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Dopamine D1 receptor antagonist and application thereof

A dopamine and receptor technology, applied in the field of small molecule drugs, can solve the problems of weakened proliferation, decreased invasion ability and increased protein expression of glioma cells

Active Publication Date: 2021-03-09
TIANJIN INST OF IND BIOTECH CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Studies have shown that DRD1 protein is highly expressed in glioma tissue, and its expression can affect the growth of glioma cells. Dopamine D1 receptor antagonists can activate adenylate cyclase (adenylate cyclase, AC) to make its protein The expression level is significantly increased, thereby increasing the expression of PKA protein, resulting in a decrease in the protein level of p-p42 / 44MAPK, and finally weakening the proliferation and invasion ability of glioma cells

Method used

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  • Dopamine D1 receptor antagonist and application thereof
  • Dopamine D1 receptor antagonist and application thereof
  • Dopamine D1 receptor antagonist and application thereof

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Embodiment Construction

[0020] Unless otherwise defined, the technical terms used in the following embodiments have the same meaning as commonly understood by those skilled in the art to which the present invention belongs. The test reagents used in the following examples, unless otherwise specified, are conventional biochemical reagents; the experimental methods, unless otherwise specified, are conventional methods.

[0021] The present invention relates to compound 2586-96-1 purchased from Chengdu Durst Biotechnology Co., Ltd.

[0022] The present invention will be described in detail below in conjunction with the embodiments and accompanying drawings.

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Abstract

The invention provides a dopamine D1 receptor antagonist and an application thereof, and relates to the field of medicinal chemistry. The invention relates to the field of medicine, in particular to adopamine D1 receptor antagonist shown in a structural formula (I), pharmaceutically acceptable salt of the dopamine D1 receptor antagonist, a pharmaceutical composition containing the dopamine D1 receptor antagonist, and an application of a compound medicine to preparation of medicines for treating or preventing related diseases or symptoms caused by high expression or over-high activity of a dopamine D1 receptor.

Description

technical field [0001] The invention belongs to the field of small molecule drugs, and in particular relates to a dopamine D1 receptor antagonist and its application. Background technique [0002] Dopamine receptors belong to the family of G protein-coupled receptors, and are receptors in organisms that function through membrane receptors. Dopamine receptors are widely distributed not only in the brain, but also throughout the human body. According to different binding forces with ligands, dopamine receptors are divided into five subtypes, namely D1, D2, D3, D4, D5, and can be divided into D1 and D2 families, wherein the D1 receptor family includes D1 and D5 subtypes , which can activate adenylate cyclase and increase intracellular cyclic adenosine monophosphate (cAMP) concentration; the D2 receptor family includes D2, D3 and D4 subtypes, which can inhibit adenylate cyclase and also interact with cells Associated with other 2nd messenger systems in the body, including acti...

Claims

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Application Information

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IPC IPC(8): C07D217/20A61K31/472A61P35/00
CPCC07D217/20A61P35/00
Inventor 林建平刘翠刘岯李金龙
Owner TIANJIN INST OF IND BIOTECH CHINESE ACADEMY OF SCI
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