Smith S A, Levy A L, Sennitt M V, Simson D L, Cawthorne M A
Biochem Pharmacol. 1985 Jul 15;34(14):2425-9. doi: 10.1016/0006-2952(85)90521-0.
Zucker fa/fa rats exhibit glucose intolerance in comparison with lean Fa/? littermates. A single acute dose of BRL 26830 (2.9 mg/kg p.o.) improved glucose tolerance in Fa/? littermates but exacerbated glucose intolerance in the fa/fa rats. This latter effect occurred in spite of an increase in the plasma insulin concentration. Chronic treatment of Zucker fa/fa rats with BRL 26830 (2.9 mg/kg) for 24 days or more produced a significant reduction in the area under the glucose tolerance curve. In addition, the glucose decay rate (k%) following the administration of insulin intravenously was significantly increased in the BRL 26830-treated rats suggesting that tissue insulin sensitivity was increased. Glucose turnover measurements show that chronic treatment of Zucker fa/fa rats with BRL 26830 produced a significant increase in the rate of glucose utilization integrated over a 3 hr period, but this increase was, in part, off-set by an increase in the endogenous rate of glucose production. The ultimate fate of the extra glucose that is metabolized is not known but it is suggested that it might be used to support the thermogenic response that is also activated by BRL 26830.
与瘦型 Fa/? 同窝仔鼠相比,Zucker fa/fa 大鼠表现出葡萄糖不耐受。单次急性给予 BRL 26830(2.9 毫克/千克,口服)可改善 Fa/? 同窝仔鼠的葡萄糖耐量,但会加剧 fa/fa 大鼠的葡萄糖不耐受。尽管血浆胰岛素浓度有所升高,但仍出现了后一种效应。用 BRL 26830(2.9 毫克/千克)对 Zucker fa/fa 大鼠进行 24 天或更长时间的慢性治疗,可使葡萄糖耐量曲线下面积显著减小。此外,在接受 BRL 26830 治疗的大鼠中,静脉注射胰岛素后的葡萄糖衰减率(k%)显著增加,这表明组织胰岛素敏感性增强。葡萄糖周转率测量结果显示,用 BRL 26830 对 Zucker fa/fa 大鼠进行慢性治疗,在 3 小时期间内葡萄糖利用率显著提高,但这种提高部分被内源性葡萄糖生成速率的增加所抵消。额外代谢的葡萄糖的最终去向尚不清楚,但有人认为它可能用于支持也由 BRL 26830 激活的产热反应。