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    Brotizolam

    ACTIVE PHARMA INGREDIENTS

    FINISHED DOSAGE FORMULATIONS

    GLOBAL SALES INFORMATION

    REF. STANDARDS & IMPURITIES

    PharmaCompass
    $ API Ref.Price (USD/KG) : 23,609Xls

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    2D Structure
    Also known as: Lendormin, Lendorm, 57801-81-7, Mederantil, Sintonal, We 941
    Molecular Formula
    C15H10BrClN4S
    Molecular Weight
    393.7  g/mol
    InChI Key
    UMSGKTJDUHERQW-UHFFFAOYSA-N
    FDA UNII
    5XZM1R3DKF
    Brotizolam is a triazolo-benzodiazepine derivative with sedative, hypnotic, anxiolytic and anticonvulsant activities. Brotizolam binds to the benzodiazepine binding site on the gamma aminobutyric acid (GABA)-A receptor in the central nervous system (CNS). This leads to an increase in the opening of chloride channels, membrane hyperpolarization and increases the inhibitory effect of GABA on the CNS.
    1 2D Structure

    2D Structure

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    4-bromo-7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaene
    2.1.2 InChI
    InChI=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
    2.1.3 InChI Key
    UMSGKTJDUHERQW-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    CC1=NN=C2N1C3=C(C=C(S3)Br)C(=NC2)C4=CC=CC=C4Cl
    2.2 Other Identifiers
    2.2.1 UNII
    5XZM1R3DKF
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. Lendorm

    2. Lendormin

    3. Lindormin

    4. Sintonal

    5. We 941

    2.3.2 Depositor-Supplied Synonyms

    1. Lendormin

    2. Lendorm

    3. 57801-81-7

    4. Mederantil

    5. Sintonal

    6. We 941

    7. Nimbisan

    8. 2-bromo-4-(2-chlorophenyl)-9-methyl-6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine

    9. We-941

    10. 5xzm1r3dkf

    11. Chembl32479

    12. 2-bromo-4-(2-chlorophenyl)-9-methyl-6h-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepine

    13. We-941-bs

    14. 2-bromo-4-(o-chlorophenyl)-9-methyl-6h-thieno(3,2-f)-s-triazolo(4,3-a)(1,4)diazepine

    15. Ncgc00183872-01

    16. 6h-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepine, 2-bromo-4-(2-chlorophenyl)-9-methyl-

    17. 6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine, 2-bromo-4-(2-chlorophenyl)-9-methyl-

    18. Brotizolamum

    19. Brotizolamum [inn-latin]

    20. Einecs 260-964-5

    21. Unii-5xzm1r3dkf

    22. Brn 0839277

    23. Lendormine

    24. Indormyl

    25. Ladormin

    26. Brotizolam [usan:inn:ban:jan]

    27. Lendormin (tn)

    28. 2-bromo-4-(2-chlorophenyl)-9-methyl-6h-thieno-[3,2-f][1,2,4]-triazolo[4,3-a][1,4]diazepine

    29. Brotizolam [mi]

    30. Brotizolam [inn]

    31. Brotizolam [jan]

    32. Brotizolam [usan]

    33. Dsstox_cid_2692

    34. Brotizolam [mart.]

    35. 8-bromo-6-(o-chlorophenyl)-1-methyl-4h-s-triazolo(3,4c)thieno(2,3e)-1,4-diazepine

    36. Brotizolam [who-dd]

    37. Dsstox_rid_76694

    38. Dsstox_gsid_22692

    39. Schembl44067

    40. Brotizolam (jp17/usan/inn)

    41. Dtxsid0022692

    42. Chebi:31308

    43. We 941-bs

    44. Brotizolam [ep Monograph]

    45. Brotizolam 0.1 Mg/ml In Methanol

    46. Brotizolam 1.0 Mg/ml In Methanol

    47. Zinc2570830

    48. Tox21_113601

    49. Bdbm50011875

    50. Akos016014338

    51. Db09017

    52. Cas-57801-81-7

    53. Db-053108

    54. D01744

    55. L000775

    56. Q850074

    57. 4-n-pentylphenyl-4-trans-n-propylcyclohexylcarboxylate

    58. 2-bromo-4-(2-chloro-phenyl)-9-methyl-6h-1-thia-5,7,8,9a-tetraaza-cyclopenta[e]azulene

    59. 2-bromo-4-(o-chlorophenyl)-9-methyl-6h-thieno[3,2-f]-s-triazolo[4,3-a]-[1,4]diazepine

    60. 2-bromo-4-(2-chlorophenyl)-9-methyl-6h-thieno(3,2-f)-s-triazolo(4,3-a)(1,4)diazepine

    61. 4-bromo-7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaene

    62. 8-bromo-6-(o-chlorophenyl)-1-methyl-4h-s-triazolo(3,4-c)thieno(2,3-e)-1,4-diazepine

    2.4 Create Date
    2005-03-25
    3 Chemical and Physical Properties
    Molecular Weight 393.7 g/mol
    Molecular Formula C15H10BrClN4S
    XLogP32.8
    Hydrogen Bond Donor Count0
    Hydrogen Bond Acceptor Count4
    Rotatable Bond Count1
    Exact Mass391.94981 g/mol
    Monoisotopic Mass391.94981 g/mol
    Topological Polar Surface Area71.3 Ų
    Heavy Atom Count22
    Formal Charge0
    Complexity465
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Indication

    Brotizolam is indicated for 2-4 weeks in the treatment of severe or debilitating insomnia.

    5 Pharmacology and Biochemistry
    5.1 MeSH Pharmacological Classification

    Hypnotics and Sedatives

    Drugs used to induce drowsiness or sleep or to reduce psychological excitement or anxiety. (See all compounds classified as Hypnotics and Sedatives.)

    5.2 ATC Code

    N05CD09

    S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355

    N - Nervous system

    N05 - Psycholeptics

    N05C - Hypnotics and sedatives

    N05CD - Benzodiazepine derivatives

    N05CD09 - Brotizolam

    5.3 Absorption, Distribution and Excretion

    Absorption

    The plasma concentration profile of brotizolam can be described as a one compartmental open model with first-order absorption.

    Volume of Distribution

    0.63 l/kg.

    Clearance

    Total clearance: 109 ml/min.

    5.4 Metabolism/Metabolites

    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).

    Brotizolam has known human metabolites that include 6-hydroxy-BRT and alpha-hydroxy-BRT.

    S73 | METXBIODB | Metabolite Reaction Database from BioTransformer | DOI:10.5281/zenodo.4056560

    5.5 Biological Half-Life

    4.4 hours.