首页> 外国专利> PROTECTION OF NEURONS AGAINST GLUTAMATE-INDUCED DAMAGE IN GLAUCOMA AND OTHER CONDITIONS

PROTECTION OF NEURONS AGAINST GLUTAMATE-INDUCED DAMAGE IN GLAUCOMA AND OTHER CONDITIONS

机译:预防由谷氨酸引起的青光眼和其他情况的神经元损伤

摘要

The present invention is directed to a method of protecting cells of the nervous system from glutamate-induced cytotoxicity, such as the type that is mimicked by administration of N-methyl-D-aspartate (NMDA), and which is associated with conditions such as ischemia or glaucoma. In general, the method comprises increasing the activity of a cannabinoid agonist that binds specifically to an endogenous cannabinoid receptor, such as the endogenous cannabinoid receptors CB1 or CB2, to protect the cells against glutamate-induced neurotoxicity. This can be done either by the administration of a cannabinoid agonist such as a physiologically acceptable salt of R(+)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4-benzoxazinyl]-(1-naphthalenyl)methanone, preferably the mesylate salt, or by blocking degradation of naturally-occurring endogenous cannabinoid agonists in the cells, such as by inhibition of anandamide amidohydrolase. Administration can be performed by one of several routes, such as enterally, transdermally, or transmucosally.
机译:本发明涉及保护神经系统细胞免受谷氨酸诱导的细胞毒性的方法,所述谷氨酸诱导的细胞毒性例如是通过施用N-甲基-D-天冬氨酸(NMDA)所模拟的类型,并且与诸如缺血或青光眼。通常,该方法包括提高与内源性大麻素受体(例如内源性大麻素受体CB1或CB2)特异性结合的大麻素激动剂的活性,以保护细胞免受谷氨酸诱导的神经毒性。可以通过施用大麻素激动剂,例如R(+)-[2,3-二氢-5-甲基-3-[(吗啉基)甲基]吡咯并[1,2,3]的生理可接受盐来完成-de] -1,4-苯并恶嗪基]-(1-萘基)甲酮,优选为甲磺酸盐,或通过阻止细胞中天然存在的内源性大麻素激动剂的降解,例如通过抑制花生四烯酸酰胺酰胺水解酶。可以通过几种途径之一进行施用,例如肠内,透皮或透粘膜。

著录项

  • 公开/公告号WO0247691A1

    专利类型

  • 公开/公告日2002-06-20

    原文格式PDF

  • 申请/专利权人 AYOUB GEORGE S.;

    申请/专利号WO2001US48848

  • 发明设计人 AYOUB GEORGE S.;

    申请日2001-12-12

  • 分类号A61K31/535;

  • 国家 WO

  • 入库时间 2022-08-22 00:36:04

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