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新型作用机制的抗抑郁药咯利普兰在三种不同体内动物模型中无抗胆碱能活性。

Absence of anticholinergic activity of rolipram, an antidepressant with a novel mechanism of action, in three different animal models in vivo.

作者信息

Wachtel H, Löschmann P A, Pietzuch P

机构信息

Research Laboratories of Schering AG, Berlin, West.

出版信息

Pharmacopsychiatry. 1988 Sep;21(5):218-21. doi: 10.1055/s-2007-1014679.

Abstract

Rolipram, in contrast to the tricyclic antidepressants amitriptyline and imipramine or the acetylcholine receptor antagonist atropine, failed to antagonize the salivation, hypothermia, or tremor caused in mice by the muscarinic receptor agonists pilocarpine or oxotremorine. The absence of anticholinergic activity, the extremely low therapeutic dose, and the novel mechanism of antidepressant action suggest that rolipram may also be a well tolerable antidepressant suitable for the treatment of problematic subpopulations of depressives such as elderly patients.

摘要

与三环类抗抑郁药阿米替林和丙咪嗪或乙酰胆碱受体拮抗剂阿托品不同,咯利普兰未能拮抗毒蕈碱受体激动剂毛果芸香碱或氧化震颤素在小鼠中引起的唾液分泌、体温过低或震颤。缺乏抗胆碱能活性、极低的治疗剂量以及新颖的抗抑郁作用机制表明,咯利普兰可能也是一种耐受性良好的抗抑郁药,适用于治疗有问题的抑郁症亚群体,如老年患者。

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