首页> 外国专利> use of 2 - amino - 6 - allyl - 5,6,7,8 - tetrahydro in thiazolo (4.5) azepins to manufacture a for the treatment of parkinson's disease. the parkinsonism suitable product.

use of 2 - amino - 6 - allyl - 5,6,7,8 - tetrahydro in thiazolo (4.5) azepins to manufacture a for the treatment of parkinson's disease. the parkinsonism suitable product.

机译:使用噻唑罗(4.5)氮杂庚酸酯中的2-氨基-6-烯丙基-5,6,7,8-四氢联苯生产用于治疗帕金森氏病的药物。帕金森氏症合适的产品。

摘要

2-Amino-6-allyl-5,6, 7,8-tetrahydro- 4H-thiazolo(4,5-d)azepine (I) and its acid addition salts for the treatment of Parkinson's disease or parkinsonism are new. (I) dihydrochloride (B-HT920) is a known selective agonist of presynaptic dopaminergic receptors (e.g. Acta Pharmacol.Toxicol. 1983, 52, 51-56, J.Neural Transmission 1983, 59, 129-137). Biological test results are given in the specification demonstrating that B-HT920 also exerts an agonistic effect on denervated or degenerated post-synaptic dopaminergic structures of the brain and is therefore useful in the treatment of Parkinsonism. Tests described include inhibition of exploratory and stereotyped movement in naive rats, effects on ipsilateral rotation in the rat ibotenic acid model and on contralateral rotation in the 6-OHDA model, and effects on the MPTP Parkinsonism model in the rhesus monkey.
机译:用于治疗帕金森氏病或帕金森氏症的2-氨基-6-烯丙基-5,6,7,8-四氢-4H-噻唑洛(4,5-d)氮杂(I)及其酸加成盐是新的。 (I)二盐酸盐(B-HT920)是突触前多巴胺能受体的已知选择性激动剂(例如Acta Pharmacol.Toxicol.1983,52,51-56,J.Neural Transmission 1983,59,129-137)。说明书中给出了生物学测试结果,表明B-HT920也对神经的失神经或变性的突触后多巴胺能结构发挥激动作用,因此可用于治疗帕金森氏症。所描述的测试包括在幼稚大鼠中抑制探索性和定型运动,对大鼠卵磷脂酸模型中的同侧旋转和6-OHDA模型中的对侧旋转产生影响以及对恒河猴的MPTP帕金森症模型产生影响。

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