Gunn (–UGT1)
Normal (+UGT1)
TR (–Mrp2)
Embedded Image No Yes, as acyl glucuronides No
Embedded Image No No No
Embedded Image No Yes, as acyl glucuronides No
Embedded Image Yes Yes Yes
Embedded Image Yes Yes, unchanged and as acyl glucuronides No
Embedded Image
Yes
Yes
No