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Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 1978 Dec; Vol. 21 (12), pp. 1290-4. - Publication Year :
- 1978
-
Abstract
- A simple, one-step chemical oxidation of triazolam (7) to its 4-hydroxy analogue, 7a, has been developed and applied to other triazolo- and imidazobenzodiazepines. The reaction may be used to convert diazepam to temazepam. 4-Hydroxytriazolo[4,3-a][1,4]benzodiazepines have low central nervous system sedative and anticonvulsant activity in sharp contrast to metabolites of diazepam which remain active. While 10, an alpha-hydroxy metabolite of triazolam, retains much of the activity of 7, 10a, and alpha,4-dihydroxy metabolite of triazolam, is 250 times less potent than 7 on the nicotine-antagonism assay and over 300 times less potent on the traction assay.
- Subjects :
- Animals
Anticonvulsants chemical synthesis
Benzodiazepines pharmacology
Diazepam chemical synthesis
Diazepam pharmacology
Hydroxylation
Male
Methods
Mice
Oxidation-Reduction
Triazolam analogs & derivatives
Triazolam pharmacology
Triazoles chemical synthesis
Triazoles pharmacology
Anti-Anxiety Agents chemical synthesis
Benzodiazepines chemical synthesis
Diazepam analogs & derivatives
Triazolam chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0022-2623
- Volume :
- 21
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 31483
- Full Text :
- https://doi.org/10.1021/jm00210a022