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Nueva diana molecular de la neurotoxicidad
专利权人:
EXONHIT THERAPEUTICS SA
发明人:
RESINK, ANNELIES,AIT IKHLEF, ALI,SCHWEIGHOFFER, FABIEN
申请号:
ES08160783
公开号:
ES2348348T5
申请日:
2002.08.13
申请国别(地区):
ES
年份:
2013
代理人:
摘要:
Detecting excitotoxicity and neuronal stress in a subject comprises in vitro measurement of phosphodiesterase-4 (PDE4), particularly PDE4B, or detecting the presence of a mutant form of the mRNA for PDE4B, particularly a form that lacks all or part of the 3-non-coding region. Independent claims are also included for the following: (1) Use of a compound (A) that inhibits or reduces expression or activity of PDE4B for treatment of neurodegenerative diseases (2) Primers (B) containing 8-20 consecutive residues from the nucleotide region 2384-2869 of a murine PDE4B sequence (S1) or 2461-4068 of a human PDE4B sequence and (3) Kits for analyzing expression of PDE4. - ACTIVITY : Nootropic Neuroprotective Antiparkinsonian Anticonvulsant Cerebroprotective. Granular neurons from the cerebellum of rats were treated with N-methyl-D-aspartate (i) and serine or kainate (ii), to stimulate excititoxicity. When this treatment was carried out in presence of 50 M pentoxifylline, toxicity was reduced from about 40 to 20% in (i) and from about 30 to 10% in (ii). - MECHANISM OF ACTION : Inhibiting expression or activity of PDE4B, which is present at elevated level in pathological nerve tissue.Uso de al menos un compuesto de la familia de las pirazolopiridinas capaz de inhibir o reducir la actividad de PDE4, para la preparación de una composición farmacéutica destinada a inhibir o reducir la excitotoxicidad neuronal en fase temprana de por lo menos una enfermedad neurodegenerativa elegida entre la enfermedad de Alzheimer y la enfermedad de Parkinson.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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