Bermann M C, Berthelot P, Bonte J P, Debaert M, Lesieur D, Brunet C, Cazin M, Lesieur I, Luyckx M, Cazin J C
Arzneimittelforschung. 1982;32(6):604-10. doi: 10.1002/chin.198243267.
Chemical and pharmacological properties of potent anorectic compounds with phenylpiperazinyl structure were studied. Among them, the three derivatives having the most interesting anorectic activity are product VI obtained by pharmacomodulation from amfepramone and the compounds IV and V, analogs of GABA. The derivative VI possesses an anorectic activity very similar to that of fenfluramine, namely: modification of feeding behaviour in treated rats, wasting away and decrease of adipose tissue. The two other compounds and more particularly compound V seem to be effective even when treatment is over. Perhaps this is in relation with metabolic effects modifying the regulation of feeding behaviour in the central nervous system. In fact, these compounds have substituents able to interfere with GABA systems.
对具有苯哌嗪基结构的强效食欲抑制剂化合物的化学和药理性质进行了研究。其中，具有最有趣的食欲抑制活性的三种衍生物是通过对安非拉酮进行药效调制得到的产物VI以及GABA类似物化合物IV和V。衍生物VI具有与芬氟拉明非常相似的食欲抑制活性，即：改变受试大鼠的摄食行为、消瘦以及脂肪组织减少。另外两种化合物，尤其是化合物V，即使在治疗结束后似乎仍有效果。这可能与改变中枢神经系统中摄食行为调节的代谢效应有关。事实上，这些化合物具有能够干扰GABA系统的取代基。
