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Application of Kadcoccitones A in preparing monoamine oxidase (MAO) inhibitor

A monoamine oxidase and inhibitor technology, applied in the application field of Kadcoccitones A in the preparation of monoamine oxidase MAO inhibitors, can solve problems such as limited application, and achieve the effect of highlighting substantial characteristics

Inactive Publication Date: 2013-12-25
NANJING ZHENGLIANG MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its application is limited because of the high blood pressure caused by "cheese reaction"

Method used

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  • Application of Kadcoccitones A in preparing monoamine oxidase (MAO) inhibitor
  • Application of Kadcoccitones A in preparing monoamine oxidase (MAO) inhibitor
  • Application of Kadcoccitones A in preparing monoamine oxidase (MAO) inhibitor

Examples

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Effect test

Embodiment 1

[0012] Embodiment 1: the preparation of compound Kadcoccitones A tablet involved in the present invention:

[0013] Take 5 grams of compound Kadcoccitones A, add 195 grams of dextrin, mix well, and conventionally press it into 1000 tablets.

Embodiment 2

[0014] Embodiment 2: the preparation of compound Kadcoccitones A capsules involved in the present invention:

[0015] Get 5 grams of compound Kadcoccitones A, add 195 grams of starch, mix well, and pack into capsules to make 1000 capsules.

[0016] The following pharmacodynamic experiments will further illustrate its drug activity.

[0017] The compound Kadcoccitones A detects the inhibitory activity to MAO-A and MAO-B with the method of fluorescent probe, and described method is carried out according to the following steps:

[0018] Dissolve the sample to be tested in DMSO to prepare a series of samples with concentration gradient. Take 4ul of MAO (10mg / ml), boric acid buffer (PH=8.4), 50ul of BSA (50mg / ml), add the sample solution to be tested, mix well, react in a water bath at 30-38°C for 3h, and then add probe 7 -(3-Aminopropoxy)coumarin 2ul (50mmol / ml), the final concentration of the inhibitor is 0~10-2mmol / l, and the mixture is reacted in a water bath at 30±5℃ for 12h...

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Abstract

The invention provides application of Kadcoccitones A in preparing a monoamine oxidase (MAO) inhibitor. Compared with the existing MAO inhibitor, the Kadcoccitones A has greatly higher activity and selectivity for MAO-A and MAO-B. The application of the Kadcoccitones A in preparing the MAO inhibitor is disclosed for the first time; and the Kadcoccitones A has high activity for inhibiting MAO, has the characteristic of outstanding materiality, and apparently has marked progresses when being used for treating MAO maladjustment related diseases.

Description

technical field [0001] The present invention relates to a new application of compound Kadcoccitones A, in particular to the application of Kadcoccitones A in the preparation of monoamine oxidase MAO inhibitors. Background technique [0002] Since the anti-tuberculosis drug isoniazid was found to be a potential MAO inhibitor, research on MAO inhibitors has become a hot topic. Iproniazid became the first MAO inhibitor, because it was discovered that this kind of MAO inhibitor containing hydrazine structure can also inactivate P450s and cause liver toxicity; and studied the non-hydrazine MAO inhibition represented by tranylcypromine Agents, this category can be called the second generation. But because "cheese reaction" causes high blood pressure, its application is limited. Therefore, it is quite necessary and urgent to develop a newer and more efficient monoamine oxidase inhibitor. [0003] The compound Kadcoccitones A involved in the present invention is a 2012 publicatio...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61P43/00
Inventor 不公告发明人
Owner NANJING ZHENGLIANG MEDICAL TECH
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