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用Lineweaver-Burk分析法研究哺乳动物多巴胺受体拮抗剂对玛瑙螺巨型神经元中多巴胺诱导电流的阻断作用。

Lineweaver-Burk analysis for the blocking effects of mammalian dopamine receptor antagonists on dopamine-induced currents in Achatina giant neurones.

作者信息

Emaduddin M, Takeuchi H

机构信息

Department of Physiology, Gifu University School of Medicine, Japan.

出版信息

Gen Pharmacol. 1996 Oct;27(7):1209-13. doi: 10.1016/s0306-3623(96)00045-6.

DOI:10.1016/s0306-3623(96)00045-6
PMID:8981069
Abstract
  1. We had demonstrated (Emaduddin et al., 1995) the blocking effects of the three mammalian dopamine receptor antagonists, (+/-)-SKF83566 (mammalian dopamine D1-like receptor antagonist), (+)-UH232 (D2 and D3-like receptor antagonist) and (+/-)-sulpiride (D2-like receptor antagonist) on the dose (pressure duration)-response curves of dopamine in the three giant neurone types, LVMN (left visceral multiple spike neurone), d-RPeAN (dorsal-right pedal anterior neurone) and v-LCDN (ventral-left cerebral distinct neurone), of Achatina fulica Férussac under voltage clamp. In the present study, we analyzed these data by Lineweaver-Burk plot. 2. Dopamine-induced inward currents (Iin) of the two neurone types, LVMN and d-RPeAN, were blocked by (+/-)-SKF83566 and (+)-UH232 in partly noncompetitive and partly uncompetitive manners. (+/-)-Sulpiride had no effect on these currents. 3. In contrast, dopamine-induced outward current (Iout) of v-LCDN was inhibited competitively by (+/-)-sulpiride and noncompetitively by (+)-UH232. (+/-)-SKF83566 had no effect on this current. 4. Therefore, we consider that the pharmacological features of the dopamine receptors of Achatina neurones are not identical in detail to those of the mammalian dopamine receptors.
摘要
  1. 我们(Emaduddin等人,1995年)已经证明了三种哺乳动物多巴胺受体拮抗剂,(±)-SKF83566(哺乳动物多巴胺D1样受体拮抗剂)、(+)-UH232(D2和D3样受体拮抗剂)和(±)-舒必利(D2样受体拮抗剂)在电压钳制下对福寿螺Ferussac的三种巨型神经元类型,即左内脏多峰神经元(LVMN)、右背足前神经元(d-RPeAN)和左腹侧脑特异神经元(v-LCDN)中多巴胺的剂量(压力持续时间)-反应曲线的阻断作用。在本研究中,我们通过Lineweaver-Burk图分析了这些数据。2. (±)-SKF83566和(+)-UH232以部分非竞争性和部分非竞争性方式阻断了LVMN和d-RPeAN这两种神经元类型中多巴胺诱导的内向电流(Iin)。(±)-舒必利对这些电流没有影响。3. 相比之下,v-LCDN中多巴胺诱导的外向电流(Iout)被(±)-舒必利竞争性抑制,被(+)-UH232非竞争性抑制。(±)-SKF83566对该电流没有影响。4. 因此,我们认为福寿螺神经元多巴胺受体的药理学特征与哺乳动物多巴胺受体的药理学特征在细节上并不相同。

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