tert-Butylbicycloortho[3H]benzoate (3H-TBOB) toxicokinetics and disposition in rats.
1. Toxicokinetics of tert-butylbicycloortho[3H]benzoate (3H-TBOB) administered into the right atrium of rat heart can be described by the biexponential equation: ct = Ae-1.6t + Be-0.013t. 2. The fast initial phase of 3H-TBOB decline in blood (t1/2 = 0.5 min) is due to its absorption by lungs. 3H-TBOB is then transferred into liver, the primary organ of its metabolic detoxication. The high apparent distribution volumes for 3H-TBOB (1.3 and 7.1 l/kg for the initial and the terminal phase, respectively) are probably due to its lipophilicity and partitioning into lipoid tissue membranes. 3. Acid-labile TBOB is not completely hydrolysed in gastric fluid. A portion of 3H-TBOB administered into the stomach is absorbed within 3 min into the circulatory system. 4. Intra-arterially administered 3H-TBOB distributes in the brain in a lateral and regional pattern. 5. Two types of 3H-TBOB metabolites are excreted in urine and faeces. Both are more polar than the parent compound. The major components of the fraction were tentatively identified as hippuric and benzoic acid.
Zierer
R
R
Department of Agricultural Biochemistry, University of Hawaii, Honolulu 96822.
Seifert
J
J
D000818:Animals; D001711:Biotransformation; D001921:Brain / Q000378:metabolism; D001643:Bridged Bicyclo Compounds / Q000493:pharmacokinetics / Q000633:toxicity*; D019086:Bridged Bicyclo Compounds, Heterocyclic; D005243:Feces / Q000737:chemistry; D007269:Injections, Intra-Arterial; D007275:Injections, Intravenous; D007441:Intubation, Gastrointestinal; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D014018:Tissue Distribution
D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; C046308:tert-butylbicyclo-2-benzoate