Day C, Bailey C J
Department of Pharmaceutical and Biological Sciences, Aston University, Birmingham, UK.
Int J Obes Relat Metab Disord. 1998 Jul;22(7):619-23. doi: 10.1038/sj.ijo.0800636.
Sibutramine is a reuptake inhibitor of 5-hydroxytryptamine and noradrenaline, being developed as a treatment for obesity.
To investigate the effect of sibutramine on glucose homeostasis in obese-hyperglycaemic insulin-resistant ob/ob mice.
Sibutramine 5 mg/kg once daily was administered orally to ob/ob mice for six weeks.
Sibutramine treatment decreased body weight gain by 12% without a significant overall change in daily food intake. Sibutramine reduced the hyperinsulinaemia by 31%, and lowered plasma non-esterified fatty acids (NEFA) by 17%. Basal plasma glucose concentrations were not significantly altered by sibutramine, but glucose concentrations fell more rapidly after an i.p. glucose challenge, despite lower insulin concentrations. The rate of insulin-induced glucose disappearance was increased by 10% during sibutramine treatment. First administration of sibutramine, 5 mg/kg, did not acutely alter basal plasma glucose, insulin or NEFA concentrations in ob/ob mice, although NEFA concentrations were raised after 24 h.
The results indicate that chronic administration of sibutramine can reduce weight gain, lower NEFA concentrations, decrease hyperinsulinaemia and ameliorate the insulin resistance of ob/ob mice.
西布曲明是一种5-羟色胺和去甲肾上腺素再摄取抑制剂,正被开发用于治疗肥胖症。
研究西布曲明对肥胖-高血糖胰岛素抵抗ob/ob小鼠葡萄糖稳态的影响。
对ob/ob小鼠每日口服一次5 mg/kg西布曲明,持续六周。
西布曲明治疗使体重增加减少了12%,而每日食物摄入量无显著总体变化。西布曲明使高胰岛素血症降低了31%,并使血浆非酯化脂肪酸(NEFA)降低了17%。西布曲明未显著改变基础血浆葡萄糖浓度,但腹腔注射葡萄糖激发后,尽管胰岛素浓度较低,葡萄糖浓度下降更快。在西布曲明治疗期间,胰岛素诱导的葡萄糖消失率提高了10%。首次给予5 mg/kg西布曲明并未急性改变ob/ob小鼠的基础血浆葡萄糖、胰岛素或NEFA浓度,尽管24小时后NEFA浓度升高。
结果表明,长期给予西布曲明可减轻体重增加、降低NEFA浓度、减少高胰岛素血症并改善ob/ob小鼠的胰岛素抵抗。