Application of Norsampsone B in preparing MAO (monoamine oxidase) inhibitor

A technology of monoamine oxidase and inhibitor, which is applied in the application field of preparing monoamine oxidase MAO inhibitor, and achieves the effect of outstanding substantive characteristics

Inactive Publication Date: 2016-03-23
ZIBO DINGLI PATENT INFORMATION CONSULTING CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But because "cheesereaction" causes high

Method used

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  • Application of Norsampsone B in preparing MAO (monoamine oxidase) inhibitor
  • Application of Norsampsone B in preparing MAO (monoamine oxidase) inhibitor
  • Application of Norsampsone B in preparing MAO (monoamine oxidase) inhibitor

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Effect test

Embodiment 1

[0014] Embodiment 1: the preparation of compound Norsampsone B tablet involved in the present invention:

[0015] Take 5 grams of compound Norsampsone B and add 195 grams of dextrin, mix well, and conventionally press it into 1000 tablets.

Embodiment 2

[0016] Embodiment 2: the preparation of the compound Norsampsone B capsule involved in the present invention:

[0017] Take 5 grams of compound Norsampsone B, add 195 grams of starch, mix well, and pack into capsules to make 1000 capsules.

[0018] The following pharmacodynamic experiments will further illustrate its drug activity.

[0019] The compound NorsampsoneB 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:

[0020] 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, the mixture is then reacted in a water bath at 30±5°C for 12h, and...

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Abstract

The invention provides application of Norsampsone B in preparing a MAO (monoamine oxidase) inhibitor, compared with the existing MAO inhibitor, the inhibitory activity and the selectivity of MAO-A and MAO-B of the Norsampsone B are greatly improved. The application of the Norsampsone B in preparing the MAO inhibitor is disclosed for the first time, and the inhibitory activity to the MAO is high, the Norsampsone B has outstanding substantive features, and obviously has remarkable improvement for treating diseases relevant to imbalance of the MAO at the same time.

Description

technical field [0001] The present invention relates to a new application of compound Norsampsone B, in particular to the application of Norsampsone B 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 "cheesereaction" 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 Norsampsone B involved in the present invention is a new compound published...

Claims

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Application Information

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IPC IPC(8): A61K31/122A61P43/00
CPCA61K31/122A61K9/2059A61K9/4866
Inventor 田丽华
Owner ZIBO DINGLI PATENT INFORMATION CONSULTING CO LTD
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