Department of Pharmacology, UT Southwestern Medical Center, Dallas, TX 75390, USA.
Laboratory of Molecular Genetics, Howard Hughes Medical Institute, The Rockefeller University, New York, NY 10065, USA.
Cell Metab. 2023 Mar 7;35(3):429-437.e5. doi: 10.1016/j.cmet.2023.02.005.
Animals that consume fermenting fruit and nectar are at risk of exposure to ethanol and the detrimental effects of inebriation. In this report, we show that the hormone FGF21, which is strongly induced by ethanol in murine and human liver, stimulates arousal from intoxication without changing ethanol catabolism. Mice lacking FGF21 take longer than wild-type littermates to recover their righting reflex and balance following ethanol exposure. Conversely, pharmacologic FGF21 administration reduces the time needed for mice to recover from ethanol-induced unconsciousness and ataxia. FGF21 did not counteract sedation caused by ketamine, diazepam, or pentobarbital, indicating specificity for ethanol. FGF21 mediates its anti-intoxicant effects by directly activating noradrenergic neurons in the locus coeruleus region, which regulates arousal and alertness. These results suggest that this FGF21 liver-brain pathway evolved to protect against ethanol-induced intoxication and that it might be targeted pharmaceutically for treating acute alcohol poisoning.
食用发酵水果和花蜜的动物有暴露于乙醇和醉酒有害影响的风险。在本报告中,我们表明,乙醇在鼠和人肝脏中强烈诱导的激素 FGF21 刺激从醉酒中苏醒,而不改变乙醇代谢。缺乏 FGF21 的小鼠比野生型同窝仔需要更长的时间来恢复它们的翻正反射和平衡,以应对乙醇暴露。相反,药物 FGF21 的给药减少了小鼠从乙醇引起的无意识和共济失调中恢复所需的时间。FGF21 没有对抗氯胺酮、地西泮或戊巴比妥引起的镇静作用,表明其对乙醇的特异性。FGF21 通过直接激活蓝斑核区域的去甲肾上腺素能神经元来介导其抗中毒作用,蓝斑核区域调节觉醒和警觉性。这些结果表明,这种 FGF21 肝脑途径的进化是为了防止乙醇引起的中毒,并且它可能被用于治疗急性酒精中毒的药物靶向。