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|Title:||Multiple Targeting Approaches on Histamine H3 Receptor Antagonists||Authors:||Khanfar, Mohammad A
|Keywords:||GPCR; NO; enzymes; histamine; multiple targeting; transporter||Issue Date:||2016||Project:||None||Journal:||FRONTIERS IN NEUROSCIENCE||Abstract:||
With the very recent market approval of pitolisant (Wakix®), the interest in clinical applications of novel multifunctional histamine H3 receptor antagonists has clearly increased. Since histamine H3 receptor antagonists in clinical development have been tested for a variety of different indications, the combination of pharmacological properties in one molecule for improved pharmacological effects and reduced unwanted side-effects is rationally based on the increasing knowledge on the complex neurotransmitter regulations. The polypharmacological approaches on histamine H3 receptor antagonists on different G-protein coupled receptors, transporters, enzymes as well as on NO-signaling mechanism are described, supported with some lead structures.
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