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Monoamine oxidase (MAO) inhibitor and application thereof

A technology of monoamine oxidase and inhibitors, applied in the field of medicine, to achieve the effect of highlighting substantive characteristics and strong inhibitory activity

Inactive Publication Date: 2015-12-02
NANJING HUAKUANG INFORMATION CONSULTING CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But because "cheesereaction" causes high blood pressure, its application is limited

Method used

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  • Monoamine oxidase (MAO) inhibitor and application thereof
  • Monoamine oxidase (MAO) inhibitor and application thereof
  • Monoamine oxidase (MAO) inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Embodiment 1: the preparation of the compound Spirostane-typeglycoside tablet involved in the present invention:

[0014] Take 5 grams of the compound Spirostane-typeglycoside, add 195 grams of dextrin, mix well, and routinely press it into 1000 tablets.

Embodiment 2

[0015] Embodiment 2: the preparation of compound Spirostane-typeglycoside capsules involved in the present invention:

[0016] Take 5 grams of the compound Spirostane-typeglycoside, add 195 grams of starch, mix well, and make 1000 capsules.

[0017] The following pharmacodynamic experiments will further illustrate its drug activity.

[0018] The compound Spirostane-typeglycoside was tested for its inhibitory activity on MAO-A and MAO-B by fluorescent probe method,

[0019] The method is carried out according to the following steps: the sample to be tested is dissolved in DMSO to form a series of samples with concentration gradients. 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), inhibitor final concentration 0~10 -2 mmol / l, the mixture was then reacted in a water bath at 30±5°C for 12 hours, and d...

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PUM

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Abstract

The invention belongs to the field of medicine, and particularly provides a monoamine oxidase (MAO) inhibitor and application thereof. The MAO inhibitor is composed of a compound Spirostane-type glycoside and excipients. Compared with existing MAO inhibitors, the MAO inhibitor has the advantages that both inhibiting activity and selectivity to MAO-A and MAO-B are improved greatly, application of Spirostane-type glycoside in preparating the MAO inhibitor is disclosed for the first time, and Spirostane-type glycoside is high in inhibiting activity to MAO, has protruding substantive characteristics and has remarkable progress obviously when being used for treating diseases related to MAO disorder.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a monoamine oxidase MAO inhibitor and application thereof. 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 Spirostane-typeglycoside involved in the present invention is a new compound published in 2013 (GaoussouTimité, et al., Str...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61P31/06C07J71/00
Inventor 李洋
Owner NANJING HUAKUANG INFORMATION CONSULTING CENT
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