Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Insect repellent tetramisole capable of serving as novel antiarrhythmic drug

A technology of arrhythmia and tetramisole, applied in tetramisole, the application field in the preparation of drugs for treating arrhythmia

Pending Publication Date: 2020-02-28
SHANXI MEDICAL UNIV
View PDF0 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] But so far, there is only such an I as zacopride K1 Specific agonists are publicly reported

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Insect repellent tetramisole capable of serving as novel antiarrhythmic drug
  • Insect repellent tetramisole capable of serving as novel antiarrhythmic drug
  • Insect repellent tetramisole capable of serving as novel antiarrhythmic drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1. Effect of insect repellant tetramisole on resting potential and action potential of left ventricular myocytes.

[0043] because I K1 It is the main ion current that determines the resting potential (RMP) level and the terminal repolarization of the action potential (AP) phase 3. We observed the effects of the insect repellent tetramisole on the resting potential and action potential of left ventricular myocytes.

[0044] (1) Acute isolation of rat left ventricular cardiomyocytes by collagenase method

[0045] Healthy adult male SD rats (body weight 220-250 g) were selected and anesthetized by intraperitoneal injection of pentobarbital sodium (40 mg / kg). cold, 100% oxygen saturation), after quick trimming, the heart was suspended in the Langendorff perfusion device for perfusion (the perfusate was filled with 100% oxygen throughout, and retrogradely perfused through the aorta to the coronary arteries). First perfuse for 8-10 minutes (calcium-free Tyrode's so...

Embodiment 2

[0052] Example 2. Tetramisole can up-regulate rat left ventricular myocyte I K1 Protein

[0053] In rat ventricular myocytes, Kir2.1 is a constituent of I K1 Most dominant channel protein isoform. Rat left ventricular myocytes isolated by collagenase were incubated with 10 μmol / L tetramisole for 24 hours to detect the expression of Kir2.1 protein. Tetramisole upregulates I in rat ventricular myocytes K1 Protein expression (P image 3 ), indicating that tetramisole can serve as I K1 agonist.

Embodiment 3

[0054] Example 3. Effect of Tetramisole on Acute Ischemic Arrhythmia in Rats

[0055] (1) Modeling method: adult male SD rats (220-250 g) healthy adult SD rats were fasted overnight before the operation, anesthetized with sodium pentobarbital (65 mg / kg, i.p.), and cut below the thyroid cartilage Tracheal intubation was performed after the trachea, artificially ventilated by a small animal ventilator (DH-1, Chengdu Instrument Factory, Chengdu, China) with a tidal volume of 30 ml / kg body weight, a respiratory rate of 60 breaths / min, and a respiratory ratio of 2:1. Open the pericardium, ligate the left anterior descending branch of the left coronary artery with 6 / 0 suture at 2 mm above the lower edge of the left atrial appendage, and perform partial ischemia for 15 minutes. The elevation of ST segment is a sign of successful ligation (myocardial ischemia); after loosening Refill for 15 minutes. Limb II lead ECG was continuously recorded and analyzed (RM6240, BiopacSystem, Chengd...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
electrical resistanceaaaaaaaaaa
Login to View More

Abstract

The invention discloses application of tetramisole in preparing drug for treating arrhythmia. It is found for the first time that tetramisole can effectively serve as an IK1 specific agonist, has effect similar to that of zacopride and can serve as antiarrhythmic drug, so that a new treatment way which is effective and safe is provided.

Description

technical field [0001] The invention relates to a cardiovascular disease drug, in particular to the application of tetramisole in the preparation of drugs for treating arrhythmia. Background technique [0002] At present, almost all antiarrhythmic drugs in clinical use are various ion channel blockers, and their main targets act on Na . Kv , Ca ion channels. Disorder drugs fall into four categories: [0003] Class I: Sodium channel blockers [0004] I a : Moderate intensity (moderate blockade of sodium channels), quinidine, procainamide [0005] I b : Mild blockade of sodium channels, lidocaine, phenytoin, mexiletine, tocainide [0006] I c : Severe sodium channel blockade, propafenone, flecainide [0007] These drugs block sodium channels, alter conduction in unidirectional tissue regions, and eliminate reentry. [0008] Class II: β receptor blockers, such as propranolol, these drugs can reduce the 4-phase depolarization current and reduce self-discipline. [0009]...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/429A61P9/06
CPCA61K31/429A61P9/06
Inventor 贺培凤卢学春于琦刘清华袁永旭武建光刘鸿齐
Owner SHANXI MEDICAL UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com