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Application of 1-[2-(3-amino-6-methylthiophene [2,3-b] quinolyl)] ethyl ketone in preparation of vasodilator agent

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

Inactive Publication Date: 2015-03-25
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At the same time, the results of long-term administration in rats found that: 200mg / kg / d PU-14 subcutaneous injection 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]

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  • Application of 1-[2-(3-amino-6-methylthiophene [2,3-b] quinolyl)] ethyl ketone in preparation of vasodilator agent
  • Application of 1-[2-(3-amino-6-methylthiophene [2,3-b] quinolyl)] ethyl ketone in preparation of vasodilator agent
  • Application of 1-[2-(3-amino-6-methylthiophene [2,3-b] quinolyl)] ethyl ketone in preparation of vasodilator agent

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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 method. 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 m...

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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...

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Application Information

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