Screening method for histamine H1 receptor antagonist

A technology of receptor antagonists and screening methods, applied in the field of drug screening research, can solve the problems of anticholinergic weight gain and other problems, and achieve high sensitivity and high throughput effects
CN106544392AInactive Publication Date: 2017-03-29DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
Publication Date
2017-03-29
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a screening method for a histamine H1 receptor antagonist. By adopting unmarked cell target point pharmacology technology, DMR response signals generated after histamine acts on A-431 cells or A-549 cells are monitored. Desensitization is conducted in a dose-dependent mode through the DMR response signals generated after the histamine acts on the A-431 cells or the A-549 cells, high-expression H1 receptors on the A-431 cells or the A-549 cells are certified, and the DMR response signals generated after the receptors are activated can be successfully monitored. The DMR response signals are not generated when the A-431 cells or the A-549 cells are preprocessed by a specificity histamine H1 receptor antagonist, but the DMR response signals of the histamine is antagonized in a dose-dependent mode after the histamine is added again. In this way, the screening method for the histamine H1 receptor antagonist is successfully established. The DMR response signals generated when to-be-screened compounds subject preprocessing to the A-431 cells or the A-549 cells are monitored firstly; and if the to-be-screened compounds do not generate the DMR response signals, the DMR response signals of the histamine are antagonized after the histamine is added again, and antagonistic activity of the compounds on the H1 receptors are judged according to the antagonized extent of the response signals.
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Description

technical field

[0001] The invention belongs to the field of drug screening research, in particular to a screening method for histamine H1 receptor antagonists. Background technique

[0002] Histamine usually exists in mast cells and basophils in an inactive state. After external stimuli such as trauma and antigen-antibody reactions, histamine is released outside the cells in an activated form and participates in inflammatory reactions. [1] . Histamine exerts its physiological effects by binding to histamine receptors. There are four types of histamine receptors in the human body: H1, H2, H3 and H4 receptors. These four types of histamine receptors are all G protein-coupled receptors (GPCRs), which transduce extracellular signals to the second intracellular signal system through G proteins [1,2] . The allergic inflammatory effect mediated by histamine mainly binds to H1 receptors, causing hyperemia, edema and itching of the skin and mucous membranes. Asthma, anaphylacti...

Claims

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