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[受体的临床方面;从动物模型到生理病理概念。芬氟拉明的经验]

[Clinical aspects of receptors; from animal models to physiopathological concepts. Experience with fenfluramine].

作者信息

Arnaud O, Rolland Y

机构信息

Institut de Recherches Internationales Servier, Courbevoie, France.

出版信息

J Pharm Belg. 1992 Jul-Aug;47(4):328-36.

PMID:1403600
Abstract

The fenfluramine racemate belongs to a new therapeutic class of molecules acting on food intake, without psychostimulant or addictive potential. This molecule was extensively studied in the treatment of obesity and its action was better understood by studying the dextrogyre and levogyre enantiomers. New methods allowed to show that dexfenfluramine (the dextrogyre isomer) worked through a serotoninergic activity which was responsible for the effect on food intake and disorders of eating behavior. New pharmacological concepts have emerged by using this molecule and new animal models, nearer to human pathology, were found (stress induced eating, carbohydrate selection...). Molecular Biology and Neurosciences have already led to a better knowledge of the central mechanism of action of the molecule by describing its effect on receptors and binding sites; however a lot of other concepts remain to be discovered.

摘要

芬氟拉明外消旋体属于一类作用于食物摄入的新型治疗性分子,无精神兴奋或成瘾潜力。该分子在肥胖治疗方面得到了广泛研究,通过对右旋和左旋对映体的研究,对其作用有了更深入的了解。新方法表明,右芬氟拉明(右旋异构体)通过5-羟色胺能活性发挥作用,这一活性导致了对食物摄入及饮食行为紊乱的影响。利用该分子出现了新的药理学概念,还发现了更接近人类病理的新动物模型(应激性进食、碳水化合物选择等)。分子生物学和神经科学已经通过描述该分子对受体和结合位点的作用,使人们对其中心作用机制有了更好的认识;然而,还有许多其他概念有待发现。

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