Bromazolam
(Synonyms: 8-溴-1-甲基-6-苯基-4H-[1,2,4]三氮唑并[4,3-A][1,4]苯并二氮杂卓) 目录号 : GC42980
An Analytical Reference Standard
Cas No.:71368-80-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Kinase experiment [1]: | |
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Preparation Method |
They were treated with pHLS9 (2 mg protein /mL), 25 μg/mL Alamethicin (UGT reaction mixture B), 90 mM phosphate buffer (pH 7.4), 2.5 mM mg 2+, 2.5 mM isocitrate, and 0.6 mM at 37°C NADP +, 0.9 U/mL isocitrate dehydrogenase, 100 U/mL superoxide dismutase and 0.1 mM acetyl-CoA. Then, 2.5 mM UDP-glucuronic acid (UGT reaction mixture solution A), 40 μM PAPS, 1.2 mM SAM, 1 mM dithiothreitol, 10 mM glutathione, and 50 μM clobromazolam or Bromazolam were added. |
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Reaction Conditions |
50 μM Bromazolam for 360min in 37°C |
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Applications |
Bromazolam metabolites were identified in pHLS9 incubation. |
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References: [1]: Wagmann L, Manier SK, Felske C, Gampfer TM, Richter MJ, Eckstein N, Meyer MR. Flubromazolam-Derived Designer Benzodiazepines: Toxicokinetics and Analytical Toxicology of Clobromazolam and Bromazolam. J Anal Toxicol. 2021 Nov 9;45(9):1014-1027. doi: 10.1093/jat/bkaa161. PMID: 33048135. |
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Bromazolam is a triazolobenzodiazepine that is known as research chemical XLI-268[1]. Bromazolam is structurally similar to alprazolam but is the bromo rather than the chloro analog[2]. Bromazolam metabolites were identified in pHLS9 incubation[3].Bromazolam (XLI-268) is a triazolobenzodiazepine (TBZD),It is the bromo instead of chloro analogue of alprazolam and has similar sedative and anxiolytic effects to it and other benzodiazepines.Bromazolam is a non subtype selective agonist at the benzodiazepine site of GABAA receptors, with a binding affinity of 2.81nM at the α1 subtype, 0.69nM at α2 and 0.62nM at α5.
References:
[1]: PubChem. 8-Bromo-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine. pubchem.ncbi.nlm.nih.gov website. Accessed August 18, 2021. https://pubchem.ncbi.nlm.nih.gov/compound/12562546
[2]: McDermott S, Johnson BE, Balasanova AA. Phenibut and Bromazolam Use Disorders Requiring Hospitalization for Medically Supervised Withdrawal. Prim Care Companion CNS Disord. 2022 Jul 12;24(4):21cr03119. doi: 10.4088/PCC.21cr03119. PMID: 35830740.
[3]: Wagmann L, Manier SK, Felske C, Gampfer TM, Richter MJ, Eckstein N, Meyer MR. Flubromazolam-Derived Designer Benzodiazepines: Toxicokinetics and Analytical Toxicology of Clobromazolam and Bromazolam. J Anal Toxicol. 2021 Nov 9;45(9):1014-1027. doi: 10.1093/jat/bkaa161. PMID: 33048135.
溴马唑仑是一种三唑并苯并二氮杂卓，被称为研究化学品 XLI-268[1]。溴马唑仑在结构上与阿普唑仑相似，但它是溴代而非氯代类似物[2]。在 pHLS9 孵育中鉴定了溴马唑仑代谢物[3]。溴马唑仑 (XLI-268) 是一种三唑并苯二氮卓类药物 (TBZD)，它是阿普唑仑的溴代而非氯代类似物，具有与其类似的镇静和抗焦虑作用和其他苯二氮卓类药物。溴马唑仑是 GABAA 受体苯二氮卓位点的非亚型选择性激动剂，在 α1 亚型上的结合亲和力为 2.81nM，在 α2 上的结合亲和力为 0.69nM，在 α5 上的结合亲和力为 0.62nM。
| Cas No. | 71368-80-4 | SDF | |
| 别名 | 8-溴-1-甲基-6-苯基-4H-[1,2,4]三氮唑并[4,3-A][1,4]苯并二氮杂卓 | ||
| 化学名 | 8-bromo-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine | ||
| Canonical SMILES | CC1=NN=C(N1C2=CC=C(Br)C=C23)CN=C3C4=CC=CC=C4 | ||
| 分子式 | C17H13BrN4 | 分子量 | 353.2 |
| 溶解度 | 5mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8313 mL | 14.1563 mL | 28.3126 mL |
| 5 mM | 0.5663 mL | 2.8313 mL | 5.6625 mL |
| 10 mM | 0.2831 mL | 1.4156 mL | 2.8313 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Bromazolam Blood Concentrations in Postmortem Cases-A British Columbia Perspective
J Anal Toxicol 2023 Apr 14;47(4):385-392.PMID:36715069DOI:10.1093/jat/bkad005.
Bromazolam is a designer benzodiazepine that was first detected in British Columbia in January 2021. Postmortem cases were analyzed using a comprehensive blood drug screening procedure by liquid chromatography-high-resolution mass spectrometry before being retrospectively analyzed using an in-house novel psychoactive substances data processing method. Bromazolam was detected in 41 postmortem cases in 2021 and quantitatively confirmed by standard addition, using liquid chromatography-tandem mass spectrometry. The mean Bromazolam concentration observed was 11.4 ± 53.7 ng/mL (median concentration: 1.6 ng/mL), with a range from 0.5 to 319.3 ng/mL and the majority of cases co-occurring with fentanyl. These low concentrations may be indicative of a presumed enhancement of opioid effects, rather than being used as a stand-alone drug. Bromazolam was always detected with opioids (fentanyl and carfentanil), stimulants (methamphetamine) and/or other benzodiazepines (etizolam and flualprazolam). To our knowledge, this is the first report to provide concentrations of Bromazolam in postmortem blood samples in Canada.
Flubromazolam-Derived Designer Benzodiazepines: Toxicokinetics and Analytical Toxicology of Clobromazolam and Bromazolam
J Anal Toxicol 2021 Nov 9;45(9):1014-1027.PMID:33048135DOI:10.1093/jat/bkaa161.
Flubromazolam is widely known as highly potent designer benzodiazepine (DBZD). Recently, the two flubromazolam-derived new psychoactive substances (NPS) clobromazolam and Bromazolam appeared on the drugs of abuse market. Since no information concerning their toxicokinetics in humans is available, the aims of the current study were to elucidate their metabolic profile and to identify the isozymes involved in their phase I and phase II metabolism. In vitro incubations with pooled human liver S9 fraction were performed and analyzed by liquid chromatography coupled to orbitrap-based high-resolution tandem mass spectrometry (LC-HRMS-MS). Biosamples after the ingestion of Bromazolam allowed the identification of metabolites in human plasma and urine as well as the determination of Bromazolam plasma concentrations by LC-HRMS-MS using the standard addition method. In total, eight clobromazolam metabolites were identified in vitro as well as eight Bromazolam metabolites in vitro and in vivo. Predominant metabolic steps were hydroxylation, glucuronidation and combinations thereof. Alpha-hydroxy Bromazolam glucuronide and Bromazolam N-glucuronide are recommended as screening targets in urine. Bromazolam and its alpha-hydroxy metabolite are recommended if conjugate cleavage is part of the sample preparation procedure. The Bromazolam plasma concentrations were determined to be 6 and 29 μg/L, respectively. Several cytochrome P450 (CYP) and uridine 5'-diphospho-glucuronosyltransferase (UGT) isozymes were shown to catalyze their metabolic transformations. CYP3A4 was involved in the formation of all phase I metabolites of both NPS, while UGT1A4 and UGT2B10 catalyzed their N-glucuronidation. Several UGT isoforms catalyzed the glucuronidation of the hydroxy metabolites. In conclusion, the determined Bromazolam plasma concentrations in the low micrograms per liter range underlined the need for sensitive analytical methods and the importance of suitable urine screening procedures including DBZD metabolites as targets. Such an analytical strategy should be also applicable for clobromazolam.
Determination of Cross-Reactivity of Novel Psychoactive Substances with Drug Screen Immunoassays Kits in Whole Blood
J Anal Toxicol 2022 Aug 13;46(7):726-731.PMID:34791285DOI:10.1093/jat/bkab110.
The purpose of this study was to examine the impact of 59 novel psychoactive compounds on common enzyme-linked immunosorbent assay (ELISA) testing kits. Concentrations above and below the individual kit reporting limits in each class were measured. Compounds that exhibited cross-reactivity were then spiked individually using a seven-point response curve to determine the level of cross-reactivity. Diclazepam, delorazepam, phenazepam, flualprazolam, Bromazolam, adinazolam, 3-methoxy-PCP, 3-hydroxy-PCP (3-OH-PCP), phenylfentanyl, para-methylacetylfentanyl and para-fluorofuranylfentanyl were determined to cross-react in the respective kits below. Herein, we detail the cross-reactivity that was observed with the above novel psychoactive substances on Immunalysis Benzodiazepine (BEN), Phencyclidine (PCP), Fentanyl (FEN), Buprenorphine (BUP), Opiates (OPI) and Oxycodone (OXY) Direct ELISA kits.
New trends of new psychoactive substances (NPS)-infused chocolate: Identification and quantification of trace level of NPS in complex matrix by GC-MS and NMR
Talanta 2023 Apr 1;255:124257.PMID:36630788DOI:10.1016/j.talanta.2023.124257.
For the first time, the identification and quantification of trace level of new psychoactive substances (NPS) in a complex chocolate matrix have been reported. Since the beginning of 2022, suspected NPS-infused chocolate samples confiscated in inbound packages have been continuously sent to our laboratory for analysis. The qualitative gas chromatography-mass spectrometry (GC-MS) results were verified by 1H nuclear magnetic resonance (1H NMR) and 19F NMR to distinguish between potential aromatic isomers. A total of 11 NPS including deoxymethoxetamine, 3-OH-PCP, 6-APB, 4-APB, 4-OH-MiPT, 3-FEA, 2-FEA, 3-MMC, Bromazolam, 2-FDCK, and ADB-BUTINACA were detected in 65 seized chocolate samples. A general 1H quantitative NMR (1H qNMR) method for quantification of 297 types of NPS in complex chocolate matrixes was devised for the first time after rigorous analysis of various critical features of merit, including suitable deuterated solvent, internal standard, quantitative peaks, and instrument acquisition parameters. Validation of the method using six different types of NPS afforded limits of detection of 0.05-0.1 mg/mL, limits of quantification of 0.01-0.03 mg/mL, repeatability and reproducibility lower than 0.5% and 3.6%, recoveries of 91.7%∼104.4%, and absence of matrix effect. The quantitative analysis of 65 seized chocolate samples by 1H qNMR and 19F qNMR showed that the content of NPS was in the range of 0.5 mg/g∼44.1 mg/g. Generally, the developed qNMR method was simple, fast, precise, and can be performed without reference materials of NPS. Since the type and content of NPS are relatively random, chocolate consumers will face huge health risks. Therefore, this new trend of NPS-infused chocolate deserves and requires more attention from national NPS monitoring departments as well as forensic laboratories.