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Clotiazepam

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ACTIVE PHARMA INGREDIENTS

2 API Suppliers, 1 EU WC, 2 Listed Suppliers, $ API Reference Price

2 API Suppliers
1 EU WC
2 Listed Suppliers
$ API Reference Price

FINISHED DOSAGE FORMULATIONS

6 FDF Dossiers, 6 Europe

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6 Europe

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6 Finished Drug Prices

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6 Finished Drug Prices

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Synopsis

ACTIVE PHARMA INGREDIENTS

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API REF. PRICE (USD/KG)

$ 3,369

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Chemistry

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Also known as: Rize, Trecalmo, Rizen, Tienor, Rise, 33671-46-4

Molecular Formula

C₁₆H₁₅ClN₂OS

Molecular Weight

318.8 g/mol

InChI Key

CHBRHODLKOZEPZ-UHFFFAOYSA-N

FDA UNII

ZCN055599V

Clotiazepam is a thienodiazepine, not approved for sale in the U.S. or Canada, but has been approved in the U.K. It is a schedule IV drug in Canada.

1 2D Structure

Clotiazepam

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

5-(2-chlorophenyl)-7-ethyl-1-methyl-3H-thieno[2,3-e][1,4]diazepin-2-one

2.1.2 InChI

InChI=1S/C16H15ClN2OS/c1-3-10-8-12-15(11-6-4-5-7-13(11)17)18-9-14(20)19(2)16(12)21-10/h4-8H,3,9H2,1-2H3

2.1.3 InChI Key

CHBRHODLKOZEPZ-UHFFFAOYSA-N

2.1.4 Canonical SMILES

CCC1=CC2=C(S1)N(C(=O)CN=C2C3=CC=CC=C3Cl)C

2.2 Other Identifiers

2.2.1 UNII

ZCN055599V

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Y 6047

2. Y-6047

3. Y6047

2.3.2 Depositor-Supplied Synonyms

1. Rize

2. Trecalmo

3. Rizen

4. Tienor

5. Rise

6. 33671-46-4

7. Clotiazepamum [inn-latin]

8. Y 6047

9. 5-(2-chlorophenyl)-7-ethyl-1-methyl-3h-thieno[2,3-e][1,4]diazepin-2-one

10. 5-(o-chlorophenyl)-7-ethyl-1,3-dihydro-1-methyl-2h-thieno(2,3-e)-1,4-diazepin-2-one

11. 5-(2-chlorophenyl)-7-ethyl-1-methyl-1,3-dihydro-2h-thieno(2,3-e)(1,4)diazepin-2-one

12. Zcn055599v

13. 2h-thieno(2,3e)(1,4)-diazepin-2-one, 5-(o-chlorophenyl)-7-ethyl-1,3-dihydro-1-methyl-

14. 5-(2-chlorophenyl)-7-ethyl-1-methyl-1,3-dihydro-2h-thieno[2,3-e][1,4]diazepin-2-one

15. Clotiazepamum

16. Distensan

17. Veratran

18. Clozan

19. Clotiazepam [inn:jan]

20. 2h-thieno(2,3-e)(1,4)diazepin-2-one, 1,3-dihydro-5-(o-chlorophenyl)-7-ethyl-1-methyl-

21. 2h-thieno[2,3-e]-1,4-diazepin-2-one, 5-(2-chlorophenyl)-7-ethyl-1,3-dihydro-1-methyl-

22. Rize (tn)

23. Einecs 251-627-3

24. Brn 0623332

25. Unii-zcn055599v

26. Dea No. 2752

27. Y-6047

28. Clotiazepam [mi]

29. Clotiazepam [inn]

30. Clotiazepam [jan]

31. Clotiazepam (jp17/inn)

32. Clotiazepam [mart.]

33. Schembl44592

34. Clotiazepam [who-dd]

35. Zinc1207

36. Chembl1697737

37. Dtxsid0022852

38. Chebi:31425

39. Hy-u00317

40. Akos005065735

41. Cs-7319

42. Db01559

43. D01328

44. Q2263999

45. 2h-thieno[2,3-e]-1,4-diazepine-2-one, 5-(2-chlorophenyl)-7-ethyl-1,3-dihydro-1-methyl-

46. 5-(2-chlorophenyl)-7-ethyl-1-methyl-1h,2h,3h-thieno[2,3-e][1,4]diazepin-2-one

2.4 Create Date

2005-03-25

3 Chemical and Physical Properties

Molecular Formula	C₁₆H₁₅ClN₂OS
Molecular Weight	318.8 g/mol
XLogP3	3.5
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	2
Exact Mass	318.0593620 g/mol
Monoisotopic Mass	318.0593620 g/mol
Topological Polar Surface Area	60.9 Å²
Heavy Atom Count	21
Formal Charge	0
Complexity	442
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

For the treatment of anxiety disorders.

5 Pharmacology and Biochemistry

5.1 Pharmacology

Clotiazepam is a thienodiazepine possessing anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It increases the stage 2 non-rapid eye movement sleep.

5.2 ATC Code

N05BA21

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

N05B - Anxiolytics

N05BA - Benzodiazepine derivatives

N05BA21 - Clotiazepam

5.3 Metabolism/Metabolites

Hepatic.

Clotiazepam has known human metabolites that include Hydroxy-clotiazepam and desmethyl-clotiazepam.

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

5.4 Biological Half-Life

4 hours

5.5 Mechanism of Action

Clotiazepam acts at the benzodiazepine receptors (BZD). This agonizes the action of GABA, increasing the frequency of opening of the channel chlorinates and penetration of the ions chlorinates through the ionophore. Increase in membrane polarization decreases the probability of discharge of neurons.

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API Reference Price

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