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Brotizolam

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ACTIVE PHARMA INGREDIENTS

5 API Suppliers, 1 CEP/COS, 3 JDMF, 1 EU WC, 3 Listed Suppliers, $ API Reference Price

5 API Suppliers
1 CEP/COS
3 JDMF
1 EU WC
3 Listed Suppliers
$ API Reference Price

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3 FDF Dossiers, 2 Europe, 1 South Africa

3 FDF Dossiers
2 Europe
1 South Africa

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2 Finished Drug Prices

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Synopsis

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Chemistry

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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

Brotizolam

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 Formula	C₁₅H₁₀BrClN₄S
Molecular Weight	393.7 g/mol
XLogP3	2.8
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	1
Exact Mass	391.94981 g/mol
Monoisotopic Mass	391.94981 g/mol
Topological Polar Surface Area	71.3 Å²
Heavy Atom Count	22
Formal Charge	0
Complexity	465
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

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.

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