Indanazoline
(Synonyms: 印咪唑啉) 目录号 : GC34030
Indanazoline(Farate的一水盐酸盐活性物质)有着显著的血管收缩作用。
Cas No.:40507-78-6
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
Indanazoline (as monohydrochloride active substance of Farial) is characterized by a pronounced vasoconstrictive action.
In animal experiments the new imidazoline derivative indanazoline (as monohydrochloride active substance of Farial) is characterized by a pronounced vasoconstrictive action after local or intravenous application[1].
[1]. Kretzschmar R, et al. [Pharmacology of N-(2-imidazolin-2-yl)-N-(4-indanyl)amino (indanazoline), a new vasoconstrictive imidazoline compound]. Arzneimittelforschung. 1980;30(10):1746-60.
| Cas No. | 40507-78-6 | SDF | |
| 别名 | 印咪唑啉 | ||
| Canonical SMILES | C1(NC2=CC=CC3=C2CCC3)=NCCN1 | ||
| 分子式 | C12H15N3 | 分子量 | 201.27 |
| 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 | 4.9685 mL | 24.8423 mL | 49.6845 mL |
| 5 mM | 0.9937 mL | 4.9685 mL | 9.9369 mL |
| 10 mM | 0.4968 mL | 2.4842 mL | 4.9685 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。
[Synthesis of N-(2-imidazolin-2-yl)-N-(4-indanyl)amine (Indanazoline) (author's transl)]
Arzneimittelforschung 1980;30(10):1733-7.PMID:7192113doi
The synthesis of the new vasoconstrictive agent N-(2.3-Dihydro-1H-indan-4-yl)-2.5-dihydro-1H-imidazol-2-amine (Indanazoline, Farial) and the proof of its structure by spectroscopic methods is reported.
[On the decongesting effect of the novel imidazole derivative N-(2-imidazolin-2-yl)-N-(4-indanyl)amine (Indanazoline) (author's transl)]
Arzneimittelforschung 1980;30(10):1785-7.PMID:6159902doi
In 35 test persons with normal nasal condition the newly developed imidazole derivative 2-(2-imidazolin-2-yl)-N-(4-indanyl)amine hydrochloride (Indanazoline E-VA-16, active principle of Farial) was tested for its decongesting influence on nasal mucosa and for its tolerability using anterior rhinomanometric techniques and comparing the results with those of xylometazoline. 10 min after application of either drug the stream volume increased significantly thus evidencing decongestion of the nasal mucosa. There was no substantial difference between the two substances. 8 h after application the initial values were virtually reached again in both treated groups. Since Indanazoline showed little effect in conditions of minor respiratory resistance but was highly effective against increased initial respiratory resistance it is concluded that its therapeutic safety margin might be larger. The reactive hyperemia observed after both drugs should not be overvalued. Blood pressure and pulse rate were not appreciably influenced at any time. Both drugs were well tolerated.
[On the galenical development of a nose spray from N-(2-imidazolin-2-yl)-N-(4-indanyl)amine monohydrochloride (Indanazoline) (author's transl)]
Arzneimittelforschung 1980;30(10):1738-46.PMID:6159899doi
An account if given of the aim of the galenical development of the new remedy, indanazolin nose-spray. The description of the quality of the active ingredient N-(2-imidazolin-2-yl)-N-(4-indanyl)amine monohydrochloride (Indanazoline, Farial) and the dosage form allows a pharmaceutical evaluation. The descriptions of the organoleptic, physical and chemical properties of the active substance are given in detail. The formulation, the procedures for manufacturing, and the specifications for the packaging materials give some idea of the galenical aspects. The quality of the finished dosage form is defined by means of product specifications relating to the identity, purity, and potency, and is proved by suitably designed stability studies. Finally a detailed summary is made of the analytical methods which were used.
[Pharmacology of N-(2-imidazolin-2-yl)-N-(4-indanyl)amino (Indanazoline), a new vasoconstrictive imidazoline compound]
Arzneimittelforschung 1980;30(10):1746-60.PMID:7192114doi
In animal experiments the new imidazoline derivative N-(2-imidazolin-2-yl)-N-(4-indanyl)amine (Indanazoline, E-VA-16, as monohydrochloride active substance of Farial) is characterized by a pronounced vasoconstrictive action after local or intravenous application. This is due to a direct action of the compound on alpha-adrenergic receptors. When applied systemically E-VA-16 being a peripherally acting alpha-sympathomimetic induces a rise in blood pressure and a reduction of heart rate and exerts antiphlogistic, spasmolytic, hyperglycemic and diuretic actions. When given by the intranasal route the substance influences blood pressure and heart rate only at concentrations considerably higher than those intended for use in therapy. After enteral administration the effective doses also markedly exceed the single therapeutic doses. There was no evidence of side-effects restricting the use of the drug as compared to other imidazoline derivatives. Studies on the isolated perfused rabbit ear, however, indicated a broader therapeutic range in local application.
Nasal decongestion with imidazoline derivatives: acoustic rhinometry measurements
Eur J Clin Pharmacol 1999 Mar;55(1):7-12.PMID:10206078DOI:10.1007/s002280050585.
Objective: The objective of this single-blind study was to establish whether there are any differences between conventional imidazoline-containing nasal drops with regard to duration of action and decongestion potential. Methods: Six different substances were each administered to 108 healthy volunteers (nine groups of 12 adults), respectively, in the concentration recommended for adults (and two also in that recommended for infants) over a period of 8 h in comparison with 0.9% NaCl. The volumetric measurement of the nasal lumen was conducted by means of acoustic rhinometry (Rhinoklack). Results: The decongestive effect of all imidazoline preparations set in relatively uniformly, without any appreciable differences. After 20 min all the products exhibited approximately 60% of their maximum decongestive effect, which was achieved after approximately 40 min, having produced an increase in volume of approximately 20%. In contrast, in terms of duration of action, considerable differences between the individual products were to be discerned: Indanazoline 0.118%, naphazoline 0.02% and tetryzoline 0.1% had no effect whatsoever after 4 h. Oxymetazoline 0.05% and 0.01%, xylometazoline 0.025% and 0.1%, and tramazoline 0.1264% still had an appreciable effect after 4 h, while after 8 h only oxymetazoline 0.05% and 0.01% still had a relevant decongestive effect. A rebound effect associated with reactive hyperaemia was observed after 8 h in all short-acting products (Indanazoline, naphazoline, tetryzoline and tramazoline), which in the case of Indanazoline was even associated with a reduction in the nasal lumen. Interestingly, there were no differences between the xylometazoline and oxymetazoline concentrations recommended for adults and those for infants in terms of efficacy. The low-dose concentrations of the preparations for infants appear to be sufficient to produce a satisfactory therapeutic effect.