Disposition and metabolism of radiolabelled pentachloroanisole in rats and rabbits.
Male Sprague-Dawley rats and New Zealand White rabbits were administered 14C-labelled pentachloroanisole (PCA) in corn oil by gavage as single doses of 25 mg/kg and were then placed in individual metabolism cages for as long as 4 days. Peak blood level of radioactivity occurred 6 hr after administration of the dose to rats and between 3 and 4 hr in rabbits; the blood elimination half-life ranged from 8 to 15 hr in rats and averaged 6 hr in rabbits. Rats excreted an average of 54.2% of the administered radiolabel in the urine and 32.4% in the faeces during the 96 hr following the dose; rabbits excreted an average of 84.2 and 13.1% of the radiolabel in the urine and faeces, respectively, during this time. Examination of the metabolites in the rat showed that 60% of the urinary radioactivity was attributable to tetrachlorohydroquinone (TCH), 3% to free pentachlorophenol (PCP) and 29% to conjugated PCP; faecal metabolites were PCP (85.7%), TCH (4.3%) and polar metabolite(s) (10%). In the rabbit, 58% of the urinary radioactivity was attributable to TCH, 8% to free PCP and 34% to conjugated PCP. Faecal metabolites consisted of PCP and conjugated material.
Ikeda
G J
GJ
Pharmacokinetics and Metabolism Branch, Food and Drug Administration, Laurel, MD 20708.
Sapienza
P P
PP
Warr
P I
PI
D000284:Administration, Oral; D000818:Animals; D000840:Anisoles / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002250:Carbon Radioisotopes; D002855:Chromatography, Thin Layer; D005243:Feces / Q000737:chemistry; D006207:Half-Life; D006873:Hydroquinones / Q000032:analysis / Q000652:urine; D007553:Isotope Labeling; D008297:Male; D010416:Pentachlorophenol / Q000032:analysis / Q000652:urine; D011817:Rabbits; D011865:Radioisotope Dilution Technique; D051381:Rats; D017207:Rats, Sprague-Dawley; D012588:Scintillation Counting; D014018:Tissue Distribution
D000840:Anisoles; D002250:Carbon Radioisotopes; D006873:Hydroquinones; C015421:pentachloroanisole; C044578:2,3,5,6-tetrachlorohydroquinone; D010416:Pentachlorophenol