Application of Aphanamixoid A to preparation of monoamine oxidase (MAO) inhibitor

A technology of aphanamixoida, 1.aphanamixoida, which is applied in the field of application of Aphanamixoid A in MAO inhibitors, can solve problems such as limited application, and achieve the effect of strong inhibitory activity and outstanding substantive characteristics

Inactive Publication Date: 2013-05-29
吴俊华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

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

Method used

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  • Application of Aphanamixoid A to preparation of monoamine oxidase (MAO) inhibitor
  • Application of Aphanamixoid A to preparation of monoamine oxidase (MAO) inhibitor
  • Application of Aphanamixoid A to preparation of monoamine oxidase (MAO) inhibitor

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Embodiment 1

[0013] Embodiment 1: the preparation of compound AphanamixoidA tablet involved in the present invention:

[0014] Get 20 grams of compound Aphanamixoid A, add 180 grams of conventional excipients for tablet preparation, mix well, and make 1000 tablets with a conventional tablet press.

Embodiment 2

[0015] Embodiment 2: the preparation of compound AphanamixoidA capsules involved in the present invention:

[0016] Get 20 grams of compound Aphanamixoid A, add conventional auxiliary materials for preparing capsules such as 180 grams of starch, mix well, and pack into capsules to make 1000 tablets.

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

[0018] Compound AphanamixoidA 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:

[0019] 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), final inhibitor concentration 0~10 -2 mmol / l, the mixture was the...

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Abstract

The invention provides an application of Aphanamixoid A to the preparation of a monoamine oxidase (MAO) inhibitor. Compared with the existing MAO inhibitor, the MAO inhibitor provided by the invention is greatly improved on the aspects of inhibitory activity and selectivity to MAO-A and MAO-B. The application of the Aphanamixoid A to the preparation of the MAO inhibitor, related by the invention, is disclosed for the first time; a framework type of the Aphanamixoid A is brand new, and Aphanamixoid A has unexpected strong inhibitory activity to MAO, so that no possibility that any revelation is given by other compounds exists, and Aphanamixoid A has remarkable substantive features and is also remarkably improved on the aspect of treating MAO imbalance related diseases.

Description

technical field [0001] The present invention relates to the application of Aphanamixoid 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 "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 Aphanamixoid A involved in the present invention is a new skeleton compound published in 2012 (Cai, J.Y.etal., 2012. Aphanamixoid A, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P43/00
Inventor 冯怡龚霞李丽丽吴俊华
Owner 吴俊华
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