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Indanazoline Sale

(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。

Indanazoline Chemical Structure

Cas No.:40507-78-6

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1mg
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产品描述

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.

Chemical Properties

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
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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
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Research Update

[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.