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雷氯必利对大鼠探究性运动活动、跑步机运动、条件性回避行为和僵住症的影响:雷氯必利、氟哌啶醇和普拉克莫之间的行为特征比较

Effects of raclopride on exploratory locomotor activity, treadmill locomotion, conditioned avoidance behaviour and catalepsy in rats: behavioural profile comparisons between raclopride, haloperidol and preclamol.

作者信息

Hillegaart V, Ahlenius S

出版信息

Pharmacol Toxicol. 1987 May;60(5):350-4. doi: 10.1111/j.1600-0773.1987.tb01525.x.

Abstract

Raclopride, a new potential antipsychotic agent blocking central dopamine (D2) receptors, was found to suppress exploratory locomotor activity, treadmill locomotion and conditioned avoidance response in rats. The threshold dose for effects in these test situations was about 0.5 mg/kg intraperitoneally. A considerably higher dose, 16 mg/kg intraperitoneally, was needed to produce maximal catalepsy. Maximal effects were obtained within 1-2 hrs and the duration of the effect was 2-8 hrs, depending on the test situation. The behavioural profile of raclopride is different from the classic antipsychotic haloperidol, blocking central dopamine (DA) receptors, as well as from the partial DA agonist preclamol, which inhibits central DA neurotransmission by activating DA autoreceptors. Thus, although similar to haloperidol in other respects, comparatively high doses of raclopride are needed to produce catalepsy, indicating less propensity to produce severe extrapyramidal side effects. Raclopride and preclamol are about equipotent in suppressing exploratory locomotor activity. However, raclopride is more potent than preclamol in suppressing treadmill locomotion, conditioned avoidance behaviour and catalepsy.

摘要

雷氯必利是一种新型潜在抗精神病药物,可阻断中枢多巴胺(D2)受体,研究发现它能抑制大鼠的探究性运动活动、跑步机运动和条件性回避反应。在这些测试情境中产生效应的阈剂量约为腹腔注射0.5毫克/千克。要产生最大程度的僵住症,则需要腹腔注射相当高的剂量,即16毫克/千克。最大效应在1 - 2小时内出现,效应持续时间为2 - 8小时,具体取决于测试情境。雷氯必利的行为特征不同于经典抗精神病药物氟哌啶醇(后者可阻断中枢多巴胺(DA)受体),也不同于部分DA激动剂普拉克莫(后者通过激活DA自身受体抑制中枢DA神经传递)。因此,尽管雷氯必利在其他方面与氟哌啶醇相似,但产生僵住症需要相对较高的剂量,这表明其产生严重锥体外系副作用的倾向较小。雷氯必利和普拉克莫在抑制探究性运动活动方面效力相当。然而,在抑制跑步机运动、条件性回避行为和僵住症方面,雷氯必利比普拉克莫更有效。

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