CAS: 60902-27-4

Phenacetin-d3 is a radioactive isotope of phenacetin that has been used to study drug metabolism. It is reconstituted with a deuterium atom at the 3 position. Phenacetin-d3 binds to the membrane transporter protein, P-glycoprotein, and it does not bind to other transporters such as MRP1 and BCRP. The binding of phenacetin-d3 to P-glycoprotein alters the activity of the transporter in a manner that is dependent on the concentration of drugs in plasma. This effect has been shown using both chemical ionization mass spectrometry and liquid chromatography tandem mass spectrometry techniques with plasma samples from patients who are taking statins.

Applications Phenacetin-d3 is the labeled analogue of Phenacetin (P294580), an analgesic, antipyretic; component of APC tablets, analgesic mixture also containing aspirin and caffeine. Phenacetin is reasonably anticipated to be a human carcinogen; analgesic mixtures containing Phenacetin are listed as known human carcinogens. References Boyd, et al.: Toxicol. Appl. Pharmacol., 1, 240 (1959); Dubach, C.U., et al.: N. Engl. J. Med., 308, 357 (1983)