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多巴胺激动剂对大鼠不同脑区自身受体功能的相对效价。

Relative potency of dopamine agonists on autoreceptor function in various brain regions of the rat.

作者信息

Westfall T C, Naes L, Paul C

出版信息

J Pharmacol Exp Ther. 1983 Jan;224(1):199-205.

PMID:6848743
Abstract

The effect of six dopamine agonists including apomorphine, epinine, dopamine, piribedil, lergotrile and bromocriptine on the incorporation of [3H]tyrosine into dopamine was studied in slices and synaptosomes prepared from various brain areas containing dopamine terminals including striatum, nucleus accumbens, olfactory tubercle and medial basal hypothalamus. It was observed that all of these drugs were active in causing a decrease in dopamine synthesis in these various brain areas. The catecholamine agonists apomorphine, epinine and dopamine were more potent in inhibiting dopamine synthesis in the mesolimbic structures than in the striatum. On the other hand, apomorphine and epinine were less potent while dopamine was more potent in the medial basal hypothalamus. The ergoline drugs were weak agonists in all structures studied. It is concluded that autoreceptor regulation of dopamine synthesis is more active in the mesolimbic compared with the nigrostriatal dopamine pathway while autoreceptors may be absent in the median eminence.

摘要

研究了包括阿扑吗啡、表肾上腺素、多巴胺、吡贝地尔、麦角腈和溴隐亭在内的六种多巴胺激动剂对从含有多巴胺终末的不同脑区(包括纹状体、伏隔核、嗅结节和内侧基底下丘脑)制备的脑片和突触体中[3H]酪氨酸掺入多巴胺的影响。观察到所有这些药物均能有效降低这些不同脑区的多巴胺合成。儿茶酚胺激动剂阿扑吗啡、表肾上腺素和多巴胺在抑制中脑边缘结构中的多巴胺合成方面比在纹状体中更有效。另一方面,阿扑吗啡和表肾上腺素在内侧基底下丘脑的效力较弱,而多巴胺的效力较强。麦角灵类药物在所研究的所有结构中均为弱激动剂。结论是,与黑质纹状体多巴胺通路相比,中脑边缘多巴胺合成的自身受体调节更为活跃,而正中隆起可能不存在自身受体。

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