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目的:研究左旋千金藤啶碱(SPD)和其同类物CSL、THPB10对大鼠纹状体D1、D2多巴胺(DA)受体作用特性。方法:24mA直流电刺激体外灌流之大鼠纹状体脑薄片,每5min收集灌流液测定[3H]DA释放量;分离大鼠纹状体突触体,用放免方法测定腺苷酸环化酶活性。结果:D2受体激动剂LY171555显著抑制电刺激诱发的[3H]DA释放,SPD、CSL和THPB10翻转LY171555的抑制作用,SPD、CSL、THPB10也诱发DA释放。在用Butaclamol封闭D2受体后,SPD和CSL以剂量依赖方式激活常敏大鼠纹状体突触体腺苷酸环化酶,而THPB10无作用。结论:合双羟基的SPD及其同类物CSL对DA受体不同亚型有激动/阻滞不同效应。
AIM: To investigate the effects of levamisole (SPD) and its analogues CSL and THPB10 on dopamine D1 and D2 receptors in rat striatum. Methods: The rat brain striatum was perfused with 24mA DC, and the release of [3H] DA was measured every 5 minutes. The striatum synaptosomes were isolated and the adenylate cyclase activity . Results: D2 receptor agonist LY171555 significantly inhibited the release of [3H] DA induced by electrical stimulation, and the inhibition of LY171555 was reversed by SPD, CSL and THPB10. The release of DA was also induced by SPD, CSL and THPB10. After blockade of D2 receptors with Butaclamol, SPD and CSL activated striatal synaptosomal adenylate cyclase in an allergic rat in a dose-dependent manner, with no effect of THPB10. CONCLUSIONS: Biphasic dihydroxy SPDs and their cognate CSLs have different agonist / block effects on different subtypes of DA receptors.