N-Desmethylflunitrazepam
(Synonyms: 去甲基氟西泮,Norflunitrazepam) 目录号 : GC45522An Analytical Reference Material
Cas No.:2558-30-7
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
N-Desmethylflunitrazepam is an analytical reference material categorized as an benzodiazepine.[1] It is a metabolite of flunitrazepam . This product is intended for research and forensic applications.
Reference:
[1]. Katselou, M., Papoutsis, I., Nikolaou, P., et al. Metabolites replace the parent drug in the drug arena. The cases of fonazepam and nifoxipam. Forensic Toxicol. 35(1), (2017).
| Cas No. | 2558-30-7 | SDF | |
| 别名 | 去甲基氟西泮,Norflunitrazepam | ||
| 化学名 | 5-(2-fluorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one | ||
| Canonical SMILES | O=C1CN=C(C2=CC=CC=C2F)C3=C(C=CC([N+]([O-])=O)=C3)N1 | ||
| 分子式 | C15H10FN3O3 | 分子量 | 299.3 |
| 溶解度 | 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 | 3.3411 mL | 16.7056 mL | 33.4113 mL |
| 5 mM | 0.6682 mL | 3.3411 mL | 6.6823 mL |
| 10 mM | 0.3341 mL | 1.6706 mL | 3.3411 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。
Metabolic Profile of Flunitrazepam: Clinical and Forensic Toxicological Aspects
Drug Metab Lett 2017 Nov 17;11(1):14-20.PMID:28403803DOI:10.2174/1872312811666170407164216.
Background: Flunitrazepam (FNZ) is a potent hypnotic, sedative, and amnestic drug used to treat insomnia and as a pre-anesthetic agent. The illicit practice in drug-facilitated sexual assault led to important clinical and forensic concerns. Objective: In this work the metabolism of FNZ, and pharmacological- and toxicological-related effects, were fully reviewed. Methods: FNZ and related known metabolizing enzymes and metabolites were searched in books and in PubMed (U.S. National Library of Medicine) without a limiting period. Results: Major metabolic pathways include N-demethylation, 3-hydroxylation, nitro-reduction, and further N-acetylation of the amino group, yielding N-Desmethylflunitrazepam, 3-hydroxy-flunitrazepam, 7-aminoflunitrazepam, and 7-acetamidoflunitrazepam, respectively. A combination of these reactions may lead to the formation of 7-amino-N-desmethylflunitrazepam, 7-acetamido-N-desmethylflunitrazepam, 3- hydroxy-7-aminoflunitrazepam, 3-hydroxy-7-acetamidoflunitrazepam, 3-hydroxy-N-desmethylflunitrazepam and glucuronide conjugates. Genotypic variations in enzymes, interactions with other drugs or stability of FNZ during storage can result in large interindividual variability in the toxicological results. Conclusion: It is aimed that knowing the metabolism of FNZ may lead to the development of new analytical strategies for early detection, since this drug is typically present in very low concentrations in blood and urine when used to facilitate sexual assault.
Determination of flunitrazepam and its metabolites in blood by high-performance liquid chromatography-atmospheric pressure chemical ionization mass spectrometry
J Chromatogr B Biomed Sci Appl 1998 Aug 25;713(2):361-9.PMID:9746251DOI:10.1016/s0378-4347(98)00207-2.
A selective assay of flunitrazepam (F) and its metabolites 7-aminoflunitrazepam (7-AF), N-Desmethylflunitrazepam (N-DF) and 3-hydroxyflunitrazepam (3-OHF) with liquid chromatography-atmospheric pressure chemical ionization mass spectrometry (LC-APCI-MS, positive ions) is described. The drugs were isolated from serum, blood or urine using a solid-phase extraction procedure previously applied to various drugs of abuse. F-d3 and 7-AF-d3 were used as internal standards. The drugs were separated on ODS column in acetonitrile-50 mM ammonium formate buffer, pH 3.0 (45:55, v/v). After analysis of mass spectra taken in full scan mode, a selected-ion monitoring detection was applied with following ions: m/z 284 (7-AF and F), 287 (7-AF-d3 and F-d3), 314 (F), 300 (N-DF and 3-OHF), 317 (F-d3), 330 (3-OHF). The limits of detection were: 0.2 microg/l for F and 7-AF, 1 microg/l for N-DF and 3-OHF. The method was linear in the range 1-500 microg/l, the recoveries ranged from 92 to 99%. The method was applied for determination of F and metabolites in clinical and forensic samples. LC-APCI-MS seems to be a method of choice for these compounds.
Mass Spectra and Cross-Contribution of Ion Intensity Between Drug Analytes and Their Isotopically Labelled Analogs - Benzodiazepines and Their Derivatives
Forensic Sci Rev 2009 Jul;21(2):69-144.PMID:26242324doi
With GC-MS as the preferred method and isotopically labeled analogs (ILAs) of the analytes as the internal standards (ISs) of choice for quantitative determination of drugs/metabolites in biological specimens, one important aspect associated with chemical derivatization (CD) is that the CD products derived from the analyte and the selected IS must generate ions suitable for designating the analyte and the IS. These ions must not have significant cross-contribution (CC), i.e., ISs' contribution to the intensities of the ions designating the analytes, and vice versa. With this in mind, the authors have reviewed literature and information provided by manufacturers, searching for suitable CD reagents, CD methods, and ILAs of the analytes related to the following 18 benzodiazepines: oxazepam, diazepam, nordiazepam, nitrazepam, temazepam, clonazepam, 7-aminoclonazepam, prazepam, lorazepam, flunitrazepam, 7-aminoflunitrazepam, N-desalkylflurazepam, N-Desmethylflunitrazepam, 2-hydroxyethylflurazepam, estazolam, alprazolam, α-hydroxyalprazolam, and α-hydroxytriazolam. These analytes and ILAs were derivatized with various derivatization groups, followed by GC-MS analysis. The resulting mass spectrometric data are systematically presented in two forms: (a) full-scan mass spectra; and (b) CC data of ion-pairs with potential for designating the analytes and their respective ILAs (candidates of ISs in quantitative analytical protocols). Many of these full-scan mass spectra are not yet available in the literature and should be of reference value to laboratories engaged in the analysis of these drugs/metabolites. Full-scan MS data were further used to select ion-pairs with potential for designating the analytes and ISs in quantitative analysis protocols. The CC data of these ion-pairs were evaluated using data collected in selected ion monitoring mode and systematically tabulated, making the data readily available for analysts searching for this important analytical parameter.
Automated in-tube solid-phase microextraction coupled with liquid chromatography-electrospray ionization mass spectrometry for the determination of selected benzodiazepines
J Anal Toxicol 2000 Nov-Dec;24(8):718-25.PMID:11110028DOI:10.1093/jat/24.8.718.
A simple, rapid, and sensitive method, which allowed us to simultaneously determine seven benzodiazepines (diazepam, nordiazepam, temazepam, oxazepam, 7-aminoflunitrazepam, N-Desmethylflunitrazepam, and clonazepam) in buffer solution and in urine and serum samples, was investigated by automated in-tube solid-phase microextraction (SPME) coupled with liquid chromatography-electrospray ionization mass spectrometry (LC-ESI-MS). In-tube SPME, in which the analytes were extracted from the sample directly into an open tubular capillary column by repeated draw/eject cycles of sample solution, is an extraction technique for organic compounds in aqueous samples. The separation of benzodiazepines was carried out under ion-suppressed reversed-phase conditions by using methanol/50mM ammonium acetate in water (60:40) as a mobile phase with a Supelco LC-18 column. The optimal extraction condition was 10 draw/eject cycles of 30 mL of sample in 100mM Tris-HCl (pH 8.5) at a flow rate of 0.3 mL/min using a piece of 60-cm length Supelco-Q plot capillary column as the extraction capillary. The quantitative study was explored by operating in selected-ion monitoring (SIM) mode. The calibration curves were linear in the range from 0.5 ng/mL or 2 ng/mL to 500 ng/mL. The detection limits were from 0.02 ng/mL to 2 ng/mL. At the optimized capillary and fragmentor voltages, the characteristic ions for each compound clearly showed up in the spectra and it is possible to use the LC-MS to identify these compounds. The method was applied to the analysis of biological samples without interfering peaks. However, the recoveries for some of the compounds in serum samples need to be further improved.
Sweeping technique combined with micellar electrokinetic chromatography for the simultaneous determination of flunitrazepam and its major metabolites
J Chromatogr A 2006 Mar 31;1110(1-2):240-4.PMID:16483590DOI:10.1016/j.chroma.2006.01.070.
A sweeping technique, in conjunction with micellar electrokinetic chromatography, for the simultaneous determination of flunitrazepam and its major metabolites, 7-aminoflunitrazepam and N-Desmethylflunitrazepam, is described. The optimized conditions for the sweeping and separation were a pH 9.5 buffer, 25mM borate, 50mM cetyltrimethylammonium bromide, 30% MeOH (v/v), and a 151-mm injection length. The calibration functions were all linear with the coefficient of determination (r(2)) exceeding 0.996 for the three target compounds. Using the sweeping procedure, the limits of detection were determined to be 13.4, 5.6, and 12.0ng/mL for flunitrazepam, 7-aminoflunitrazepam, and N-Desmethylflunitrazepam, respectively, and the sensitivity enhancement for each compound was within the range of 110-200 fold. The RSDs for the retention time and the peak area were less than 4.10%. The optimized sweeping method was also used to examine a spiked urine sample. We conclude that sweeping with micellar electrokinetic chromatography has considerable potential use in clinical and forensic analyses of flunitrazepam and its metabolites.