Thonzylamine
(Synonyms: Neohetramine) 目录号 : GC25994Thonzylamine (Neohetramine) is an antihistamine and anticholinergic drug.
Cas No.:91-85-0
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
Thonzylamine (Neohetramine) is an antihistamine and anticholinergic drug.
| Cas No. | 91-85-0 | SDF | Download SDF |
| 别名 | Neohetramine | ||
| 分子式 | C16H22N4O | 分子量 | 286.37 |
| 溶解度 | DMSO: 57 mg/mL (199.04 mM);Water: 57 mg/mL (199.04 mM);Ethanol: 13 mg/mL (45.40 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 | 3.492 mL | 17.4599 mL | 34.9199 mL |
| 5 mM | 0.6984 mL | 3.492 mL | 6.984 mL |
| 10 mM | 0.3492 mL | 1.746 mL | 3.492 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。
Design, synthesis and biological activity of a novel ethylenediamine derivatives as H1 receptor antagonists
Bioorg Med Chem 2019 Dec 15;27(24):115127.PMID:31703894DOI:10.1016/j.bmc.2019.115127.
In this study, a series of novel ethylenediamine compounds were obtained by structural modification of the lead compounds with Thonzylamine, and using the principle of modifying by bioisostere formation and modification with alkyl groups. In vitro assay, the biological activities showed that the target compounds have good properties in inhibiting mast cell degranulation and releasing histamine and β-aminohexidase, such as the compounds 5c, 5g, 5k, 5l and 5o, especially of compound 5k to mast cell degranulation is IC50 = 0.0106 ± 0.001 μmol⋅L-1, histamine release was IC50 = 0.0192 ± 0.005 μmol⋅L-1 and β-hexosaminidase release was IC50 = 0.0455 ± 0.002 μmol⋅L-1in vitro. At the same time, in vivo biological activities assay results showed that have a good Histamie induce bronchospasm effect with relatively long duration and good protective effect in vivo, among which the protective effect of compound 5k was 79.74 ± 0.30%, compounds 5c, 5g, 5k, 5l and 5o could inhibit the capillary permeability of increasing which were caused by histamine.
Sensitive spectrofluorimetric and spectrophotometric methods for the determination of Thonzylamine hydrochloride in pharmaceutical preparations based on coupling with dimethylbarbituric acid in presence of dicyclohexylcarbodiimide
J Pharm Biomed Anal 2000 Mar;22(2):257-64.PMID:10719908DOI:10.1016/s0731-7085(99)00261-7.
Two sensitive and selective spectrophotometric and spectrofluoimetric procedures were developed for the determination of Thonzylamine hydrochloride (THAH) in tablets and nasal drops. The methods are based on König reaction which resulted in an orange-yellow fluorescent product. The orange-yellow product of the interaction between the dicyclohexylcarbodiimide (DCC), THAH and dimethylbarbituric acid (DMBA) showed an absorption maximum at 492 nm, a first-derivative signal at 494 nm and a fluorescence emission peak at 518 nm (lambda(ex)=492 nm). The orange-yellow color was found to be stable for at least 2 h. The reaction conditions were studied and optimized. The reaction obeys Beer's law over the ranges 8-20 and 0.2-2.0 microg ml(-1) for the derivative spectrophotometric and fluorimetric measurements, respectively. The detection limits were found to be 0.29 and 0.018 microg ml(-1) for the spectrophotometric and fluorimetric measurements, respectively. The proposed methods were applied to the analysis of pharmaceutical formulations containing THAH, either alone or in combination with naphazoline nitrate.
Carbon-13 magnetic resonance spectroscopy of drugs II: antihistamines
J Pharm Sci 1976 Jul;65(7):1019-23.PMID:8624DOI:10.1002/jps.2600650716.
The natural abundance carbon-13 magnetic resonance spectra of a series of antihistamines (pheniramine, chlorpheniramine, methapyrilene, tripelennamine, pyrilamine, and Thonzylamine) were detemined using the pulse Fourier transform technique. The chemical shifts were assigned with the aid of long-range carbon-13-hydrogen coupling constants.
[4-[Benzyl-(2-dimethylaminoethyl)amino]pyrimidine compounds with selective antagonistic activity against H1-histamine receptors]
Farmaco Sci 1984 Mar;39(3):189-99.PMID:6143687doi
This paper describes the synthesis of 2- and 4-[benzyl-(2-dimethylaminoethyl)amino]pyrimidine compounds and their antihistaminic properties studied on isolated guinea-pig ileum. Calculated pA2 values show that the antihistaminic activity of 4-[p.methoxybenzyl-(2-dimethylaminoethyl)amino]pyrimidine is specific and potent (8-10 times higher than that of Thonzylamine).