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Application of chromane compound HEF-04 in relaxing blood vessel smooth muscle

A technology of vascular smooth muscle and HEF-04, applied in the field of medicine

Inactive Publication Date: 2010-01-06
SHENYANG PHARMA UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The chemical name of the chroman compound HEF-04 is 7-[2-(4-morpholinyl)ethoxy]chroman hydrochloride (7-[2-(4-morpholinyl)ethoxy]chroman hydrochloride), is The drug was first synthesized by the research group of Professor Hu Chun from the Organic Chemistry Laboratory of Shenyang Pharmaceutical University, and the anti-platelet aggregation activity has been preliminarily investigated. The results show that the compound has a strong anti-platelet aggregation activity, but so far no relevant HEF -04 The report on the effect of relaxing vascular smooth muscle, the applicant found for the first time that the compound has the effect of relaxing vascular smooth muscle after various experimental screenings

Method used

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  • Application of chromane compound HEF-04 in relaxing blood vessel smooth muscle
  • Application of chromane compound HEF-04 in relaxing blood vessel smooth muscle
  • Application of chromane compound HEF-04 in relaxing blood vessel smooth muscle

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Experimental program
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Effect test

Embodiment 1

[0025] Embodiment 1: in vitro experiment

[0026] 1.1 Effects of HEF-O4 on the tension of isolated rabbit vascular smooth muscle induced by spasmodic agents

[0027] After the tension of the specimen is stable, adjust the baseline to zero, record a section of waveform, add spasmodic agent (barium chloride 2mg / ml, potassium chloride 60mmol / L) into the bath tube to induce contraction, and when the maximum contraction is reached, fully wash After the samples were recovered and stabilized, the same concentration of spasmodic agent was used to induce the second contraction. When the contraction was basically the same as the previous contraction, HEF-04 was added cumulatively (10 -5 mol / L~3*10 -3 mol / L). Record the data so that the maximum contraction range of the convulsant is 100%, the relaxation percentage is the ordinate, and the logarithmic concentration of HEF-04 is the abscissa to draw the relaxation dose-effect curve, and the data are represented by mean ± standard error a...

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Abstract

The invention relates to the technical field of medicine and provides an application of chromane compound HEF-04 in relaxing blood vessel smooth muscle. In animal in vitro experiment, HEF-04 can relax rabbit in vitro blood vessel smooth muscle shrunk by barium chloride and potassium chloride; the vasodilation effect of chromane compound HEF-04 is not inhibited by the incubation of methylene blue, on the contrary, the blood vessel dose-effect curve shifts left due to higher level of potassium in spasm-induced agent; EC50 value has significant difference before and after the incubation. Documents report that the existence of NO and PGI2 can weaken the generation of EDHF; after NO and PGI2 are inhibited, the effect of endothelium-dependent vascular relaxation caused by EDHF is more prominent, showing that the vascular relaxation effect of HEF-04 is possibly related to the increase of EDHF releasing or caused by the interactions of vascular endothelium relaxing factors.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to the use of a chroman compound HEF-04 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-04 is 7-[2-(4-morphol...

Claims

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Application Information

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IPC IPC(8): A61K31/5377A61P9/12A61P9/10A61P9/04A61P13/12
Inventor 付守廷胡春王冰兰惠瑜
Owner SHENYANG PHARMA UNIVERSITY
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