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利苏瑞德对纹状体突触体中多巴胺合成的抑制作用:(-)-舒必利的立体特异性逆转。

Inhibition of dopamine synthesis in striatal synaptosomes by lisuride: stereospecific reversal by (-)-sulpiride.

作者信息

Tissari A H, Atzori L, Galdieri M T

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1983 Feb;322(1):89-91. doi: 10.1007/BF00649358.

Abstract

Lisuride, an ergot D2 dopamine receptor agonist inhibited dopamine synthesis in striatal synaptosomes concentration-dependently. Significant inhibition was detected at 10(-8) M, and the inhibition by 10(-4) M lisuride was 50%. The inhibitory effect of lisuride was reversed by more than 50% not only by the D1-D2 dopamine receptor blocker haloperidol but also by the D2 dopamine receptor blocker(-)-sulpiride. The effect of sulpiride was stereospecific. Under the same test conditions a similar inhibition of dopamine synthesis by apomorphine was reversed by the neuroleptics almost completely. The results suggest that there are dopamine autoreceptors controlling dopamine synthesis in synaptosomes and these receptors resemble D2 dopamine receptors according to the nomenclature of Kebabian and Calne (1979).

摘要

利舒脲,一种麦角D2多巴胺受体激动剂,能浓度依赖性地抑制纹状体突触体中的多巴胺合成。在10(-8) M时检测到显著抑制,10(-4) M利舒脲的抑制率为50%。利舒脲的抑制作用不仅被D1-D2多巴胺受体阻滞剂氟哌啶醇逆转了50%以上,也被D2多巴胺受体阻滞剂(-)-舒必利逆转了50%以上。舒必利的作用具有立体特异性。在相同的测试条件下,阿扑吗啡对多巴胺合成的类似抑制几乎被这些抗精神病药物完全逆转。结果表明,突触体中存在控制多巴胺合成的多巴胺自身受体,根据Kebabian和Calne(1979年)的命名法,这些受体类似于D2多巴胺受体。

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