Doxefazepam
(Synonyms: 度氟西泮,SAS-643) 目录号 : GC63590
Doxefazepam 是一种苯并二氮 (benzodiazepine) 衍生物。具有抗焦虑，抗惊厥作用。
Cas No.:40762-15-0
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
Doxefazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties.
Groups of 50 male and 50 female Sprague-Dawley rats are given food containing sufficient Doxefazepam, a benzodiazepine derivative, to ensure intakes of 0, 3, 10, or 30 mg/kg/day. Rats are treated for 104 weeks and then euthanized. An extensive autopsy is performed on those animals that died intercurrently and on euthanized animals. The chronic administration of Doxefazepam does not influence the survival of the rats. A significant linear trend in the incidence of hepatocellular neoplasms, primarily benign, is observed in the female treated groups. This higher incidence is not associated to a higher occurrence of focal hyperplasia or other preneoplastic lesions in treated rats. The brain, a target organ for the pharmacological activity of Doxefazepam, is carefully examined to search for microscopic foci of proliferative cells. A total of 12 and 6 malignant gliomas are observed in male and female rats, respectively; only two are noticed at autopsy. These tumors are mainly of the oligodendroglioma type commonly found in aged rats[1]. Doxefazepam is investigated in a series of toxicological studies. Oral LD50 values are greater than 2000 mg/kg in mice, rats and dogs, while endoperitoneal LD50 values are 746 and 544 mg/kg in the mice and rats, respectively, and greater than 1000 mg/kg in the dogs[2].
[1]. Borelli G, et al. Carcinogenicity study of doxefazepam administered in the diet to Sprague-Dawley rats. Fundam Appl Toxicol. 1990 Jul;15(1):82-92.
[2]. Bertoli D, et al. Toxicological evaluations of the benzodiazepine doxefazepam. Arzneimittelforschung. 1989 Apr;39(4):480-4.
| Cas No. | 40762-15-0 | SDF | |
| 别名 | 度氟西泮,SAS-643 | ||
| 分子式 | C17H14ClFN2O3 | 分子量 | 348.76 |
| 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 | 2.8673 mL | 14.3365 mL | 28.673 mL |
| 5 mM | 0.5735 mL | 2.8673 mL | 5.7346 mL |
| 10 mM | 0.2867 mL | 1.4337 mL | 2.8673 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。
Effects of Doxefazepam on normal sleep. An EEG and neuropsychological study
Neuropsychobiology 1984;11(2):133-9.PMID:6483162DOI:10.1159/000118066.
The effects on sleep of a putative hypnotic, benzodiazepine (Doxefazepam), were studied in 7 healthy volunteers. Subjects were administered placebo or the active compound at 10-, 20-, and 40-mg oral dose prior to 13 consecutive nights during which they slept in the EEG laboratory. Full-night EEG recordings were obtained, and the hypnogram was determined. The subjective characteristics of sleep (quality, dreams, etc.) were defined by self-administered rating scales; neuropsychological and quantitative waking EEG measurements were performed before drug/placebo administration and in the morning following the final awakening, in order to identify possible signs of 'hangover'. Volunteers thereafter slept at home for 15 nights, self-administering 10 mg Doxefazepam each night, and returned to the laboratory for 2 additional full-night sleep recordings. The drug plasma concentration was monitored during the study. Doxefazepam (10 mg) reduced the number of intermediate awakenings and the shifts between distinct sleep phases; single 20- or 40-mg doses or a 2-week administration of 10 mg Doxefazepam increased significantly the total sleep duration and the percent duration of the phase 2 and the synchronized sleep and decreased the percent duration of phase 1 and of the intermediate awakenings. Volunteers reported an improvement in the subjective 'quality' of sleep, while evident signs of 'hangover' were not observed. The compound appeared to be of potential use as a sleep regulator.
Carcinogenicity study of Doxefazepam administered in the diet to Sprague-Dawley rats
Fundam Appl Toxicol 1990 Jul;15(1):82-92.PMID:1973676DOI:10.1016/0272-0590(90)90165-g.
Groups of 50 male and 50 female Sprague-Dawley rats were given food containing sufficient Doxefazepam, a benzodiazepine derivative, to ensure intakes of 0, 3, 10, or 30 mg/kg/day. These dosages respectively correspond to 2, 20, and 60 times the mean daily hypnotic dose level of an adult man. Rats were treated for 104 weeks and then euthanized. An extensive autopsy was performed on those animals that died intercurrently and on euthanized animals. The chronic administration of Doxefazepam did not influence the survival of the rats. No treatment-related changes in clinical signs and body weight gains occurred and malignant tumor rates were similar in controls and treated animals. A significant linear trend in the incidence of hepatocellular neoplasms, primarily benign, was observed in the female treated groups. This higher incidence was not associated to a higher occurrence of focal hyperplasia or other preneoplastic lesions in treated rats. The brain, a target organ for the pharmacological activity of Doxefazepam, was carefully examined to search for microscopic foci of proliferative cells. A total of 12 and 6 malignant gliomas were observed in male and female rats, respectively; only two were noticed at autopsy. These tumors were mainly of the oligodendroglioma type commonly found in aged rats. Their incidence was slightly higher in treated rats, but results were not of statistical significance. The overall evaluation of the present study indicates that Doxefazepam is noncarcinogenic in rats. However, the increase in liver adenomas found here as well as in previous bioassays with similar drugs and the lack of reliable historical data on the incidence of brain tumors in benzodiazepine-treated rodents suggest that additional experimental and epidemiological studies should be undertaken to exhaustively assess the toxic potential of this widely used class of drugs.
Toxicological evaluations of the benzodiazepine Doxefazepam
Arzneimittelforschung 1989 Apr;39(4):480-4.PMID:2568837doi
1-(2-Hydroxyethyl)-3-hydroxyl-7-chloro-1,3-dihydro-5-(O-fluorophenyl)-2H - 1,4-benzodiazepin-2-one (Doxefazepam, SAS 643, Doxans) was investigated in a series of toxicological studies. Oral LD50 values were greater than 2000 mg/kg in mice, rats and dogs, while endoperitoneal LD50 values were 746 and 544 mg/kg in the mice and rats, respectively, and greater than 1000 mg/kg in the dogs. Subacute and chronic studies in rats and dogs evidenced a transient ataxia after administration of the test compound, which was dose-dependent in the subacute experiment, and occurred only at the highest dose in the chronic studies. No pathological findings were registered at necropsy or in microscopic observations, except an increase of liver weight at the highest dosage in the chronic study in the rat. Doxefazepam did not exert any teratogenic effects in rats and rabbits. Moreover in rats it did not alter the reproductive performance. The mutagenic studies did not reveal any mutagenic potential. In the cancerogenicity study in rats Doxefazepam did not show positive carcinogenic potential.