The Biotransformation of 8-Chloro-6-phenyl-4H-s-triazolo[4, 3-a][1,4] benzodiazepine (D-40TA), a New Central Depressant, in Man, Dog and Rat
- 1 January 1974
- journal article
- research article
- Published by Taylor & Francis in Xenobiotica
- Vol. 4 (7) , 441-456
- https://doi.org/10.3109/00498257409052107
Abstract
1. Metabolic studies of 8-chloro-6-phenyl-4H-s-triazolo [4,3-a] [1,4] benzodiazepine (D—40TA) in man, dog and rat led to identification of the following metabolites: six hydroxylation products; 8-chloro-2,4-dihydro-6-phenyl-1H-s-triazolo[4,3-a] [1,4]benzodiazepin-1-one (I), 8-chloro-6-(4-hydroxyphenyl)-4H-s -triazolo[4,3-a][1,4]benzodiazepine (II), 8-chloro-6- (3-hydroxyphenyl)-4H-s-triazolo[4,3-a] [1,4] benzodiazepine (III), 8-chloro-4-hydroxy-6-phenyl-4H-s- triazolo[4,3-a][1,4]benzodiazepine (IV), 8-chloro-2,4-dihydro-6- (4-hydroxy-phenyl)-1H-s-triazolo[4,3-a] [1,4] benzodiazepin-1-one (V) and 8-chloro-2,4-dihydro-6-(3-hydroxyphenyl)- 1H-s- triazolo[4,3-a][1,4]benzodiazepin-1-one (VI); five ring-opened metabolites; 5-chloro-2-(4H-1,2,4-triazol-4-yl) -benzophenone (VII), 5-chloro-2- (2,3-dihydro-3-oxo- 4H -1,2,4- triazol-4-yl)benzophenone (VIII), 5-chloro-2- (2,3-dihydro-3-oxo-4H - 1,2,4-triazol-4-yl)-2-hydroxybenzophenone (IX), 5-chloro-2- (2,3-dihydro-3-oxo-4H-1,2,4-triazol-4-yl)-4'-hydroxybenzophenone...Keywords
This publication has 13 references indexed in Scilit:
- Metabolism of 8-Chloro-6-phenyl-4H-s-triazolo[4,3-α][1,4]-benzodiazepine (D–40TA), a New Central Depressant. II. Species Difference in MetabolismXenobiotica, 1974
- Metabolism of 8-Chloro-6-phenyl-4H-s-triazolo[4,3-α][1,4]-benzodiazepine (D–40TA), a New Central Depressant. I. Absorption, Distribution and Excretion in RatsXenobiotica, 1974
- Heterocycles. VII. Novel and Facile Syntheses of s-Triazolo-[4, 3-a] [1, 4] benzodiazepine DerivativesCHEMICAL & PHARMACEUTICAL BULLETIN, 1973
- Metabolism of 6-Chloro-5-cyclohexylindane-1-carboxylic Acid (TAI-284), a New Non-steroidal Anti-inflammatory Agent. II. Isolation and Identification of Metabolites in the Perfusate of the Isolated Liver Perfusion in RatsXenobiotica, 1973
- PHARMACOLOGICAL STUDIES ON NEW POTENT CENTRAL DEPRESSANTS, 8-CHLORO-6-PHENYL-4H-s-TRIAZOLO [4, 3a] [1, 4] BENZODIAZEPINE (D-40TA) AND ITS 1-METHYL ANALOGUE (D-65MT)The Japanese Journal of Pharmacology, 1971
- STRUCTURE-ACTIVITY RELATIONSHIP OF s-TRIAZOLO 1, 4-BENZODIAZEPINES IN CENTRAL NERVOUS DEPRESSANT ACTIONThe Japanese Journal of Pharmacology, 1971
- Metabolism of14C-medazepam hydrochloride in dog, rat and manBiochemical Pharmacology, 1970
- Syntheses and structures of 7-chloro-2-hydrazino-5-phenyl-3H-1,4-benzodiazepines and some isomeric 1,4,5-benzotriazocinesTetrahedron Letters, 1970
- Chlordiazepoxide metabolites in the rat. Characterization by high resolution mass spectrometryBiochemical Pharmacology, 1968
- Diazepam metabolites in the rat: Characterization by high-resolution mass spectrometry and nuclear magnetic resonanceArchives of Biochemistry and Biophysics, 1967