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在通过 SCH 23390 阻断 D-1 受体后,高剂量阿扑吗啡诱导的镇静和睡眠。

Sedation and sleep induced by high doses of apomorphine after blockade of D-1 receptors by SCH 23390.

作者信息

Gessa G L, Porceddu M L, Collu M, Mereu G, Serra M, Ongini E, Biggio G

出版信息

Eur J Pharmacol. 1985 Feb 26;109(2):269-74. doi: 10.1016/0014-2999(85)90429-7.

Abstract

The effect of SCH 23390, a selective blocker of D-1 receptors, on apomorphine-induced behavioural and EEG changes was studied in rats. In control rats, a low dose of apomorphine (50 micrograms/kg s.c.) produced sedation associated with EEG synchronization. A high dose of apomorphine (1 mg/kg s.c.) produced stereotypy associated with EEG desynchronization. At the dose of 1 mg/kg i.p., SCH 23390 decreased motor activity but failed to alter the EEG pattern. The administration of either the low or high dose of apomorphine to SCH 23390-treated rats elicited a marked sedative response associated with EEG synchronization. The EEG synchronization produced by apomorphine (50 micrograms/kg) in SCH 23390-treated rats was prevented by (-)-sulpiride (25 mg/kg i.p.), a D-2 receptor blocker. It is concluded that by preventing the excitatory response to apomorphine SCH 23390 discloses the existence of a population of D-2 receptors mediating sedation and sleep.

摘要

在大鼠中研究了D-1受体选择性阻断剂SCH 23390对阿扑吗啡诱导的行为和脑电图变化的影响。在对照大鼠中,低剂量阿扑吗啡(50微克/千克皮下注射)产生与脑电图同步相关的镇静作用。高剂量阿扑吗啡(1毫克/千克皮下注射)产生与脑电图去同步相关的刻板行为。腹腔注射剂量为1毫克/千克时,SCH 23390降低了运动活性,但未能改变脑电图模式。给经SCH 23390处理的大鼠注射低剂量或高剂量阿扑吗啡均引发了与脑电图同步相关的明显镇静反应。阿扑吗啡(50微克/千克)在经SCH 23390处理的大鼠中产生的脑电图同步被D-2受体阻断剂(-)-舒必利(25毫克/千克腹腔注射)阻断。得出的结论是,通过阻止对阿扑吗啡的兴奋反应,SCH 23390揭示了介导镇静和睡眠的一群D-2受体的存在。

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