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.

Khanfar, M.A., Affini, A., Lutsenko, K., Nikolic, K., Butini, S., Stark, H. (2016). Multiple Targeting Approaches on Histamine H3 Receptor Antagonists. FRONTIERS IN NEUROSCIENCE, 10, 201 [10.3389/fnins.2016.00201].

Multiple Targeting Approaches on Histamine H3 Receptor Antagonists

BUTINI, STEFANIA;
2016-01-01

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.
2016
Khanfar, M.A., Affini, A., Lutsenko, K., Nikolic, K., Butini, S., Stark, H. (2016). Multiple Targeting Approaches on Histamine H3 Receptor Antagonists. FRONTIERS IN NEUROSCIENCE, 10, 201 [10.3389/fnins.2016.00201].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/995504
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