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New medical application of chromane compound HEF-05

A technology of HEF-05 and compounds, applied in the field of medicine

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

AI Technical Summary

Problems solved by technology

In addition, in the treatment of infants, there is no completely effective drug to treat intestinal spasms
There are currently no literature reports on this

Method used

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  • New medical application of chromane compound HEF-05
  • New medical application of chromane compound HEF-05
  • New medical application of chromane compound HEF-05

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Example 1: Synthesis of HEF-05

[0015] The chemical name of the chroman compound HEF-05 is 7-[2-(diethylamino)ethoxy]chroman hydrochloride, and its synthesis method is as follows:

[0016] Under stirring at room temperature, 66 mL of 70% perchloric acid solution was added dropwise to a suspension solution of 100 g of 2',4'-dihydroxyacetophenone and 580 mL of triethyl orthoformate. The color of the reaction solution gradually deepened to brownish red, and a large amount of heat was released. After the reaction solution was cooled to room temperature, 1750 mL of anhydrous diethyl ether was added, and a large amount of precipitates were formed immediately, filtered with suction, the filter cake was evaporated to dry diethyl ether, heated to 1000 mL of water and refluxed for 5 minutes, cooled, and a large amount of precipitates were precipitated, and stood overnight to obtain 31.5 g of a red crude product , recrystallized from 500 mL of ethanol to obtain 16.7 g of pale pi...

Embodiment 2

[0023] Example 2: Relaxation effect of HEF-05 on isolated small intestinal smooth muscle of rabbits

[0024] 1. Experimental materials

[0025] 1. Animals:

[0026] New Zealand rabbits, both male and female, weighing 2.0-2.5kg, provided by the Experimental Animal Center of Shenyang Pharmaceutical University, certificate number: Liaoshidongzi No. 033.

[0027] 2. Instrument:

[0028] HSS-1(B) constant temperature bath, RM6240B multi-channel physiological signal acquisition and processing system, JZJ01 muscle tension transducer, TG-328A electro-optical analytical balance, T-500 electronic balance, medical oxygen supply (95% O 2 +5%CO 2 ), micropipette IIIWKY type 50-250μl

[0029] 3. Drugs and reagents

[0030] Sodium Chloride (NaCl): Potassium Chloride (KCl), Magnesium Sulfate (MgSO 4 ·7H 2 O), sodium dihydrogen phosphate (NaH 2 PO 4 ), anhydrous calcium chloride (CaCl 2 ), sodium bicarbonate (NaHCO 3 ), glucose (Glucose), barium chloride (BaCl 2 ), Potassium dihydr...

Embodiment 3

[0043] Example 3: Mechanism and ATP-sensitivity K of HEF-05 on small intestinal smooth muscle relaxation + channel relationship

[0044] 1. Experimental materials

[0045] With embodiment 2.

[0046] 2. Experimental method

[0047] 1. Specimen preparation

[0048] With embodiment 2.

[0049] 2. Glibenclamide’s effect on HEF-05 diastolic BaCl 2 Effects of Contraction on Isolated Rabbit Small Intestinal Smooth Muscle

[0050] After the tension of the rabbit small intestine specimen is stable, adjust the baseline to zero, record a waveform, and add BaCl to the bath tube 2 (2mg / ml), after obtaining stable contraction, cumulatively add HEF-05 (10 -6 mol / L~10 -3 mol / L), get HEF-05 diastolic BaCl 2 The dose-effect curve of contraction; fully rinse the tissue, and after the specimen recovers its activity, add glibenclamide solution (10 -5 mol / L), incubated for 10 minutes to block ATP-sensitive K + channel, add BaCl to the bath tube again 2 (2mg / ml), after obtaining stable ...

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Abstract

The invention relates to the technical field of medicine, mainly relating to the applications of chromane compound HEF-05 in preparing intestinal canal smooth muscle spasmolytic and in serving as potassium ion channel opener; the invention further comprises a preparation method of the inspected object HEF-05 in the invention. In animal in vitro experiment, HEF-05 can not only relax the amplitude and the tension of spontaneous activities of rabbit in vitro intestinal canal smooth muscle, but also relax the shrinkage of small intestine smooth muscle caused by acetylcholine chloride, barium chloride and potassium chloride. In addition, preliminary study on the relaxation mechanism of chromane compound HEF-05 proves that the relaxation effect of chromane compound HEF-05 is inhibited after the small intestine smooth muscle is incubated by ATP-sensitive potassium channel blocking agent Glibenclamide, therefore, HEF-05 can be used for preparing spasmolytic which is used for treating intestinal canal smooth muscle spasm, and can also be served as potassium ion channel opener.

Description

technical field [0001] The invention relates to the technical field of medicine, mainly relates to the new medical application of chroman compound HEF-05, in particular to the use of the chroman compound HEF-05 in preparing an antispasmodic agent for intestinal smooth muscle and as a potassium ion channel opener. Background technique [0002] Intestinal spasm is paroxysmal abdominal pain caused by bursts of strong contraction of the smooth muscle of the intestinal wall. The incidence includes adults and infants, and it is the most common condition in children with acute abdominal pain. There are many reasons for gastrointestinal cramping pain, but most of them are caused by gastrointestinal dysfunction, and some are caused by organic lesions of the gastrointestinal tract. When the pain caused by gastrointestinal spasm is indeed functional and the diagnosis is clear, anticholinergic drugs are generally the first choice. It relaxes smooth muscle by selectively blocking M-chol...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/353A61P1/06A61P1/00A61P1/12C07D311/58
Inventor 付守廷胡春汪慧慧黄二芳兰惠瑜
Owner SHENYANG PHARMA UNIVERSITY
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