Carburazepam (RGH 3331)
(Synonyms: 卡布西泮,RGH 3331; Uxepam) 目录号 : GC31224
Carburazepam (RGH 3331) 是一种衍生自苯二氮卓类药物的药物。
Cas No.:59009-93-7
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
Carburazepam is a drug which derives from benzodiazepine. Benzodiazepines (BZD, BZs) are a class of psychoactive drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring.
Carburazepam is a drug which derives from benzodiazepine. Benzodiazepines(BZD, BZs) are a class of psychoactive drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring[1].
[1]. International Nonproprietary Names for Pharmaceutical Substances. Proposed International Nonproprietary Names (Prop. INN): List 39. Supplement to WHO Chronicle, 1978, Vol. 32, No. 3
| Cas No. | 59009-93-7 | SDF | |
| 别名 | 卡布西泮,RGH 3331; Uxepam | ||
| Canonical SMILES | O=C(N1CC(N(C)C2=CC=C(Cl)C=C2C1C3=CC=CC=C3)=O)N | ||
| 分子式 | C17H16ClN3O2 | 分子量 | 329.78 |
| 溶解度 | Soluble 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 | 3.0323 mL | 15.1616 mL | 30.3232 mL |
| 5 mM | 0.6065 mL | 3.0323 mL | 6.0646 mL |
| 10 mM | 0.3032 mL | 1.5162 mL | 3.0323 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。
[Pharmacology of uxepam]
A new daytime tranquilizer uxepam--1-methyl-4-carbamoyl-5-phenyl-7-chloro-1,3,4,5-tetrahydro-2H-1, 4-benzodiazepine-2-on (RGH-3331) administered to animals removes emotional-behavioral abnormalities under conflict situation, reduces aggressiveness induced by electric and painful stimulation, prevents convulsions induced by corasole and electric shock, prolongs the hypnotic effect of hexenal. When applied in high doses the drug suppresses the avoidance reflex, orienting-research behavior and motor activity, disturbs movement coordination. Within wide dosage range uxepam potentiates the summation activity in the central nervous system. As regards anxiolytic activity, the drug does not yield to diazepam and compares very favourably with chlordiazepoxide. The sedative and myorelaxant effects displayed by uxepam are insignificant. The data obtained make it possible to attribute uxepam to daytime tranquilizers.
Selective effect of clonazepam and (S)-uxepam on the binding of warfarin enantiomers to human serum albumin
Both clonazepam and (S)-uxepam selectively increase the binding of (S)-warfarin to human serum albumin. By liquid affinity chromatography, improved resolution of rac-warfarin was achieved.
Studies on the pharmacokinetics and metabolism of N(4)-carbamoyl-1,3,4,5-dihydro-diazepam (Uxepam(R)) in rats, dogs and man
The pharmacokinetics and metabolism of Uxepam(R), a new minor tranquillizer, have been investigated in rats [2], dogs and man. For the experiments in rats [2] separation of metabolites of 2-(14)C-uxepam was achieved by thin-layer chromatography. In the experiments on dogs and man, Extrelut microcolumns were used for preseparation. Recovery was 95% +/- 12.77 (S.D.) determined by radioactive tracer experiments. The compounds were separated and determined by reversed-phase HPLC with UV detection at 240 nm. The limit of detection for uxepam was 10 ng ml(-1). The metabolises were identified by mass spectrometry. The main metabolites in the rat were desmethyl-uxepam, 5-hydroxy-phenyl-desmethyl-uxepam and diazepam. Desmethyl-carbamoyl-dihydro-diazepam, diazepam and desmethyl-diazepam were found in human plasma. In dogs only one metabolite, desmethyl-uxepam, was detected in plasma. Enterohepatic recycling was observed in dogs and in humans.