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Application of gaboxadol to preparation of medicine for treating alzheimer's disease and pharmaceutical composition

A technique for Alzheimer's, gaboxadol, applied in the field of medicinal chemistry

Pending Publication Date: 2020-01-14
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Gaboxadol is usually used in the research of analgesics, anesthetics, anticonvulsants and food depressants, but there is no report on the application of Gaboxadol in Alzheimer's disease in the existing literature

Method used

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  • Application of gaboxadol to preparation of medicine for treating alzheimer's disease and pharmaceutical composition
  • Application of gaboxadol to preparation of medicine for treating alzheimer's disease and pharmaceutical composition
  • Application of gaboxadol to preparation of medicine for treating alzheimer's disease and pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] This example is used to illustrate that gaboxadol can effectively prevent the reduction of hippocampal neuron regeneration in AD mice, and hardly affect the hippocampal neuron regeneration in normal mice.

[0021] Three-transformed AD mice (APP KM670 / 671NL (Swedish), MAPT P301L, PSEN1 M146V) and wild-type mice were used as research objects. Four-month-old 3-transformed AD mice and wild-type mice were selected and injected with retrovirus ROV-GFP in the dentate gyrus of the hippocampus to label newborn neurons. At the same time, solvent (normal saline) or gaboxadol was injected intraperitoneally at 3 mg / kg every 2 days for two months. The brains were collected by perfusion at 6 months old, and the sections were subjected to immunohistochemistry and fluorescent staining to observe the new generation of hippocampal neurons.

[0022] Brain slice preparation includes the following steps:

[0023] A1: Inject 1% pentobarbital sodium (1.5mg / 20g) into the mouse intraperitoneal...

Embodiment 2

[0035] This example is used to illustrate that gaboxadol can effectively reduce hyperphosphorylation and abnormal aggregation of tau protein in the hippocampal dentate gyrus of AD mice, and hardly affect the phosphorylation level of tau protein in normal mice.

[0036] 3-transformed AD mice and wild-type mice were used as research objects. Select 4-month-old wild-type mice and 3-transformed AD mice, and inject solvent (normal saline) or gaboxadol at 3 mg / kg intraperitoneally, every 2 days for two months. At the age of 6 months, the mice were sacrificed acutely, the brain was removed, the hippocampal tissue was separated, and the protein was extracted for Western blot (WB) experiment to detect phosphorylated tau protein (p-Thr205, p-Ser396, AT8) and total tau protein (Tau5).

[0037] 3-transformed AD mice and wild-type mice were used as research objects. Select 4-month-old wild-type mice and 3-transformed AD mice, and inject solvent (normal saline) or gaboxadol at 3 mg / kg intr...

Embodiment 3

[0055] This example is used to illustrate that gaboxadol can effectively improve the learning and memory functions of AD mice without affecting the cognitive functions of normal mice.

[0056] 3-transformed AD mice and wild-type mice were used as research objects. Select 4-month-old wild-type mice and 3-transformed AD mice, and inject solvent (normal saline) or gaboxadol at 3 mg / kg intraperitoneally, every 2 days for two months. Behavioral experiments began at the age of 5 months. For 3 consecutive days before the start of the experiment, the mice were grasped to make them acclimated, and at the same time, the mice were allowed to adapt to the environment of the test box. The object-location recognition experiment is divided into two stages: exploration and testing, such as Figure 5 shown.

[0057] Exploration stage: place the mice in a box (50×50×50cm, with a small green balloon on the inner wall of the box as a visual cue) to explore freely for 5 minutes, in which two id...

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Abstract

The invention relates to the field of pharmaceutical chemistry, in particular to application of gaboxadol to preparation of a medicine for treating alzheimer's disease and a pharmaceutical composition. The pharmaceutical composition contains the gaboxadol and pharmaceutically-acceptable auxiliaries. According to the application of gaboxadol to preparation of the medicine for treating the alzheimer's disease and the pharmaceutical composition disclosed by the invention, due to the gaboxadol, rebirth of hippocampal neurons of AD mice can be promoted, excessive phosphorylation and abnormal aggregation of tau proteins are reduced, and a recognition function is improved.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to the application of gaboxadol in the preparation of medicines for treating Alzheimer's disease and the pharmaceutical composition. Background technique [0002] Alzheimer's disease (AD) is a degenerative disease of the central nervous system with progressive cognitive impairment as the main clinical manifestation, and is the most common type of dementia. The anti-AD drugs that have been approved and widely used clinically are all symptomatic treatments and cannot change the progressive deterioration of AD. Therefore, the development of new anti-AD drugs has great scientific and social significance. [0003] 4,5,6,7-Tetrahydroisoxazolo-[5,4-c]pyridin-3-ol, also known as gaboxadol, is the first to target extrasynaptic GABA-A receptors in the brain It is an anti-insomnia drug designed on the spot, which has a higher affinity with the GABA A receptor containing delta subunit, and i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4353A61P25/28
CPCA61K31/4353A61P25/28
Inventor 王建枝郑杰
Owner HUAZHONG UNIV OF SCI & TECH
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