[Biotransformation and pharmacokinetics of AWD 26-06, 8-chloro-5,10-dihydro-5-[bis(2-hydroxyethyl)aminoacetyl]-11H-dibenzo[d, c][1,4]diazepin-11-one hydrochloride in the rat].
After p.o. administration to rats AWD 26-06 (1) is rapidly but incompletely absorbed. The relatively short distribution (t1/2 alpha = 37 min) is followed by a middle-long elimination (t1/2 beta = 14 h). The volumen of distribution do not suggest an uncommon accumulation in deep compartments. About 70% of 1 were excreted unchanged with the feces. In urine and feces 18 metabolites were identified. The structure of 10 products could be elucidated. All metabolites have changed side-chains. Furthermore, the tricyclic molecule without side-chain and a N-methyl derivative were identified. The metabolites with so far unknown structure contain the unsubstituted tricyclic moiety too.
Pfeifer
S
S
Sektion Chemie, Humboldt-Universität zu Berlin.
Gedan
A
A
Franke
P
P
Klemm
W
W
Morgenroth
U
U
D000818:Animals; D001711:Biotransformation; D003984:Dibenzazepines / Q000378:metabolism* / Q000493:pharmacokinetics / Q000652:urine; D005243:Feces / Q000737:chemistry; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013056:Spectrophotometry, Ultraviolet
D003984:Dibenzazepines; C060713:AWD 26-06
Biotransformation und Pharmakokinetik von AWD 26-06, 8-Chlor-5,10-dihydro-5-[bis(2-hydroxyethyl)aminoacetyl]-11H- dibenzo[d,c][1,4]diazepin-11-on-hydrochlorid an der Ratte.