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布替林与一些相关标准三环类抗抑郁药的比较药理学研究。

Comparative pharmacological studies on butriptyline and some related standard tricyclic antidepressants.

作者信息

Jaramillo J, Greenberg R

出版信息

Can J Physiol Pharmacol. 1975 Feb;53(1):104-12. doi: 10.1139/y75-014.

Abstract

Butriptyline was compared with imipramine and other tricyclic antidepressants for its ability to modify: (a) contractions of the cat nictitating membrane induced by noradrenaline (NA) and 5-hydroxytryptamine (5-HT), (b) the adrenergic neuron blocking action of guanethidine in the guinea pig vas deferns, (c) the rabbit's electroencephalogram (EEG) and physostigmine arousal, and (d) the sleep pattern of the rat. Imipramine and amitriptyline potentiated the NA and 5-HT effects on the nictitating membrane and antagonized the inhibitory actions of guanethidine in the guinea pig vas deferens, whereas iprindole and butriptyline were ineffective. These results are consistent with the ability of these drugs to block the neuronal uptake of catecholamines. Butriptyline was a potent blocker of the arousal reaction induced by physostigmine. Butriptyline (20--30 mg/kg) and amitriptyline (10--20 mg/kg) reduced rapid eye movement sleep with a conmitant increase in non-rapid eye movement sleep. This may be a reflection of the dual activity observed in the clinic with these compounds, namely, antidepressant and antianxiety effects.

摘要

将布替林与丙咪嗪及其他三环类抗抑郁药进行比较,观察其对以下方面的影响:(a) 去甲肾上腺素(NA)和5-羟色胺(5-HT)诱导的猫瞬膜收缩;(b) 胍乙啶对豚鼠输精管的肾上腺素能神经元阻断作用;(c) 兔子的脑电图(EEG)及毒扁豆碱引起的唤醒反应;(d) 大鼠的睡眠模式。丙咪嗪和阿米替林增强了NA和5-HT对瞬膜的作用,并拮抗了胍乙啶对豚鼠输精管的抑制作用,而茚满二酮和布替林则无此作用。这些结果与这些药物阻断儿茶酚胺神经元摄取的能力一致。布替林是毒扁豆碱诱导的唤醒反应的有效阻断剂。布替林(20 - 30毫克/千克)和阿米替林(10 - 20毫克/千克)减少快速眼动睡眠,同时非快速眼动睡眠增加。这可能反映了这些化合物在临床上观察到的双重活性,即抗抑郁和抗焦虑作用。

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