Brotizolam

CAS No:
57801-81-7 Category:
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Product Details:

  • CAS No: 57801-81-7
  • AHFC code:
  • Synonyms: 2-Bromo-4-(2-chlorophenyl)-9-methyl-6H-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepine, 2-Bromo-4-(o-chlorophenyl)-9-methyl-6H-thieno(3,2-f)-s-triazolo(4,3-a)(1,4)diazepine, 6H-Thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepine, 2-bromo-4-(2-chlorophenyl)-9-methyl-, 8-Bromo-6-(o-chlorophenyl)-1-methyl-4H-s-triazolo(3,4c)thieno(2,3e)-1,4-diazepine, BRN 0839277, Brotizolam, Brotizolamum, Brotizolamum [INN-Latin], EINECS 260-964-5, Lendorm, Lendormin, UNII-5XZM1R3DKF, WE 941
  • ATC Code: N05CD09
  • Chemical Formula: C15H10N4
  • Molecular Weight: 393.7
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB09017
  • SMILES: Cc1nnc2n1-c3c(cc(s3)Br)C(=NC2)c4ccccc4Cl
  • InChl: 1S/C15H10BrClN4S/c1-8-19-20-13-7-18-14(9-4-2-3-5-11(9)17)10-6-12(16)22-15(10)21(8)13/h2-6H,7H2,1H3
  • PubChem: 2451
  • IUPAC: 2-Bromo- 4-(2-chlorphenyl)- 9-methyl- 6H-thieno (3,2-f)(1,2,4) triazolo (4,3-a)(1,4)benzodiazepine

Additional Details

Indication:
Brotizolam is indicated for the short-term treatment (2-4 weeks) of severe or debilitating insomnia.
Pharmacodynamics:
Mode of Action:
Metabolism:
There are two primary metabolites: 1-methyl-hydroxy- and the 4-hydroxy-derivatives (Eberts et al., 1981; Boehringer Ingelheim, product information). The 4-hydroxymetabolites have a pharmacological activity which is far less than that of the parent drugs, but the 1-methyl-hydroxymetabolites probably have comparable activity (Gall et al., 1978; Jochemsen et al., 1982; Sethy & Harris, 1982; Jochemsen et al., unpublished results). These active compounds are, however, not present in plasma in measurable amounts following a single dose of brotizolam to young healthy subjects (Jochemsen et al., 1982; Jochemsen et al., unpublished results).
Toxicity:
General Reference:
Jochemsen R, Wesselman JG, van Boxtel CJ, Hermans J, Breimer DD: Comparative pharmacokinetics of brotizolam and triazolam in healthy subjects. Br J Clin Pharmacol. 1983;16 Suppl 2:291S-297S. Pubmed
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