Applications of Ternatusine A in preparing monoamine oxidase MAO inhibitor

A monoamine oxidase and inhibitor technology, which is applied in the application field of Ternatusine A in the preparation of monoamine oxidase MAO inhibitors, can solve problems such as limited application, and achieve the effect of strong inhibitory activity and outstanding substantive characteristics.

Inactive Publication Date: 2017-03-15
ZIBO DINGLI PATENT INFORMATION CONSULTING CO LTD
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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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  • Applications of Ternatusine A in preparing monoamine oxidase MAO inhibitor
  • Applications of Ternatusine A in preparing monoamine oxidase MAO inhibitor
  • Applications of Ternatusine A in preparing monoamine oxidase MAO inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0013] Take 5 grams of compound Ternatusine A and add 195 grams of dextrin, mix well, and make 1000 tablets with a conventional tablet machine.

Embodiment 2

[0014] Embodiment 2: the preparation of the compound Ternatusine A capsule involved in the present invention:

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

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

[0017] Compound Ternatusine 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, 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°C for 12h, and then tested with a fully f...

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Abstract

The invention provides applications of Ternatusine A in preparing a monoamine oxidase (MAO) inhibitor. Compared with conventional monoamine oxidase inhibitors, the inhibitory activity of the monoamine oxidase (MAO) inhibitor, and the selectivity of the monoamine oxidase (MAO) inhibitor on MAO-A and MAO-B are increased greatly. The applications of Ternatusine A in preparing the monoamine oxidase (MAO) inhibitor are disclosed for the first time, the skeleton type of the monoamine oxidase (MAO) inhibitor is new, inhibition activity of the monoamine oxidase (MAO) inhibitor on monoamine oxidase is unexpectedly high, no revelation is provided by other compounds, prominent substantive features are achieved, and obvious progress is achieved when the monoamine oxidase (MAO) inhibitor is used for treating monoamine oxidase disorder related diseases.

Description

technical field [0001] The present invention relates to a new application of compound Ternatusine A, in particular to the application of Ternatusine 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 Ternatusine A involved in the present invention is a compound published in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/407A61P43/00
CPCA61K31/407
Inventor 田丽华
Owner ZIBO DINGLI PATENT INFORMATION CONSULTING CO LTD
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