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2-溴麦角酰脲,一种麦角衍生物,具有多巴胺拮抗和血清素激动特性。

2-Bromolisuride, an ergot derivative, with dopamine antagonistic and serotonin agonistic properties.

作者信息

Fink H, Morgenstern R, Ott T

机构信息

Institute of Pharmacology and Toxicology, Charité Humboldt-University, DDR, Berlin.

出版信息

Pharmacol Biochem Behav. 1991 Feb;38(2):321-5. doi: 10.1016/0091-3057(91)90285-a.

Abstract

The open-field test was used to study the involvement of dopaminergic and serotonergic mechanisms in the effects of 2-bromolisuride on locomotor activity in the rat. 2-Bromolisuride produced a dose-dependent inhibition of spontaneous locomotor activity. This is most likely due to an antagonistic action at postsynaptic dopamine receptors. Low doses of 2-bromolisuride potentiated apomorphine-induced hypermotility. This potentiating effect was not mediated by a blockade of presynaptic dopamine receptors, because it was not prevented by 6-OHDA lesion of the nucleus accumbens. The potentiating effect of 2-bromolisuride was completely blocked by the serotonin antagonists cyproheptadine and ritanserin. It is suggested that 2-bromolisuride possesses dopamine antagonistic and serotonin agonistic properties.

摘要

采用旷场试验研究多巴胺能和5-羟色胺能机制在2-溴利舒脲对大鼠运动活动影响中的作用。2-溴利舒脲对自发运动活动产生剂量依赖性抑制。这很可能是由于对突触后多巴胺受体的拮抗作用。低剂量的2-溴利舒脲增强了阿扑吗啡诱导的运动亢进。这种增强作用不是由对突触前多巴胺受体的阻断介导的,因为伏隔核的6-羟基多巴胺损伤并不能阻止这种作用。2-溴利舒脲的增强作用被5-羟色胺拮抗剂赛庚啶和利坦色林完全阻断。提示2-溴利舒脲具有多巴胺拮抗和5-羟色胺激动特性。

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