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Use of CD38 enzyme inhibitor in treating bronchial hyperresponsiveness diseases

A technology of airway hyperresponsiveness and inhibitors, which is applied in the direction of respiratory diseases, organic active ingredients, and medical preparations containing active ingredients, etc., and can solve problems such as complicated operation, long modeling time, and low success rate

Active Publication Date: 2014-03-26
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, researchers use more airway hyperresponse models as ovalbumin (OVA)-sensitized mouse and mouse models, but the disadvantages of this modeling method are long modeling time, low success rate and complicated operation

Method used

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  • Use of CD38 enzyme inhibitor in treating bronchial hyperresponsiveness diseases
  • Use of CD38 enzyme inhibitor in treating bronchial hyperresponsiveness diseases
  • Use of CD38 enzyme inhibitor in treating bronchial hyperresponsiveness diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Physicochemical properties of compound T[5-(3-phenylpropionylamino)-N-(4-ethoxycarbonylphenyl)-1H-3-indolecarboxamide]

[0030] The structural formula of compound T is as figure 1 As shown, the molecular weight is 455.51, light yellow-white powder, melting point 192-194°C, soluble in DMF and acetone, slightly soluble in methanol and dichloromethane, insoluble in water, and decomposes in the presence of strong acid and strong alkali. Its solubility and acid-base stability can be proved by the following experiments.

[0031] 1. Solubility test

[0032] Purpose: To test the solubility of compound T in different solvents

[0033] Principle: At 20°C, the amount of dissolved solvent in 100g of solvent is 1-10g is soluble, 0.01g-1g is slightly soluble, and less than 0.01g is insoluble. Add a certain amount of solvent to the quantitative sample and observe the dissolution.

[0034] Method: Take 2mg sample, add solvent and shake, clear and transparent without soli...

Embodiment 2

[0045] Example 2: Pharmacodynamic evaluation of two CD38 enzyme inhibitors in mouse airway hyperresponsive disease model

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Abstract

The invention relates to a medicament for treating bronchial hyperresponsiveness diseases, which is 5-(3-phenyl propionyl amino)-N-(4-carbethoxy phenyl)-1H-3-indole formamide. The medicament is a CD38 enzyme inhibitor which can relax tracheal smooth muscles by inhibiting Ca<2+> release, so that bronchial hyperresponsiveness diseases can be treated in a symptomatic manner; a mouse airway hyperresponsiveness model is manufactured by utilizing ozone, and meanwhile, an emulsifier of the medicament is given for gavage treatment, so that airway resistance of the mouse treated by the medicament is obviously lowered, dynamic lung compliance is obviously increased, and lung lesion degree is relieved; besides, the experiment finds that the medicament further has anti-inflammatory effect, anti-oxidization effect, no obvious toxic and side effect, has good development value, and belongs to the field of medicaments.

Description

Technical field: [0001] The invention relates to a medicine for treating airway hyperresponsive diseases, 5-(3-phenylpropionylamino)-N-(4-ethoxycarbonylphenyl)-1H-3-indolecarboxamide. The drug is a CD38 enzyme inhibitor, which mainly achieves the therapeutic purpose by dilating tracheal smooth muscle, and has anti-inflammation and anti-oxidation effects, and belongs to the field of drugs. Background technique: [0002] Airway hyperresponsiveness refers to the excessive response of the trachea and bronchi to various stimuli, including specific antigenic stimuli and non-specific stimuli, such as physical and chemical stimuli, which is an important feature that distinguishes patients with bronchial asthma from normal people [1] . Although the inducing factors of airway hyperresponsiveness are various, and the therapeutic effects of various drugs are different, and the research on new therapies is also multi-directional, but basically from anti-inflammatory, antihistamine, alle...

Claims

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Application Information

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IPC IPC(8): A61K31/404A61P11/00
Inventor 蒲小平张亮仁邓政朱志鹏
Owner PEKING UNIV
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