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Application of NR2B negative allosteric modulator combined with GABA receptor modulator in preparation of medicine for treating Alzheimer's disease

A technology for Alzheimer's disease and allosteric modulators, applied in the field of negative allosteric modulators, to achieve significant drug synergy

Inactive Publication Date: 2020-08-04
SUZHOU CHIEN SHIUNG INST OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] However, no pharmacological studies have reported that the above-mentioned NR2B negative allosteric modulators and GABA A modulators have synergistic effects in the treatment of AD.

Method used

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  • Application of NR2B negative allosteric modulator combined with GABA receptor modulator in preparation of medicine for treating Alzheimer's disease
  • Application of NR2B negative allosteric modulator combined with GABA receptor modulator in preparation of medicine for treating Alzheimer's disease
  • Application of NR2B negative allosteric modulator combined with GABA receptor modulator in preparation of medicine for treating Alzheimer's disease

Examples

Experimental program
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Embodiment

[0039] The following example examines the improving effect of Compound 1 of the present invention combined with Basmisanil or Etazolate on learning and memory impairment in dementia model mice induced by aluminum trichloride and D-galactose.

[0040] (1) Test product

[0041] Basmisanil and Etazolate (purchased from chemscene), aluminum trichloride (commercially available), D-galactose (commercially available); compound 1 hydrochloride (hereinafter referred to as compound 1, according to the method 8 on page 49 of the patent CN201580051671.3 specification Prepared as described, substituting 2-bromo-1-(5-hydroxypyridin-2-yl)ethanone for 2-bromo-1-(4-hydroxyphenyl)ethanone).

[0042] (2) Experimental animals

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Abstract

The invention discloses application of an NR2B negative allosteric modulator combined with a GABA receptor modulator in preparation of a medicine for treating Alzheimer's disease. The inventor found that when the GABA receptor modulator, an n-alkylaryl-5-oxyaryl-octahydro-cyclopentadieno [c] pyrrole compound, is combined with the NR2B negative allosteric modulator, particularly Basisanil or Etazolate, an obviously enhanced pharmacodynamic synergistic effect is achieved in comparison with respective single drugs, which indicates that the combination of the NR2B negative allosteric modulator andthe GABA receptor modulator has positive potential application in preparation of a medicine for treating Alzheimer's disease.

Description

technical field [0001] The invention belongs to the field of pharmacy, in particular to a negative allosteric regulator of NR2B. [0002] technical background [0003] Alzheimer's disease (AD) is a brain neurodegenerative disease with memory loss and cognitive decline as the main clinical symptoms. Current research suggests that N-methyl-D-aspartate receptors (NMDARs) ) play a crucial role in synaptic transmission and synaptic plasticity, and are thought to underlie learning and memory. [0004] Activation of NMDARs has recently been shown to be associated with AD associated with synaptic dysfunction. Missense mutations in the GRIN2B coding region have only been found in the brains of AD patients, suggesting that there is a close relationship between such mutations in postsynaptic NR2B subunits and changes in synaptic structure. It was also found in primary neuronal cultures and hippocampal slices of rats and mice that Aβ (amyloid)-induced early neuronal dysfunction was med...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/403A61K31/4439A61P25/28A61P25/18A61P25/24A61P25/22
CPCA61K31/403A61K31/4439A61P25/18A61P25/22A61P25/24A61P25/28
Inventor 刘尚莲王杨朱少晖陈雪峰金晨杨成德
Owner SUZHOU CHIEN SHIUNG INST OF TECH
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