Cinolazepam
(Synonyms: 西诺西泮) 目录号 : GC43269An Analytical Reference Material
Cas No.:75696-02-5
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
Cinolazepam is an analytical reference material that is structurally categorized as a benzodiazepine. [1] It has a half-life of nine hours and has been shown to have efficacy in improving objective sleep variables in a clinical trial of situational insomnia induced by traffic noise. The physiological and toxicological properties of this compound are not known. This product is intended for research and forensic applications.
Reference:
[1]. Saletu, B., Kindshofer, G., Anderer, P., et al. Short-term sleep laboratory studies with cinolazepam in situational insomnia induced by traffic noise. Int. J. Clin. Pharmacol. Res. 7(5), 407-418 (1987).
| Cas No. | 75696-02-5 | SDF | |
| 别名 | 西诺西泮 | ||
| 化学名 | 7-chloro-5-(2-fluorophenyl)-2,3-dihydro-3-hydroxy-2-oxo-1H-1,4-benzodiazepine-1-propanenitrile | ||
| Canonical SMILES | ClC1=CC(C(C2=C(F)C=CC=C2)=NC3O)=C(C=C1)N(CCC#N)C3=O | ||
| 分子式 | C18H13ClFN3O2 | 分子量 | 357.8 |
| 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 | 2.7949 mL | 13.9743 mL | 27.9486 mL |
| 5 mM | 0.559 mL | 2.7949 mL | 5.5897 mL |
| 10 mM | 0.2795 mL | 1.3974 mL | 2.7949 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。
Muscle relaxants for pain management in rheumatoid arthritis
Cochrane Database Syst Rev 2012 Jan 18;1:CD008922.PMID:22258993DOI:10.1002/14651858.CD008922.pub2.
Background: Pain management is a high priority for patients with rheumatoid arthritis (RA). Muscle relaxants include drugs that reduce muscle spasm (for example benzodiazepines such as diazepam (Valium), alprazolam (Xanax), lorazepam (Ativan) and non-benzodiazepines such as metaxalone (Skelaxin) or a combination of paracetamol and orphenadrine (Muscol)) and drugs that prevent increased muscle tone (baclofen and dantrolene). Despite a paucity of evidence supporting their use, antispasmodic and antispasticity muscle relaxants have gained widespread clinical acceptance as adjuvants in the management of patients with chronic musculoskeletal pain. Objectives: The aim of this review was to determine the efficacy and safety of muscle relaxants in pain management in patients with RA. The muscle relaxants that were included in this review are the antispasmodic benzodiazepines (alprazolam, bromazepam, chlordiazepoxide,Cinolazepam, clonazepam, cloxazolam, clorazepate, diazepam, estazolam, flunitrazepam, flurazepam, flutoprazepam, halazepam, ketazolam, loprazolam, lorazepam, lormetazepam, medazepam, midazolam, nimetazepam, nitrazepam, nordazepam, oxazepam, pinazepam, prazepam, quazepam, temazepam, tetrazepam, triazolam), antispasmodic non-benzodiazepines (cyclobenzaprine, carisoprodol, chlorzoxazone, meprobamate, methocarbamol, metaxalone, orphenadrine, tizanidine and zopiclone), and antispasticity drugs (baclofen and dantrolene sodium). Search methods: We performed a search of the Cochrane Central Register of Controlled Trials (CENTRAL) (The Cochrane Library, 4th quarter 2010), MEDLINE (1950 to week 1 November 2010), EMBASE (Week 44 2010), and PsycINFO (1806 to week 2 November 2010). We also searched the 2008 to 2009 American College of Rheumatology (ACR) and European League Against Rheumatism (EULAR) abstracts and performed a handsearch of reference lists of relevant articles. Selection criteria: We included randomised controlled trials which compared a muscle relaxant to another therapy (active, including non-pharmacological therapies, or placebo) in adult patients with RA and that reported at least one clinically relevant outcome. Data collection and analysis: Two blinded review authors independently extracted data and assessed the risk of bias in the trials. Meta-analyses were used to examine the efficacy of muscle relaxants on pain, depression, sleep and function, as well as their safety. Main results: Six trials (126 participants) were included in this review. All trials were rated at high risk of bias. Five cross-over trials evaluated a benzodiazepine, four assessed diazepam (n = 71) and one assessed triazolam (n = 15). The sixth trial assessed zopiclone (a non-benzodiazepine) (n = 40) and was a parallel group study. No trial duration was longer than two weeks while three single dose trials assessed outcomes at 24 hours only. Overall the included trials failed to find evidence of a beneficial effect of muscle relaxants over placebo, alone (at 24 hrs, 1 or 2 weeks) or in addition to non-steroidal anti-inflammatory drugs (NSAIDs) (at 24 hrs), on pain intensity, function, or quality of life. Data from two trials of longer than 24 hours duration (n = 74) (diazepam and zopiclone) found that participants who received a muscle relaxant had significantly more adverse events compared with those who received placebo (number needed to harm (NNTH) 3, 95% CI 2 to 7). These were predominantly central nervous system side effects, including dizziness and drowsiness (NNTH 3, 95% CI 2 to 11). Authors' conclusions: Based upon the currently available evidence in patients with RA, benzodiazepines (diazepam and triazolam) do not appear to be beneficial in improving pain over 24 hours or one week. The non-benzodiazepine agent zopiclone also did not significantly reduce pain over two weeks. However, even short term muscle relaxant use (24 hours to 2 weeks) is associated with significant adverse events, predominantly drowsiness and dizziness.
Short-term sleep laboratory studies with Cinolazepam in situational insomnia induced by traffic noise
Int J Clin Pharmacol Res 1987;7(5):407-18.PMID:2889679doi
In a double-blind, placebo-controlled sleep-laboratory study the short-term effects of cinolazepam--a recently introduced 1,4 benzodiazepine with a half-life of 9 h--on the all-night sleep, morning awakening and early morning behaviour were investigated in 20 young normal subjects, whose sleep was experimentally disturbed by nocturnal traffic noise. The latter was prerecorded on tape and reproduced by loud speakers throughout the night with a sound pressure level of 68-90 dB(A) (energy equivalent mean noise level LAeq: 79dB(A)). According to the parallel group design subjects received either a placebo or 40 mg Cinolazepam. Specifically, they spent nine nights in the sleep laboratory: two adaptation nights, one baseline night on placebo, three drug or placebo nights, and three post-drug/placebo nights under traffic noise. Somnopolygraphic investigations were carried out between 22h30 and 06h00. The drug was given orally half an hour before bedtime. Each 30 sec epoch was scored according to the criteria of Rechtschaffen and Kales. In the morning the subjects were awakened by 1000 Hz tones which were increased in loudness in 10 dB steps in two minute intervals. A sleep self-rating scale for sleep and awakening quality was completed half an hour after the morning toilet. Thereafter noopsychic and thymopsychic variables were evaluated utilizing a psychometric test battery. Statistical analyses of objective sleep variables demonstrated a significant improvement of sleep maintenance after 40 mg Cinolazepam as reflected by an increase of sleep efficiency, decrease of wake time (during total sleep period) and number of awakenings as compared with the placebo. Sleep architecture was only affected slightly: sleep stage S1 decreased, S2 increased, while S3, S4 and SREM (S rapid eye movement) remained unchanged. Subjective sleep quality improved significantly as well. In the mornings there were no hangover signs, neither in subjective nor in objective psychometric and psychophysiological variables. Finally, the study suggests that man can adapt subjectively to nocturnal traffic noise over one week, although the improvement of objective sleep variables over time did not reach the level of statistical significance.
Analysis of drugs by polarography, XXXV: The polarographic behaviour of Cinolazepam[1-(2-cyanoethyl)-7-chloro-3-hydroxy-5-(2-fluorophe n yl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one] and assay of its tablets
Arch Pharm (Weinheim) 1992 Feb;325(2):65-8.PMID:1605717DOI:10.1002/ardp.19923250202.
Cinolazepam is reduced at the Dropping Mercury Electrode (DME) over the entire pH range in Britton Robinson buffers (BRB) containing 20% DMF as a solubilizer. A well-defined cathodic wave is obtained over the pH range 3-5, which is very suitable for analytical purposes. The wave was characterized as being irreversible, diffusion-controlled and free from adsorption phenomena. In acid buffers, 4 electrons are consumed in the reduction process, while in alkaline buffers the electrode reaction is somewhat complicated. Tablets containing 40 mg Cinolazepam were analysed using the polarographic and a developed HPLC method. The results obtained with both methods are in good accordance as revealed by statistical analysis. The details of the complicated mechanism of the reduction process at the DME are still under investigation but elucidated in principle.
A selective fluorimetric method for the determination of some 1,4-benzodiazepine drugs containing a hydroxyl group at C-3
J Pharm Biomed Anal 1994 Nov;12(11):1417-23.PMID:7849137DOI:10.1016/0731-7085(94)00070-0.
A highly selective and sensitive fluorimetric method was developed for the determination of four 1,4-benzodiazepine drugs containing a hydroxyl group at carbon 3, namely oxazepam, lorazepam, Cinolazepam and temazepam. The method is highly specific because other benzodiazepinee lacking the hydroxyl group at C-3 do not react similarly and hence do not interfere. The proposed method involves reduction of the target compound using Zno/HCl at room temperature with the formation of a highly fluorescent derivative within 15 min. The different experimental parameters were carefully studied and incorporated into the procedure. Under the described conditions, the proposed method is applicable over the concentration range of 0.1-1.2 micrograms ml-1 for both temazepam and Cinolazepam, and 0.2-2.5 and 1-8 micrograms ml-1 for oxazepam and lorazepam respectively. The recoveries of the title compounds from spiked urine ranged from 90.0 to 92.0% and for serum from 94.1 to 95.4% with a limit of detection (S/N = 2) of 4 ng ml-1 for all drugs. The mechanism of the fluorimetric reaction is discussed.
Separation, isolation and identification of optical isomers of 1,4-benzodiazepine glucuronides from biological fluids by reversed-phase high-performance liquid chromatography
J Chromatogr 1984 Mar 9;306:231-9.PMID:6715462DOI:10.1016/s0378-4347(00)80885-3.
A reversed-phase high-performance liquid chromatographic (HPLC) method for the determination of four separate 1,4-benzodiazepine glucuronides in urine, plasma and bile is presented. We succeeded not only in determining the single glucuronides but also in separating the enantiomers (optical isomers) of the 1,4-benzodiazepine glucuronides. The optical isomers of the glucuronides of oxazepam and Cinolazepam and of two other glucuronides of benzodiazepine metabolites could be well separated. The ratio of the isomers could be evaluated. An octadecyl reversed phase was used with a mobile phase of acetonitrile and 0.01 M orthophosphoric acid. After the initial separation, the isomers were fractionated by HPLC. After treatment with beta-glucuronidase to yield the aglycone, the separated fractions were hydrolysed to the corresponding benzophenones whose identity was confirmed by HPLC. Gas chromatography and gas chromatography-mass spectrometry demonstrated that the separated glucuronides corresponded to the enantiomeric benzodiazepines. Human urine and plasma as well as rabbit urine, plasma and bile were examined.