KSK19 - Novel Histamine H3 Receptor Ligand Reduces Body Weight in Diet Induced Obese Mice

作者: Magdalena Kotańska , Kamil Mika , Karolina Reguła , Katarzyna Szczepańska , Małgorzata Szafarz

DOI: 10.1016/J.BCP.2019.07.006

关键词:

摘要: Aims Histamine H3 receptors ligands act anorectic by blocking the autoreceptors in CNS, that results increased synthesis and disinhibition of histamine release. further influencing H1 participates leptin-dependent inhibition food intake. It also affects peripheral metabolism increasing white adipose tissue lipolysis. Thus, such as KSK19 with significant antagonistic properties at receptor might serve an useful treatment for obesity. Materials methods To induce obesity, female CD-1 mice were fed a high-fat diet 14 weeks. The test compound doses 10 or 15 mg/kg, i.p. was administrated 21 days. Glucose insulin tolerance tests performed beginning week 15. At end study, amount intraperitoneal fat pads, AlAT, IL-6 TNF-α plasma levels determined. Results Animals treated dose mg/kg showed significantly less weight gain, than from control group. use days obese improved glucose resistance. In tested did not affect locomotor activity neither lean nor after single administration, but spontaneous during three hour twentieth administrations. Conclusion is strong, selective antagonist favorable influence on body multiple administration mg/kg. Moreover it improves tolerance.

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