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Use of estrone derivative EA204 in preparing vascular smooth muscle relaxant

A technology of vascular smooth muscle, EA204, applied in the field of medicine

Inactive Publication Date: 2007-06-27
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there has been no report about the effect of EA-204 on relaxing vascular smooth muscle. After various experimental screenings, the applicant discovered for the first time that the compound has a relaxing effect on vascular smooth muscle.

Method used

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  • Use of estrone derivative EA204 in preparing vascular smooth muscle relaxant
  • Use of estrone derivative EA204 in preparing vascular smooth muscle relaxant
  • Use of estrone derivative EA204 in preparing vascular smooth muscle relaxant

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0011] 1. Experimental materials

[0012] 1. Animals:

[0013] Kunming mice, both male and female, weighing 18-22 g, were provided by the Experimental Animal Center of Shenyang Pharmaceutical University.

[0014] New Zealand rabbits, both male and female, weighing 2.0-2.5kg, were provided by the Experimental Animal Center of Shenyang Pharmaceutical University.

[0015] 2. Instrument:

[0016] 1) HSS-1(B) constant temperature bath Chengdu Instrument Factory

[0017] 2) RM6240B multi-channel physiological signal acquisition and processing system Chengdu Instrument Factory

[0018] 3) JZJ01 Muscle Tension Transducer Chengdu Instrument Factory

[0019] 4) TG-328A electro-optical analytical balance Shanghai balance instrument factory

[0020] 5) T-500 Electronic Balance Changshu Shuangjie Testing Instrument Factory

[0021] 6) Medical oxygen supply (95% O 2 +5%CO 2 ) Jizhou Fuli Medical Devices Factory, Hebei Province

[0022] 7) Micropipette Type IIIWKY 50-250μl Reagent o...

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PUM

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Abstract

The present invention relates to medicine technology, and is especially the application of estrone derivative EA204 in preparing medicine for treating vascular smooth muscle spasm disease. In in vitro animal experiment, estrone derivative EA204 can relax rabbit's in vitro descending aorta contracted with adrenalin, noradrenalin, barium chloride or potassium chloride. Estrone derivative EA204 may be used in preparing medicine for treating hypertension, coronary atherosclerosis, cerebral vascular spasm disease, etc.

Description

[0001] The invention relates to the technical field of medicine, and relates to the use of estrone derivative EA204 for preparing a vascular smooth muscle relaxant. Background technique [0002] The chemical system name of EA-204 is 3-(2-piperidin-1-yl)-ethoxy-estro-1,3,5(10)-triene-17-one (3-(2-piperidin -1-y1)-ethoxy-estra-1,3,5(10)-trien-17-one), this compound was successfully synthesized by Cooperwood, John S. et al. in 2004, and its anticancer activity was tested inspection. The results show that the compound has strong anticancer activity (Patent No. US 2005182038). So far, there has been no report about the effect of EA-204 on relaxing vascular smooth muscle. After various experimental screenings, the applicant discovered for the first time that the compound has a relaxing effect on vascular smooth muscle. [0003] Contents of the invention [0004] The invention provides the use of estrone derivative EA204 in the preparation of a vascular smooth muscle relaxant....

Claims

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Application Information

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IPC IPC(8): A61K31/565A61P21/02A61P9/00
Inventor 付守廷李娟陈国良
Owner SHENYANG PHARMA UNIVERSITY
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