Brotizolam | Indormyl | We-941 | CAS#57801-81-7 | GABA-A receptor Agonist

MedKoo Cat#: 329214 | Name: Brotizolam

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Brotizolam, also known as Indormyl and We-941, is a GABA-A receptor agonist used to treat insomnia. This drug is unscheduled in the United States. However, it is considered a scheduled substance in several countries such as Canada (Schedule IV), Germany (Schedule III), and the United Kingdom (Class C).

Chemical Structure

Brotizolam

CAS#57801-81-7

Theoretical Analysis

MedKoo Cat#: 329214

Name: Brotizolam

CAS#: 57801-81-7

Chemical Formula: C15H10BrClN4S

Exact Mass: 391.9498

Molecular Weight: 393.69

Elemental Analysis: C, 45.76; H, 2.56; Br, 20.30; Cl, 9.00; N, 14.23; S, 8.14

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 950.00	2 Weeks

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Related CAS #

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Synonym

Brotizolam; We-941; We-941-BS; We 941; We 941 BS; We941; We941BS; Indormyl; Lendormin

IUPAC/Chemical Name

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

InChi Key

UMSGKTJDUHERQW-UHFFFAOYSA-N

InChi Code

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

SMILES Code

CC1=NN=C2N1C3=C(C=C(Br)S3)C(C4=CC=CC=C4Cl)=NC2

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 393.69 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Hosono T, Homma M, Satoh M, Kohda Y. Variables influencing patient satisfaction for hypnotics: difference between zolpidem and brotizolam. J Clin Pharm Ther. 2014 Oct;39(5):507-10. doi: 10.1111/jcpt.12174. PubMed PMID: 24828966. 2: Yan X, Huang S, Ma C, Shen Y, Gu N, Chen H, Wu W, Li S, Hong Z, Li H. A randomized, double-blind, double-dummy, multicenter, controlled trial on brotizolam intervention in outpatients with insomnia. Int J Psychiatry Clin Pract. 2013 Oct;17(4):239-43. doi: 10.3109/13651501.2012.735242. PubMed PMID: 23025837. 3: Liao XY, Yamakawa M, Suto S, Shigenobu K, Makimoto K. Changes in activity patterns after the oral administration of brotizolam in institutionalized elderly patients with dementia. Psychogeriatrics. 2012 Jun;12(2):99-105. doi: 10.1111/j.1479-8301.2011.00401.x. PubMed PMID: 22712643. 4: Van Reenen CG, Hopster H, Van der Werf JT, Engel B, Buist WG, Jones RB, Blokhuis HJ, Korte SM. The benzodiazepine brotizolam reduces fear in calves exposed to a novel object test. Physiol Behav. 2009 Feb 16;96(2):307-14. doi: 10.1016/j.physbeh.2008.10.016. PubMed PMID: 18996404. 5: Tanaka N, Kinoshita H, Jamal M, Ohkubo E, Kumihashi M, Ameno K. A case of drowning whilst under the influence of brotizolam, flunitrazepam and ethanol. Soud Lek. 2011 Jan;56(1):5-6. PubMed PMID: 21413452. 6: Sugimoto Y, Kugimiya A, Yoshimura Y, Naoki H. Structural elucidation of novel degradation product of brotizolam. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3515-8. doi: 10.1016/j.bmcl.2013.04.044. PubMed PMID: 23664212. 7: Nishiyama T, Yamashita K, Yokoyama T, Imoto A, Manabe M. Effects of quazepam as a preoperative night hypnotic: comparison with brotizolam. J Anesth. 2007;21(1):7-12. PubMed PMID: 17285406. 8: Anand A, Saraf MK, Prabhakar S. Sustained inhibition of brotizolam induced anterograde amnesia by norharmane and retrograde amnesia by L-glutamic acid in mice. Behav Brain Res. 2007 Aug 22;182(1):12-20. PubMed PMID: 17561282. 9: Osanai T, Ohkubo T, Yasui N, Kondo T, Kaneko S. Effect of itraconazole on the pharmacokinetics and pharmacodynamics of a single oral dose of brotizolam. Br J Clin Pharmacol. 2004 Nov;58(5):476-81. PubMed PMID: 15521894; PubMed Central PMCID: PMC1884630. 10: Cho HJ, Jo K, Yi H, Cho SM, Abd El-Aty AM, Kim MK, Han SB, Oh JH, Kwon CH, Shim JH, Shin HC. Development and validation of a liquid chromatography method with electrospray ionization tandem mass spectrometry for the determination of brotizolam residues in beef and commercial whole milk. Biomed Chromatogr. 2011 Sep;25(9):1061-6. doi: 10.1002/bmc.1579. PubMed PMID: 21400549. 11: Tokairin T, Fukasawa T, Yasui-Furukori N, Aoshima T, Suzuki A, Inoue Y, Tateishi T, Otani K. Inhibition of the metabolism of brotizolam by erythromycin in humans: in vivo evidence for the involvement of CYP3A4 in brotizolam metabolism. Br J Clin Pharmacol. 2005 Aug;60(2):172-5. PubMed PMID: 16042670; PubMed Central PMCID: PMC1884921. 12: Ujiie Y, Fukasawa T, Yasui-Furukori N, Suzuki A, Tateishi T, Otani K. Rifampicin markedly decreases plasma concentration and hypnotic effect of brotizolam. Ther Drug Monit. 2006 Jun;28(3):299-302. PubMed PMID: 16778710. 13: Khamaisi M. Severe hypoglycaemia from repaglinide-brotizolam drug interaction: a case report and literature review. Diabet Med. 2012 Sep;29(9):1214-5. doi: 10.1111/j.1464-5491.2012.03631.x. Review. PubMed PMID: 22414218. 14: Weisenberg M, Sessler DI, Tavdi M, Gleb M, Ezri T, Dalton JE, Protianov M, Zimlichmann R. Dose-dependent hemodynamic effects of propofol induction following brotizolam premedication in hypertensive patients taking angiotensin-converting enzyme inhibitors. J Clin Anesth. 2010 May;22(3):190-5. doi: 10.1016/j.jclinane.2009.07.008. PubMed PMID: 20400005. 15: Katz N, Pillar G, Peled E, Segev A, Peled N. Sublingual Flumazenil for the Residual Effects of Hypnotics: Zolpidem and Brotizolam. Clin Pharmacol Drug Dev. 2012 Apr;1(2):45-51. doi: 10.1177/2160763X12437201. PubMed PMID: 27121218. 16: Yokota SI, Horikawa K, Akiyama M, Moriya T, Ebihara S, Komuro G, Ohta T, Shibata S. Inhibitory action of brotizolam on circadian and light-induced per1 and per2 expression in the hamster suprachiasmatic nucleus. Br J Pharmacol. 2000 Dec;131(8):1739-47. PubMed PMID: 11139454; PubMed Central PMCID: PMC1572494. 17: Silva A, Collao A, Orellana M, Meléndez J, Caviedes P, Cárdenas AM. Zopiclone, but not brotizolam, impairs memory storage during sleep. Neurosci Res. 2003 Oct;47(2):241-3. PubMed PMID: 14512149. 18: Kawahara R, Nishimura S, Inagaki Y, Taenaka N, Kawahara H. Actigraphic assessment of the preoperative hypnotic effects of brotizolam and zopiclone. Acta Anaesthesiol Belg. 2002;53(1):27-31. PubMed PMID: 11975426. 19: Uchimura N, Nakajima T, Hayash K, Nose I, Hashizume Y, Ohyama T, Habukawa M, Kotorii N, Kuwahara H, Maeda H. Effect of zolpidem on sleep architecture and its next-morning residual effect in insomniac patients: a randomized crossover comparative study with brotizolam. Prog Neuropsychopharmacol Biol Psychiatry. 2006 Jan;30(1):22-9. PubMed PMID: 16048734. 20: Senda C, Kishimoto W, Sakai K, Nagakura A, Igarashi T. Identification of human cytochrome P450 isoforms involved in the metabolism of brotizolam. Xenobiotica. 1997 Sep;27(9):913-22. PubMed PMID: 9381732.