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Application of lathyranone A to 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: 2018-04-03
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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  • Application of lathyranone A to preparation of monoamine oxidase (MAO) inhibitor
  • Application of lathyranone A to preparation of monoamine oxidase (MAO) inhibitor
  • Application of lathyranone A to preparation of monoamine oxidase (MAO) inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1: Preparation of Lathyranone A. Tablets:

[0016] Take 5 grams of compound Lathyranone A. Add 195 grams of dextrin, mix well, and make 1000 tablets with a conventional tablet machine.

Embodiment 2

[0017] Example 2: Preparation of Lathyranone A. Capsules, the compound involved in the present invention:

[0018] Take 5 grams of compound Lathyranone A. Add 195 grams of starch, mix well, and encapsulate it to make 1000 tablets.

[0019] The following pharmacodynamic experiments will further illustrate its drug activity.

[0020] Compound Lathyranone A. The inhibitory activity of MAO-A and MAO-B was detected by fluorescent probe method, and the method was carried out according to the following steps:

[0021] Dissolve the sample to be tested in DMSO to prepare a series of samples with a concentration gradient. Take 4ul of MAO (10mg / ml), boric acid buffer (PH=8.4), 50ul BSA (50mg / ml), add the sample solution to be tested, mix well, react in a water bath at 30~38℃ for 3h, then add probe 7 -(3-Aminopropoxy) coumarin 2ul (50mmol / ml), the final concentration of inhibitor is 0~10-2mmol / l, and the mixture is reacted in a water bath at 30±5℃ for 12h, using a full-function fluorescence spec...

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PUM

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Abstract

The invention provides the application of Lathyranone A. in the preparation of monoamine oxidase (MAO) inhibitors. Compared with the existing monoamine oxidase inhibitors, its inhibitory activity and selectivity to MAO‑A and MAO‑B are greatly improved. The use of Lathyranone A. involved in the present invention in the preparation of monoamine oxidase (MAO) inhibitors is disclosed for the first time. Since the skeleton type belongs to a new skeleton type, and its inhibitory activity against monoamine oxidase is unexpectedly strong, there is no inspiration from other compounds It is possible, has outstanding substantive features, and at the same time, it is obviously a significant progress in the treatment of diseases related to monoamine oxidase disorders.

Description

Technical field [0001] The present invention relates to a new use of the compound Lathyranone A., in particular to the application of Lathyranone A. in the preparation of monoamine oxidase MAO inhibitors. Background technique [0002] Since the discovery of the anti-tuberculosis drug Isoniazid as a potential MAO inhibitor, the research on MAO inhibitors has become a hot spot. Isonicotinic hydrazide became the first MAO inhibitor, because it was discovered that this type of MAO inhibitor containing a hydrazine structure can also inactivate P450s and cause liver toxicity; also studied non-hydrazine MAO inhibition represented by tranylcypromine Agents, this type can be called the second generation. But because the "cheese reaction" triggers 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 Lathyranone A. involved in the present invention is a novel pub...

Claims

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Application Information

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IPC IPC(8): A61K31/235A61K9/48A61K9/20A61P43/00
CPCA61K31/235A61K9/2059A61K9/4866
Inventor 田丽华
Owner ZIBO DINGLI PATENT INFORMATION CONSULTING CO LTD
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