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具有中枢多巴胺和去甲肾上腺素受体阻断特性的抗精神病药物对大鼠左旋多巴和(+)-苯丙胺诱导的清醒脑电图的影响。

The effects of neuroleptics with central dopamine and noradrenaline receptor blocking properties in the L-DOPA and (+)-amphetamine-induced waking EEG in the rat.

作者信息

Monti J M

出版信息

Br J Pharmacol. 1979 Sep;67(1):87-91.

Abstract

1 A study was carried out in rats (prepared for chronic sleep recording) of the effects of pretreatment with neuroleptics differing in their relative antinoradrenaline and antidopamine receptor potencies, on the L-DOPA and (+)-amphetamine-induced increase in waking EEG. 2 Haloperidol (0.6 mg/kg), which blocks central dopamine and noradrenaline (NA) receptors, reversed the EEG desynchronizing actions of L-DOPA and (+)-amphetamine. 3 Low doses of pimozide (0.4 to 0.8 mg/kg) which block dopamine receptors exclusively, were not able to modify the pharmacologically induced disruption of the sleep-awake cycle. However, at 1 mg/kg, a dose which also produces blockade of NA receptors, pimozide counteracted the increase in waking elicited by (+)-amphetamine. 4 Spiroperidol (1 to 4 mg/kg) which is devoided of NA receptor blocking properties, failed to reverse the L-DOPA or (+)-amphetamine-induced arousal. 5 Our results suggest that the increased waking time observed after the catecholamine agonists is related to an increased availability of NA rather than dopamine.

摘要
  1. 对大鼠(准备用于慢性睡眠记录)进行了一项研究,观察具有不同抗去甲肾上腺素和抗多巴胺受体效力的抗精神病药物预处理,对左旋多巴和(+)-苯丙胺诱导的清醒脑电图增加的影响。2. 阻断中枢多巴胺和去甲肾上腺素(NA)受体的氟哌啶醇(0.6毫克/千克),逆转了左旋多巴和(+)-苯丙胺的脑电图去同步化作用。3. 仅阻断多巴胺受体的低剂量匹莫齐特(0.4至0.8毫克/千克),无法改变药理学诱导的睡眠-觉醒周期紊乱。然而,在1毫克/千克时,该剂量也会产生NA受体阻断作用,匹莫齐特抵消了(+)-苯丙胺引起的清醒增加。4. 缺乏NA受体阻断特性的螺哌利多(1至4毫克/千克),未能逆转左旋多巴或(+)-苯丙胺诱导的觉醒。5. 我们的结果表明,在儿茶酚胺激动剂后观察到的清醒时间增加,与NA而非多巴胺的可用性增加有关。

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