[Pharmacokinetics of 4-oxa-5-exo-(N-methylcarbamoyloxy)-tricyclo- [5.2.1.0. 2,6-endo] dec-8-en-3-one in the rat].
Pharmacokinetics of 4-Oxa-5-exo-(N-methylcarbamoyloxy)-tricyclo- [5.2.1.0. 2,6endo]dec-8-en-3one in the Rat The pharmacokinetics of 4-oxa-5-exo-(N-methylcarbamoyloxy)-tricyclo- [5.2.1.0. 2,6endo]dec-8-en-3one (Lu 253) were investigated after oral application in male Wistar rats. The compound is extensively absorbed and mainly renally eliminated. Within 60 h, 63% of the activity is recovered in urine and faeces. After 12 h 27% of the activity is eliminated (application in polyethylene glycol). The highest total concentration of the activity in the plasma is found after 2 h, the highest of the unchanged drug is found after 1 h. The half-life is 2.9 h. The concentration in plasma is mathematically characterized by the parameters of a two-compartiment model and also independent of a model. Lu 253 is distributed in the whole organism, a maximum of activity is achieved 2 h after application. By whole-body autoradiography the entrance of the compound into liquor and an enduring accumulation in the frontal cavity is detected.
Neidlein
R
R
Pharmazeutisch-Chemischen Institut, Universität Heidelberg.
Deigner
H P
HP
D000700:Analgesics / Q000378:metabolism / Q000493:pharmacokinetics*; D000818:Animals; D001345:Autoradiography; D001646:Bile / Q000378:metabolism; D002219:Carbamates / Q000378:metabolism / Q000493:pharmacokinetics*; D006863:Hydrogen-Ion Concentration; D008297:Male; D011485:Protein Binding; D051381:Rats; D011919:Rats, Inbred Strains; D014018:Tissue Distribution
D000700:Analgesics; D002219:Carbamates; C055810:LU 253
Pharmakokinetik von 4-Oxa-5-exo-(N-methylcarbamoyloxy)-tricyclo- [5.2.1.0. 2,6endo]dec-8-en-3on an der Ratte.