Department of Pharmacological Screening, Jagiellonian University Medical College, Medyczna 9, PL 30-688 Cracow, Poland.
Department of Pharmacokinetics and Physical Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Krakow, Poland.
Biomed Pharmacother. 2021 Sep;141:111892. doi: 10.1016/j.biopha.2021.111892. Epub 2021 Jul 3.
It is important to search for a promising therapeutic target or small molecules that can control excessive eating since limiting the intake of foods, especially tasty ones, could be effective in the treatment or prevention of obesity. Some studies indicate betahistine as an unique drug having the ability to ameliorate, for example, antipsychotic-induced weight gain. This study aimed to determine whether repeated administration of betahistine (histamine H1R agonist and H3R antagonist) could be beneficial in reducing the intake of tasty foods or the body's response to overeating via mechanisms such as by influencing the levels of hormones involved in the regulation of food intake or the levels of selected metabolic parameters. Studies were performed in the excessive eating model in rats, which perfectly illustrates the harmful high-caloric intake from freely available tasty products rich in sugar and fat. Our results indicated that repeated administration of betahistine to rats caused lower gain of body mass compared to the control rats fed palatable feed. Interestingly, betahistine treatment increased the consumption of cheese, which is a source of histamine. Although betahistine did not prevent the development of metabolic disorders, such as reduced glucose tolerance, in test animals, it significantly increased the level of high-density lipoprotein cholesterol, which could certainly be considered beneficial. Further studies should be conducted to investigate the effect of repeated administration of betahistine on satiety, gastrointestinal disorders, and the preference for histamine-containing foods.
寻找有前途的治疗靶点或小分子来控制过度进食非常重要，因为限制食物摄入，尤其是美味食物的摄入，可能对肥胖的治疗或预防有效。一些研究表明，倍他司汀是一种独特的药物，具有改善例如抗精神病药引起的体重增加的能力。本研究旨在确定重复给予倍他司汀（组胺 H1R 激动剂和 H3R 拮抗剂）是否通过影响参与食物摄入调节的激素水平或选择代谢参数水平等机制有益于减少美味食物的摄入或身体对暴饮暴食的反应。在大鼠过度进食模型中进行了研究，该模型完美地说明了从自由获取的富含糖和脂肪的美味产品中摄入高热量的危害性。我们的研究结果表明，与喂食美味饲料的对照组大鼠相比，重复给予大鼠倍他司汀可降低体重增加。有趣的是，倍他司汀治疗增加了奶酪的消耗，奶酪是组胺的来源。尽管倍他司汀并没有预防试验动物发生代谢紊乱，如葡萄糖耐量降低，但它显著增加了高密度脂蛋白胆固醇的水平，这肯定可以被认为是有益的。应进一步进行研究，以调查重复给予倍他司汀对饱腹感、胃肠道紊乱和对含组胺食物的偏好的影响。
