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新型抗抑郁药文拉法辛急性给药的药理学特征。

Pharmacological profile of venlafaxine, a new antidepressant, given acutely.

作者信息

Rogóz Z, Dziedzicka-Wasylewska M, Maj J

机构信息

Institute of Pharmacology, Polish Academy of Sciences, Kraków, Poland.

出版信息

Pol J Pharmacol. 1998 Mar-Apr;50(2):107-15.

PMID:9798262
Abstract

Pharmacological effects of acute treatment with venlafaxine (VEN), a clinically active antidepressant [a noradrenaline (NA) and 5-hydroxytryptamine (5-HT) reuptake inhibitor without any affinity for neurotransmitter receptors] were studied in mice and rats. VEN inhibited the reserpine- or apomorphine-induced hypothermia and enhanced the L-5-HTP-induced head twitches in mice. It reduced the immobility time in Porsolt's test in mice and rats, but either did not change the locomotor activity (mice) or decreased it (rats). VEN reduced the locomotor hyperactivity induced by amphetamine (AMP), apomorphine (APO) and quinpirole (QUI), as well as the APO-induced stereotypy; the stereotypy induced by AMP in rats was prolonged. VEN neither changed the clonidine-induced aggressiveness in mice nor the behavioral syndrome induced by oxotremorine in rats. The obtained results indicate that VEN, given acutely, shows a pharmacological profile similar to that of tricyclic NA and 5-HT reuptake inhibitors. In contrast to the antidepressants mentioned above, VEN does not exhibit an alpha 1-adrenolytic or a cholinolytic activity (in vivo tests).

摘要

文拉法辛(VEN)是一种临床有效的抗抑郁药(一种对神经递质受体无亲和力的去甲肾上腺素(NA)和5-羟色胺(5-HT)再摄取抑制剂),研究了其急性给药在小鼠和大鼠中的药理作用。VEN抑制了利血平或阿扑吗啡诱导的体温过低,并增强了L-5-HTP诱导的小鼠头部抽搐。它减少了小鼠和大鼠在波索尔特试验中的不动时间,但要么不改变运动活性(小鼠),要么降低运动活性(大鼠)。VEN减少了由苯丙胺(AMP)、阿扑吗啡(APO)和喹吡罗(QUI)诱导的运动性多动,以及APO诱导的刻板行为;AMP在大鼠中诱导的刻板行为延长。VEN既不改变可乐定在小鼠中诱导的攻击性,也不改变毒蕈碱在大鼠中诱导的行为综合征。所得结果表明,急性给予VEN显示出与三环类NA和5-HT再摄取抑制剂相似的药理特征。与上述抗抑郁药相反,VEN不表现出α1-肾上腺素能或胆碱能活性(体内试验)。

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