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

Application of 1-[2-(3-amino-6-methylthieno[2,3-b]quinolyl)]ethanone in the preparation of vasodilators

A kind of vasodilator, applied technology, applied to the application of 1-[2-(3-amino-6-methylthieno[2,3-b]quinolyl)]ethanone in the preparation of vasodilator field, can solve problems such as electrolyte imbalance in the blood

Inactive Publication Date: 2016-11-02
PEKING UNIV
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, the results of long-term administration in rats showed that: 200mg / kg / d PU-14 subcutaneously injected for one week has obvious diuretic effect, and there is no electrolyte disorder in the blood and abnormal lipid metabolism and glucose metabolism caused by the positive control drug hydrochlorothiazide. Phenomenon [1]

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
  • Application of 1-[2-(3-amino-6-methylthieno[2,3-b]quinolyl)]ethanone in the preparation of vasodilators
  • Application of 1-[2-(3-amino-6-methylthieno[2,3-b]quinolyl)]ethanone in the preparation of vasodilators
  • Application of 1-[2-(3-amino-6-methylthieno[2,3-b]quinolyl)]ethanone in the preparation of vasodilators

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1, the pharmacodynamics test of PU-14 dilating blood vessels

[0035] 1. Expression of UT-B in vascular endothelial cells

[0036] The thoracic aortas of 8-week-old male UT-B(- / -) and UT-B(+ / +) mice were isolated, frozen sections, and UT-B were labeled by immunohistochemical methods. figure 1 The results showed that UT-B was mainly expressed on the membrane of vascular endothelial cells.

[0037] Bovine aortic endothelial cells were planted in 96-well plates, fixed with 4% paraformaldehyde when 100% confluent, and immunofluorescent staining was performed. figure 1 The results showed that UT-B was expressed on the bovine aortic endothelial cell membrane.

[0038] 2. The effect of Ach on dilation of isolated thoracic aorta of UT-B knockout mice

[0039] Grouping of experimental animals: male wild-type mice UT-B (+ / +) and UT-B knockout mice UT-B (- / -), 8 weeks old, 10 in each group.

[0040] METHODS: The ring tension of the isolated mouse thoracic aorta was ...

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

No PUM Login to View More

Abstract

The invention discloses a novel application of a medicine of 1-[2-(3-amino-6-methylthiophene [2,3-b] quinolyl)] ethyl ketone. The new application of the compound (PU-14) disclosed by the invention is an application in the preparation of a vasodilator agent medicine. The PU14 has an effect of directly relaxing blood vessels by adopting in vitro thoracic aorta and mesenteric artery models in mice and rats. The effect is similar to that of acetyl choline, and has endothelial dependence and NO dependence; the action can be blocked off by an NOS inhibitor L-NAME and a cyclooxygenase inhibitor indometacin part; and meanwhile, in vivo and in vitro research results both prove that the UT-B gene deletion or function deficiency can play a role in relaxing blood vessels by adjusting the interaction between L-Arg-NOS-NO and L-Arg-arginase-urea systems.

Description

technical field [0001] The invention relates to the application of 1-[2-(3-amino-6-methylthieno[2,3-b]quinolyl)]ethanone in the preparation of vasodilators. Background technique [0002] 1. General characteristics of the urea channel protein inhibitor PU-14 (Uti) [0003] The structural formula of urea channel protein inhibitor PU-14 is shown in formula I: [0004] [0005] Its Chinese name is: 1-[2-(3-amino-6-methylthieno[2,3-b]quinolyl)]ethanone. [0006] This compound is a high-efficiency and low-toxic small molecule compound obtained by the research group of the inventor through screening the small molecule compound library in the early stage. The previous research results proved that the small molecular compound has obvious selective blocking effect on urea channel protein UT-B. The blocking effect has been confirmed in various animal erythrocyte in vitro models, including human, rabbit, rat, and mouse. Among them, the representative compound PU-14 (Ut) was confi...

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 Patents(China)
IPC IPC(8): A61K31/4365A61P9/08A61P9/00
CPCA61K31/4743
Inventor 周虹杨宝学孙逸
Owner PEKING 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