芬氟拉明对大鼠组织单胺储备的作用。

Action of fenfluramine on monoamine stores of rat tissues.

作者信息

Costa E, Groppetti A, Revuelta A

出版信息

Br J Pharmacol. 1971 Jan;41(1):57-64. doi: 10.1111/j.1476-5381.1971.tb09935.x.

DOI:10.1111/j.1476-5381.1971.tb09935.x

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1702756/

Abstract

Fenfluramine is an anorexogenic agent used clinically because it is devoid of central stimulatory effects.2. In rats, fenfluramine causes a depletion of 5-hydroxytryptamine (5-HT) from the telencephalon + diencephalon which lasts longer than one might have expected from the biological half life of fenfluramine. The depleting effects of fenfluramine do not extend to brainstem, stomach and heart stores of 5-HT.3. Fenfluramine causes an increase in the turnover rate of tel-diencephalic 5-HT but such an acceleration could not be detected in the 5-HT stores of the brainstem.4. It is inferred that the effects of fenfluramine on brain 5-hydroxytryptamine may be related to the accumulation of a fenfluramine metabolite in 5-HT neurones.5. High doses of fenfluramine cause a depletion of catecholamine stores in brain and heart but the time course of this depletion is shorter than the depletion of brain 5-HT.

摘要

芬氟拉明是一种临床上使用的食欲抑制药，因为它没有中枢兴奋作用。
在大鼠中，芬氟拉明会导致端脑+间脑的5-羟色胺（5-HT）耗竭，其持续时间比根据芬氟拉明的生物半衰期所预期的要长。芬氟拉明的耗竭作用并不扩展到脑干、胃和心脏中的5-HT储备。
芬氟拉明会导致端脑-间脑5-HT的周转率增加，但在脑干的5-HT储备中未检测到这种加速。
据推测，芬氟拉明对脑5-羟色胺的作用可能与芬氟拉明代谢物在5-HT神经元中的积累有关。
高剂量的芬氟拉明会导致脑和心脏中的儿茶酚胺储备耗竭，但这种耗竭的时间进程比脑5-HT的耗竭要短。