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Applications of 1 type cysteinyl leukotriene receptor antagonist on preparation of medicament for treating the Alzheimer disease

A technology of cysteinyl leukotrienes, Alzheimer's disease, applied in the field of medicine

Inactive Publication Date: 2014-01-15
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far nothing about CysLT 1 The relationship between R and its antagonists and AD

Method used

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  • Applications of 1 type cysteinyl leukotriene receptor antagonist on preparation of medicament for treating the Alzheimer disease
  • Applications of 1 type cysteinyl leukotriene receptor antagonist on preparation of medicament for treating the Alzheimer disease
  • Applications of 1 type cysteinyl leukotriene receptor antagonist on preparation of medicament for treating the Alzheimer disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] cCysLT 1 R activation leads to Aβ aggregation and memory impairment

[0020] experimental method

[0021] 1. Animals and groups

[0022] Take 40 clean-grade ICR male mice aged 8 weeks and weighing 22-25 g (provided by the Comparative Medicine Center of Yangzhou University, SCXK (Su) 2007-0001), and divide them into 4 groups, which are the normal control group (PBS+ PBS), cysteinyl leukotriene D4 group (LTD4+PBS), pranlukast group (pranlukast+PBS) and pranlukast plus cysteinyl leukotriene D4 group (pranlukast+LTD4), each Group 10. After bilateral intracerebroventricular injection, the memory function of the animals was evaluated by Morris water maze test after 72 hours. After the Morris water maze test, the animals were sacrificed, the brain was taken, the hippocampus and cortex were separated, and the hippocampus and cortex were detected by ELISA, Western blot and RT-PCR respectively. Aβ 40 , Aβ 42 and CysLT 1 R level.

[0023] 2. Morris water maze test

[002...

Embodiment 2

[0040] CysLT 1 R antagonist contralateral intracerebroventricular injection of Aβ 42 The source and structure of drugs that can improve learning and memory impairment in dementia-induced mice

[0041] Pranlukast, zafirlukast, and montelukast sodium are all raw materials produced by pharmaceutical companies, and their structures are as follows:

[0042]

[0043] pranlukast

[0044] (molecular formula: C 27 h 23 N 5 o 4 Molecular weight: 481.50)

[0045]

[0046] zafirlukast

[0047] (molecular formula: C 31 h 33 N 3 o 6 S molecular weight: 575.68)

[0048]

[0049] Montelukast

[0050] (molecular formula: C 35 h 36 ClNO 3 S molecular weight: 586.18)

[0051] experimental method

[0052] 1. Model establishment and administration

[0053] Get 8 weeks old, body weight is 120 clean level ICR mice of 22-25g, male and female (provided by the comparative medical center of Yangzhou University, SCXK (Su) 2007-0001), treated with 10% chloral hydrate (350mg / kg...

Embodiment 3

[0073] CysLT 1 R antagonists and their analogs against Aβ 42 The source and structure of drugs with protective effects on primary cultured mouse neurons

[0074] Pranlukast, zafirlukast and montelukast have the same structure as above.

[0075] The eight drugs of irast, alumilast, mitrolast, peripexil, cinalast, velukast, pyramolast, and ibudilast were purchased from different pharmaceutical or chemical companies , and their structure is as follows:

[0076]

[0077] iralukast

[0078] (molecular formula: C 38 h 37 f 3 o 8 S molecular weight: 710.76)

[0079]

[0080] ablukast

[0081] (molecular formula: C 28 h 34 o 8 Molecular weight: 498.56)

[0082]

[0083] Mitrodast

[0084] (molecular weight: C 13 h 12 N 2 o 2 S molecular formula: 260.31)

[0085]

[0086] Pobilukast

[0087] (molecular weight: C 26 h 34 o 5 S molecular formula: 458.61)

[0088]

[0089] Cinalukast

[0090] (molecular formula: C 23 h 28 N 2 o 3 S molecular...

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Abstract

The invention relates to applications of a cysteinyl leukotriene receptor antagonist (CysLT1R) on preparation of a medicament for treating the Alzheimer disease. Research finds that intracerebral CysLT1R mediates A beta aggregation and dysmnesia; and by oral medication, CysLT1R antagonists such as pranlukast, zafirlukast and montelukast can improve mice memory impairment caused by A beta. The CysLT1R antagonists such as pranlukast, zafirlukast and montelukast, and analogs thereof such as iralukast, ablukast, imitrodast, pobilukast, cinalukast, verlukast, pemirolast and ibudilast, have significant protection effect on primarily-cultured mice neuron damage caused by A beta. The CysLT1R antagonists such as pranlukast, zafirlukast and montelukast, and the analogs thereof such as iralukast, ablukast, imitrodast, pobilukast, cinalukast, verlukast, pemirolast and ibudilast, can be used for preparing anti-AD medicaments.

Description

technical field [0001] The invention relates to the field of medicines, in particular to the use of a type 1 cysteinyl leukotriene receptor antagonist in the preparation of medicines for treating Alzheimer's disease. Background technique [0002] Alzheimer's disease (AD), also known as senile dementia, is characterized by β-amyloid protein (β-amyloid protein, Aβ) plaques in the brain as the main pathological feature and progressive decline in cognitive and memory functions as the main clinical manifestation. A fatal neurodegenerative disease. Its incidence is increasing year by year with the acceleration of human modernization and aging process. It is estimated that by 2050, AD patients worldwide will exceed 100 million. This widespread neurological disease not only brings great suffering to patients and their families, but also becomes the fourth leading cause of death in the elderly population. But so far there is no effective medical method to cure this disease. At pre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/41A61K31/404A61K31/47A61P25/28
Inventor 洪浩唐苏苏
Owner CHINA PHARM UNIV
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