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泰舒达,一种多巴胺激动剂-拮抗剂混合药物,在帕金森病动物模型中的研究。

Terguride, a mixed dopamine agonist-antagonist, in animal models of Parkinson's disease.

作者信息

Koller W C, Herbster G

出版信息

Neurology. 1987 Apr;37(4):723-7. doi: 10.1212/wnl.37.4.723.

Abstract

Terguride, an analogue of lisuride, decreased locomotor activity, produced cataplexy, and blocked apomorphine-induced stereotypic behavior. It did not induce stereotypies in rodents or emesis in dogs. However, in rats with unilateral 6-hydroxydopamine lesions of the substantia nigra, terguride produced contralateral rotation. Terguride bound to D-2 striatal dopamine receptors. Terguride has both agonist and antagonist actions at striatal dopamine receptors, but chronic administration did not produce behavioral supersensitivity. These pharmacologic properties differ from those of other antiparkinsonian agents; terguride may be effective for the chronic treatment of Parkinson's disease.

摘要

泰舒达(terguride)是麦角乙脲(lisuride)的类似物,可降低运动活性、引发猝倒,并阻断阿扑吗啡诱导的刻板行为。它不会在啮齿动物中诱发刻板行为,也不会在犬类中引起呕吐。然而,在单侧黑质6-羟基多巴胺损伤的大鼠中,泰舒达会引发对侧旋转。泰舒达与纹状体D-2多巴胺受体结合。泰舒达在纹状体多巴胺受体上兼具激动剂和拮抗剂作用,但长期给药不会产生行为超敏反应。这些药理学特性与其他抗帕金森病药物不同;泰舒达可能对帕金森病的长期治疗有效。

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