Application of chromane compound HEF-05 in relaxing smooth muscle of blood vessel

A technology of HEF-05 and vascular smooth muscle, applied in cardiovascular system diseases, drug combinations, medical preparations containing active ingredients, etc.

Inactive Publication Date: 2010-09-15
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far there is no report about the effect of HEF-05 on relaxing vascular smooth muscle. The applicant found for the first time that the compound has the effect of relaxing vascular smooth muscle through various experimental screenings.

Method used

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  • Application of chromane compound HEF-05 in relaxing smooth muscle of blood vessel
  • Application of chromane compound HEF-05 in relaxing smooth muscle of blood vessel
  • Application of chromane compound HEF-05 in relaxing smooth muscle of blood vessel

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Effect test

Embodiment 1

[0024] Embodiment 1: in vitro experiment

[0025] 1.1 Preparation of experimental specimens

[0026] Rabbits, both male and female, after the animal is stunned, the thoracic aorta strips are quickly stripped to make a ring-shaped specimen with a width of 3-5mm, and the specimen is placed in a bath tube filled with 10ml of nutrient solution, and one end is fixed on the ventilation hook , and the other end is connected to the tension transducer, and the tension change is recorded by the recorder. The temperature in the bath tube is maintained at 37±0.5° C., and a mixed gas (95% O2+5% CO2) is introduced at a rate of 1 to 2 bubbles per second. The initial load of the specimen is 1g, the nutrient solution is changed every 20 minutes, and the balance is 1 hour, and the experiment is started after the baseline is stable

[0027] 1.2 Effect of HEF-05 on the tension of isolated rabbit vascular smooth muscle induced by spasmogens

[0028] After the tension of the specimen is stable, ...

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Abstract

The invention relates to the technical field of medicament, and mainly relates to application of chromane compound HEF-05 in preparing a vasodilator, a potassium channel opener, a calcium channel blocker and an endothelium relaxing factor releasing agent. In an animal in-vitro experiment, HEF-05 can relax the contraction of the smooth muscle of the blood vessel of rabbits caused by barium chloride, norepinephrine and potassium chloride. In addition, in a pilot study of a relaxing mechanism, the relaxation function of the HEF-05 is inhibited after the smooth muscle of the blood vessel is incubated by the ATP-sensitive potassium channel blocker glibenclamide. After methyleneblue is added to incubate, the relaxation function of the HEF-05 can be enhanced; and after the HEF-05 is added to incubate, the dose-response curve of the calcium chloride is descended. Therefore, the HEF-05 can be used for preparing a preparation for relaxing the smooth muscle of the blood vessel and can be used as the potassium channel opener, the calcium channel blocker and the endothelium relaxing factor releasing agent.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to the use of a chroman compound HEF-05 for relaxing vascular smooth muscle. Background technique [0002] In recent years, the research on antihypertensive drugs has developed rapidly, especially the advent of new antihypertensive drugs such as β-blockers, calcium antagonists and angiotensin converting enzyme inhibitors, which has fundamentally changed the treatment of hypertension. The incidence of hypertension is high, which can cause damage to target organs, serious complications such as stroke, angina pectoris, myocardial infarction, heart failure, renal failure, etc. At present, all kinds of antihypertensive drugs have different degrees of adverse reactions, so , if a kind of antihypertensive drug with strong selectivity and less adverse reactions can be found, the application prospect will be better. [0003] The chemical name of the chroman compound HEF-05 is 7-[2-(diethylam...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/353A61P9/12A61P9/10A61P13/12
Inventor 付守廷胡春李建婷兰惠瑜
Owner SHENYANG PHARMA UNIVERSITY
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