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作 者:郭翔[1,2] 刘健 邹灵龙 金坚 王博诚[1,2] 金国章
机构地区:[1]中国科学院上海药物研究所 [2]核医学国家重点实验室
出 处:《中国药理学报》1998年第2期100-103,共4页Acta Pharmacologica Sinica
摘 要:目的:研究左旋千金藤立定(SPD)对羟多巴胺损毁大鼠纹状体中DARPP32蛋白磷酸化程度的影响.方法:反磷酸化测定脱磷DARPP32的含量.结果:SPD不改变正常大鼠纹状体中DARPP32磷酸化的程度,但能拮抗D1激动剂的作用;对羟多巴胺损毁大鼠的损侧纹状体,SPD使脱磷DARPP32的含量降低44%,给予D1拮抗剂可以拮抗这一作用.结论:在损侧纹状体,SPD显示D1激动剂的作用特性,增加DARPP32蛋白的磷酸化,而在正常纹状体,SPD表现为D1拮抗剂.AIM: To study effects of (-)stepholidine (SPD) on the phosphorylation of a dopamine and cAMPregulated phosphoprotein (DARPP32) in the striatum of oxidopaminelesioned rats. METHODS: The amount of dephosphoDARPP32 was measured by a backphosphorylation assay. RESULTS: In the striatum of control rats, SPD per se had no effect on the phosphorylation of DARPP32, but it antagonized the decrease by 28 % of dephosphoDARPP32 induced by the D1 agonist SK&F38393. In the denervated striatum of oxidopaminelesioned rats, SPD decreased the amount of dephosphoDARPP32 by 44 % . The effect of SPD was completely counteracted by the concomitant administration of the D1 antagonist Sch23390. CONCLUSION: SPD exhibits D1 agonistic action on DARPP32 phosphorylation in the denervated striatum of oxidopaminelesioned rats, but it acts as a D1 antagonist in normal striatum.
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