Eisenberg M S, Maher T J
Department of Pharmacology, Massachusetts College of Pharmacy and Allied Health Sciences, Boston 02115.
Pharmacol Biochem Behav. 1990 Apr;35(4):865-9. doi: 10.1016/0091-3057(90)90372-o.
Phenylpropanolamine (PPA, d,l-norephedrine), available in many over-the-counter nasal decongestants and appetite suppressants, is a racemic mixture of the enantiomers d- and l-norephedrine. The present study evaluates the effects of the individual PPA enantiomers on a variety of nondrug (food deprivation) and drug-induced hyperphagias (2-deoxyglucose and insulin). Racemic PPA has been shown to significantly suppress food intake in these hyperphagic models. Both l-norephedrine (5-50 mg/kg) and d-norephedrine (5-150 mg/kg), administered intraperitoneally, significantly suppressed feeding after a 4-hr fast during the dark cycle. During the light period, l-norephedrine (7.5, 10, 15 mg/kg) and d-norephedrine (75, 100, 150 mg/kg) significantly reduced food intake at the 1-hr and 3-hr time intervals in the 24-hr food deprivation-, insulin- and 2-deoxyglucose-induced hyperphagic models. Only 7.5 mg/kg l-norephedrine in the insulin-induced hyperphagia at 3 hr failed to significantly suppress feeding. These results indicate that each individual PPA enantiomer possesses the ability to suppress food intake in rats made hyperphagic by various stimuli.
苯丙醇胺(PPA,消旋去甲麻黄碱)存在于许多非处方减充血剂和食欲抑制剂中,是右旋和左旋去甲麻黄碱对映体的外消旋混合物。本研究评估了PPA各对映体对多种非药物(食物剥夺)和药物诱导的食欲亢进(2-脱氧葡萄糖和胰岛素)的影响。在这些食欲亢进模型中,消旋PPA已被证明能显著抑制食物摄入。腹腔注射左旋去甲麻黄碱(5 - 50毫克/千克)和右旋去甲麻黄碱(5 - 150毫克/千克),在黑暗周期禁食4小时后均能显著抑制进食。在光照期,左旋去甲麻黄碱(7.5、10、15毫克/千克)和右旋去甲麻黄碱(75、100、150毫克/千克)在24小时食物剥夺、胰岛素和2-脱氧葡萄糖诱导的食欲亢进模型中,在1小时和3小时间隔时显著减少食物摄入量。在胰岛素诱导的3小时食欲亢进模型中,只有7.5毫克/千克的左旋去甲麻黄碱未能显著抑制进食。这些结果表明,PPA的每个对映体都具有抑制由各种刺激引起的食欲亢进大鼠食物摄入的能力。