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Composition for competitive inhibition of orexin receptors

A technology of orexin receptors and compositions, which is applied in the field of inhibiting the binding of orexin to its receptors, can solve problems that are not yet known, and achieve excellent antagonism and inhibition of orexin receptors and the effect of inhibiting the binding of orexin to its receptors

Pending Publication Date: 2021-09-03
SUNTORY HLDG LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is not known that it is a natural compound and has an orexin receptor antagonistic inhibitory effect

Method used

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  • Composition for competitive inhibition of orexin receptors
  • Composition for competitive inhibition of orexin receptors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] The orexin receptor antagonist activity of the test substance was measured using an accessory of the Orexin 2 Receptor Reporter Assay Kit (Cayman Chemical Company).

[0057] In this evaluation system, cells expressing orexin receptors on the cell surface are used. When an agonist (orexin) binds to this orexin receptor, secreted alkaline phosphatase (SEAP) is secreted. The secreted SEAP was reacted with an alkaline phosphatase substrate, and the enzymatic activity of SEAP was measured using a photometer. Substances having orexin receptor antagonistic action (orexin receptor antagonist action) reduce the enzyme activity.

[0058] (1) Use Dulbecco's Modified Eagle's Medium-high glucose (With 4500mg / Lglucose, L-glutamine , sodium pyruvate, and sodium bicarbonate, liquid, sterile-filtered, suitable for cell culture) (Sigma-Aldrich Company), using HEK293T cells to reach 2.5×10 5 cells / mL were prepared.

[0059] (2) Sow 200 μL of the culture medium containing HEK293T cells...

Embodiment 2

[0070] For the pyrroloquinoline quinone disodium salt-added group of Example 1, cell proliferation after the addition of pyrroloquinoline quinone disodium salt was measured using WST-8 Cell Proliferation Assay Kit (Cayman Chemical Company). The determination method is based on the attached experimental guide. It is known that dehydrogenase activity is directly proportional to the number of viable cells. This kit is a kit for measuring the dehydrogenase activity released from cells into the culture medium using this principle. For the negative control group and the positive control group in Example 1, the cell proliferation after the addition of DMSO or Suvorexan was also measured in the same way.

[0071] figure 2It is a graph showing dehydrogenase activity in a negative control group (N.C.), a positive control group (P.C.), and a pyrroloquinoline quinone disodium salt-added group (PQQ). The results (mean ± standard error) are expressed as relative values ​​with the dehydr...

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PUM

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Abstract

The purpose of the present invention is to provide: a novel composition for competitive inhibition of orexin receptors which is able to inhibit orexin from binding to receptors thereof; and a method for inhibiting orexin from binding to receptors thereof. The present invention relates to a composition for competitive inhibition of orexin receptors which contains pyrroloquinoline quinone or a salt thereof as an active ingredient.

Description

technical field [0001] The present invention relates to a composition for inhibiting orexin receptor antagonism. In addition, the present invention also relates to methods for inhibiting the binding of orexin to its receptor (orexin receptor), and the like. Background technique [0002] Orexin is a neuropeptide produced by nerve cells present in the lateral hypothalamus. Orexin receptors are orexin-specific receptors. When orexin acts on orexin receptors, it can increase the degree of awakening of animals and increase food intake. Therefore, a substance having an action of inhibiting the binding of orexin to its receptor (orexin receptor antagonism inhibition action) is also expected to have an action of inhibiting arousal state and the like. [0003] Patent Document 1 describes compounds used as orexin receptor antagonists. Suvorexant is also known as an orexin receptor antagonist inhibitor. However, there is no known compound that is a natural compound and has an orexi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P25/20A61P25/28A61P43/00A23L29/00A23L33/10A61K31/4745
CPCA61P43/00A61K31/4745A61P25/20A61P25/28A23L29/045
Inventor 糸贺翔大渡边齐志高野二郎
Owner SUNTORY HLDG LTD