Oxolamine citrate (SKF-9976 citrate)
(Synonyms: 柠檬酸奥索拉明; SKF-9976 citrate; AF-438 citrate) 目录号 : GC31727
Oxolamine (SKF-9976, AF-438) citrate, a cough suppressant, is an inhibitor of CYP2B1/2. Oxolamine citrate also exhibits anti-inflammatory effect.
Cas No.:1949-20-8
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
Oxolamine (SKF-9976, AF-438) citrate, a cough suppressant, is an inhibitor of CYP2B1/2. Oxolamine citrate also exhibits anti-inflammatory effect.
[1] Xuan Zhu, et al. Biopharm Drug Dispos. 2007 Apr;28(3):125-33. [2] G GIUDICI, F LEGNANI. Minerva Med. 1961 Oct 31;52:3752-5.
| Cas No. | 1949-20-8 | SDF | |
| 别名 | 柠檬酸奥索拉明; SKF-9976 citrate; AF-438 citrate | ||
| Canonical SMILES | CCN(CC)CCC1=NC(C2=CC=CC=C2)=NO1.O=C(CC(C(O)=O)(O)CC(O)=O)O | ||
| 分子式 | C20H27N3O8 | 分子量 | 437.44 |
| 溶解度 | DMSO : ≥ 33 mg/mL (75.44 mM) | 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 | 2.286 mL | 11.4301 mL | 22.8603 mL |
| 5 mM | 0.4572 mL | 2.286 mL | 4.5721 mL |
| 10 mM | 0.2286 mL | 1.143 mL | 2.286 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。
Sustained-release dosage form of oxolamine citrate: preparation and release kinetics
J Microencapsul.1992 Apr-Jun;9(2):167-72.PMID:1593399DOI: 10.3109/02652049109021232.
One of the principal uses of microencapsulation for pharmaceuticals has been the preparation of sustained-release dosage forms which have been usually presented in the form of a suspension or gel. However, a non-disintegrating tablet would be a better formulation to obtain sustained-release effect. Microencapsulation has been employed to provide protection of the core material against atmospheric effects, to cover the unpleasant taste and to enhance the stability. A number of drugs have also been encapsulated to reduce gastric and other GI tract irritations, to alter release properties and to change availability. Oxolamine citrate is one of the synthetic derivatives of 3,5-disubstituted 1,2,4-oxodiazole, used particularly for its antitussive activity. The usual dose of the drug is 200 mg given four times a day. Its use was limited by side-effects of nausea and vomiting. In order to prevent the disadvantages caused by taking the drug four times daily, and to reduce the side-effects, a sustained-release dosage form of oxolamine citrate was prepared by the microencapsulation technique and microcapsules thus formed were pressed into tablets. Dissolution tests were done with microcapsules and tablets formed by microcapsules by using the USPXXI paddle method and dissolution kinetics were studied and evaluated.
Hallucinations in children caused by oxolamine citrate
Med J Aust.1989 Apr 17;150(8):449-50, 452.PMID:2716683DOI: 10.5694/j.1326-5377.1989.tb136567.x.
Twenty reports in Australia, Belgium and The Netherlands have implicated oxolamine-citrate cough-mixtures as a cause of hallucinations in children of less than 10 years of age. Fever is not thought to be a likely alternative explanation. Similar reactions in older children and adults have not been reported and it is possible that the recommended doses for young children are too high. Information about the use of the drug in Australia suggests that such reactions are uncommon, but the information should be interpreted cautiously.
Recent Advancement in Synthesis and Bioactivities of 1,3,4-Oxadiazole
Curr Org Synth.2022 Nov 29.PMID:36453511DOI: 10.2174/1570179420666221129153933.
Derivatives of 1,3,4-oxadiazole are effective in the treatment and cure of a wide range of diseases in medical chemistry, while industrial development has shown that they can be utilised as corrosion inhibitors and light-emitting diodes. The researchers discovered several promising synthetic strategies that created 1,3,4-oxadiazoles in extraordinarily high yields while using environmentally friendly methods. These compounds can potentially be used in a wide range of life-changing applications. Stable isomeric oxadiazole forms of pleconaril, raltegravir, butalamine, fasiplon, oxolamine, and several other drugs are among the numerous potent and effective pharmaceuticals that are now on the market. Fasiplon, butalamine, raltegravir, and pleconaril treat HIV/AIDS patients. This article has attempted to bring attention to the chemistry and pharmacology of oxadiazole and its derivatives. Oxadiazole derivatives have been used extensively as prospective therapeutic agents in clinical research, and this has become standard practice. The use of biological and in-silico models has enabled scientists to identify more synthetic analogues of cancer prevention, antifungal, and anti-HIV medications. This article provides recent information regarding procedures synthesizing 1,3,4-oxadiazoles and their biological actions on the body.
Pharmacological properties of 3-phenyl-5beta diethylaminoethyl-1,2,4-oxadiazole
Br J Pharmacol Chemother.1961 Jun;16(3):209-17.PMID:19108149DOI: 10.1111/j.1476-5381.1961.tb01080.x.
The general pharmacological properties of Oxolamine (3-phenyl-5beta-diethylaminoethyl-1,2,4-oxadiazole) are described. The antitussive activity of this drug is more apparent in tests involving a diffuse stimulation of the bronchial tree than with electrical stimulation of the superior laryngeal nerve. These results suggest a predominantly peripheral mechanism of action. Oxolamine also possesses analgesic-anti-inflammatory, local anaesthetic and antispasmodic properties. The acute and chronic toxicities of Oxolamine are low, and the experimental results indicate the absence of side effects. The possibility that the antitussive activity is related to the other pharmacological properties is discussed.
Screening of differentially expressed genes and small molecule drugs of pediatric allergic asthma with DNA microarray
Eur Rev Med Pharmacol Sci.2012 Dec;16(14):1961-6.PMID:23242723
Background: Asthma is a disease resulting from a complex interaction of multiple genetic and environmental factors. More than 200 asthma candidate genes have been identified in the past decades by using genetic association studies, positional cloning and knockout mouse approaches. Aim: This study was to identify differentially expressed genes and provide direction for medicine design related to pediatric allergic asthma with DNA microarray. Materials and methods: The gene expression profile of pediatric allergic asthma GSE18965 was downloaded from Gene Expression Omnibus database which includes 16 samples, 7 normal and 9 pediatric allergic asthma samples. The differentially expressed genes between normal and disease samples were identified by using R language. The co-expression coefficient was calculated among the differentially expressed genes to construct co-expression networks with String Software. Software DAVID and FuncAssociate were used to analyze the functions of genes in the co-expression networks. Results: A total of 133 genes were identified as differentially expressed genes between normal and disease samples, and 8 related small medicine molecules were also obtained (penbutolol, felbinac, iodixanol, josamycin, oxolamine, 3-nitropropionic acid, scriptaid, and sanguinarine) from database CMAP. The differentially expressed genes were enriched in several biological processes, in which viral transcription and lysosome were the most significant GO term of up- or down-regulated genes. Conclusions: Our present findings shed new light on the molecular mechanism of allergic asthma and provide three small molecular medicines (3-nitropropionic acid, scriptaid, and sanguinarine) which have the potential to use in clinic for treatment of allergic asthma in future.