Detail of "34031-32-8"

Reference

Intestinal uptake and metabolism of auranofin, a new oral gold-based antiarthritis drug

Intestinal uptake and metabolism of auranofin, a new oral gold-based antiarthritis drug. Tepperman, Katherine; Finer, Richard; Donovan, Stuart; Elder, R. C.; Doi, J.; Ratliff, David; Ng, Kin (Dep. Biol. Sci., Univ. Cincinnati, Cincinnati, OH 45221, USA). Science (Washington, D. C., 1883-), 225(4660), 430-2 (English) 1984. CODEN: SCIEAS. ISSN: 0036-8075. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Auranofin (I) [34031-32-8], an exptl. antiarthritis pharmaceutical, was metabolized in contact with hamster or rat gut wall to yield the deacetylated form of the drug. This product, 1-thio-b-D-glucopyranosato-S-(triethylphosphine)gold(I) [34031-29-3], passed through hamster or rat intestinal wall in an everted gut expt. The metabolite was sepd. by high-performance liq. chromatog. and characterized by retention time, chem. reactivity to yield a known product, and comparison to a synthetic sample of the metabolite.

Triethylphosphine gold: cellular uptake and disposition after single and repeated oral doses in rats

Triethylphosphine gold: cellular uptake and disposition after single and repeated oral doses in rats. Sharma, R. P.; Smillie, J.; Laverty, R. (Dep. Med., Wellcome Med. Res. Inst., Dunedin, N. Z.). J. Pharm. Pharmacol., 36(7), 441-5 (English) 1984. CODEN: JPPMAB. ISSN: 0022-3573. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The tissue and subcellular pharmacokinetics of gold following single and repeated oral doses of triethylphosphine gold (auranofin) [34031-32-8] has been studied in rats. After a single dose, the tissue and subcellular gold levels were 5-10 times lower than those reached with injectable gold compds. In the liver tissues, gold concns. peaked within 24 h followed by a biphasic clearance, with an initial rapid phase (t1/2 32 h) and a slow terminal phase (t1/2 11 days). Renal gold concns. continued to increase for 3 to 5 days and then decreased exponentially with a first order t1/2 of about 7 days. Intracellularly, between 60-80% of hepatic and 50-70% of renal gold was present in the cytosol. In rats given repeated doses of auranofin, the hepatic and renal gold concns. were 3-5 times higher than those measured after a single dose. The proportion of cellular gold present in the cytosol was markedly lower, with 43% in the liver and 30% in kidney tissues. In both the liver and kidney, gold concns. were dose-dependent, whereas in the gastrointestinal tissues, the increases as a function of dose were minimal.