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Application of spirooliganones B in preparation of monoamine oxidase (MAO) inhibitor

A monoamine oxidase and inhibitor technology, applied in the application field of preparing 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: 2015-06-17
淮安市雨秀食品有限公司
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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 spirooliganones B in preparation of monoamine oxidase (MAO) inhibitor
  • Application of spirooliganones B in preparation of monoamine oxidase (MAO) inhibitor
  • Application of spirooliganones B in preparation of monoamine oxidase (MAO) inhibitor

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Effect test

Embodiment 1

[0011] Embodiment 1: the preparation of compound Spirooliganones B tablet involved in the present invention:

[0012] Take 5 grams of compound Spirooliganones B, add 195 grams of dextrin, mix well, and conventionally press it into 1000 tablets.

Embodiment 2

[0013] Embodiment 2: the preparation of compound Spirooliganones B capsules involved in the present invention:

[0014] Take 5 grams of compound Spirooliganones B, add 195 grams of starch, mix well, and pack into capsules to make 1000 capsules.

[0015] The following pharmacodynamic experiments will further illustrate its drug activity.

[0016] Compound Spirooliganones B 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:

[0017] 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 ...

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Abstract

The invention provides the application of spirooliganones B in preparation of a monoamine oxidase (MAO) inhibitor. Compared with an existing MAO inhibitor, the spirooliganones B has the advantages that the inhibitory activity and the selectivity to MAO-A and MAO-B are improved greatly. The application of the spirooliganones B in preparation of the MAO inhibitor is disclosed for the first time. The spirooliganones B has the advantages of being high in inhibitory activity for the MAO and prominent in substantive features, and makes remarkable progress in treatment of diseases related to disorder of the MAO.

Description

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

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352
Inventor 严建山
Owner 淮安市雨秀食品有限公司
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