Biochemical Pharmacology 2019-Oct
KSK19 - Novel histamine H3 receptor ligand reduces body weight in diet induced obese mice.
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Keywords
Abstract
AIMS
Histamine H3 receptors ligands act anorectic by blocking the H3 autoreceptors in the CNS, that results in increased synthesis and disinhibition of histamine release. Histamine further influencing H1 receptors participates in the leptin-dependent inhibition of food intake. It also affects the peripheral metabolism by increasing white adipose tissue lipolysis. Thus, ligands such as KSK19 with significant antagonistic properties at the H3 receptor might serve as an useful treatment for obesity.CONCLUSION
KSK19 is a strong, selective histamine H3 receptor antagonist with a favorable influence on body weight after multiple administration at the dose of 15 mg/kg. Moreover it significantly improves glucose tolerance.