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盐酸芬氟拉明对大鼠输精管的拟交感神经活性。

The sympathomimetic activity of fenfluramine hydrochloride on rat vas deferens.

作者信息

Mottram D R, Wadhwani D

出版信息

Br J Pharmacol. 1977 Apr;59(4):615-20. doi: 10.1111/j.1476-5381.1977.tb07729.x.

Abstract
  1. The peripheral, pharmacological effects of the anorexigenic agent, fenfluramine hydrochloride, have been investigated on rat isolated vas deferens. 2. Characteristic spiked contractions were observed within 2 to 3 min after exposure to fenfluramine; these contractions reached a rate of around 13 per min and were of variable height. 3. Pre-treatment of vasa with the indirectly acting sympathomimetic amine, tyramine, greatly reduced both the height and rate of contraction induced by fenfluramine. 4. The uptake inhibitor, desipramine, required a concentration in excess of 10 micronM to affect fenfluramine-induced contractions. Effects of desipramine on fenfluramine contractions were of equal magnitude whether desipramine was administered before fenfluramine or at the height of the fenfluramine-induced contractions. 5. Pre-treatment with debrisoquine (0.5 mM), reduced the contractions in response to fenfluramine over a period of time. 6. Fenfluramine, added to vasa from rats which had been injected intraperitoneally with 5 mg/kg reserpine 24 h and 48 h previously, failed to induce its characteristic contractions. 7. It is concluded that fenfluramine can be classed as an indirectly acting sympathomimetic amine on peripheral adrenergic nerve terminals.
摘要
  1. 对食欲抑制剂盐酸芬氟拉明在大鼠离体输精管上的外周药理学作用进行了研究。2. 接触芬氟拉明后2至3分钟内观察到特征性的尖峰收缩;这些收缩频率达到每分钟约13次,高度各不相同。3. 用间接作用的拟交感神经胺酪胺对输精管进行预处理,可大大降低芬氟拉明诱导的收缩高度和频率。4. 摄取抑制剂地昔帕明需要超过10微摩尔的浓度才能影响芬氟拉明诱导的收缩。无论地昔帕明是在芬氟拉明之前给药还是在芬氟拉明诱导的收缩高峰时给药,其对芬氟拉明收缩的影响程度相同。5. 用去甲异喹胍(0.5毫摩尔)预处理,在一段时间内可降低对芬氟拉明的收缩反应。6. 向24小时和48小时前腹腔注射5毫克/千克利血平的大鼠的输精管中添加芬氟拉明,未能诱导其特征性收缩。7. 得出结论,芬氟拉明在外周肾上腺素能神经末梢可归类为间接作用的拟交感神经胺。
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef5f/1667758/973e6719b1d5/brjpharm00500-0076-a.jpg

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