Multiple Targeting Approaches on Histamine H-3 Receptor Antagonists

2016
Authors
Khanfar, Mohammad A.Affini, Anna
Lutsenko, Kiril
Nikolić, Katarina

Butini, Stefania

Stark, Holger

Article (Published version)
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Show full item recordAbstract
With the very recent market approval of pitolisant (Wakix (R)), the interest in clinical applications of novel multifunctional histamine H-3 receptor antagonists has clearly increased. Since histamine H-3 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 H-3 receptor antagonists on different G-protein coupled receptors, transporters, enzymes as well as on NO-signaling mechanism are described, supported with some lead structures.
Source:
Frontiers in Neuroscience, 2016, 10Publisher:
- Frontiers Media Sa, Lausanne
Funding / projects:
- EU COST Action CA 15135
- EU COST Action CM 1103
- EU COST Action CM 1207
- DEG - INST 208/664-1 FUGG
- DEG - Ol16112039
DOI: 10.3389/fnins.2016.00201
ISSN: 1662-453X
PubMed: 27303254
WoS: 000376632300001
Scopus: 2-s2.0-84973575248
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PharmacyTY - JOUR AU - Khanfar, Mohammad A. AU - Affini, Anna AU - Lutsenko, Kiril AU - Nikolić, Katarina AU - Butini, Stefania AU - Stark, Holger PY - 2016 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2547 AB - With the very recent market approval of pitolisant (Wakix (R)), the interest in clinical applications of novel multifunctional histamine H-3 receptor antagonists has clearly increased. Since histamine H-3 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 H-3 receptor antagonists on different G-protein coupled receptors, transporters, enzymes as well as on NO-signaling mechanism are described, supported with some lead structures. PB - Frontiers Media Sa, Lausanne T2 - Frontiers in Neuroscience T1 - Multiple Targeting Approaches on Histamine H-3 Receptor Antagonists VL - 10 DO - 10.3389/fnins.2016.00201 ER -
@article{ author = "Khanfar, Mohammad A. and Affini, Anna and Lutsenko, Kiril and Nikolić, Katarina and Butini, Stefania and Stark, Holger", year = "2016", abstract = "With the very recent market approval of pitolisant (Wakix (R)), the interest in clinical applications of novel multifunctional histamine H-3 receptor antagonists has clearly increased. Since histamine H-3 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 H-3 receptor antagonists on different G-protein coupled receptors, transporters, enzymes as well as on NO-signaling mechanism are described, supported with some lead structures.", publisher = "Frontiers Media Sa, Lausanne", journal = "Frontiers in Neuroscience", title = "Multiple Targeting Approaches on Histamine H-3 Receptor Antagonists", volume = "10", doi = "10.3389/fnins.2016.00201" }
Khanfar, M. A., Affini, A., Lutsenko, K., Nikolić, K., Butini, S.,& Stark, H.. (2016). Multiple Targeting Approaches on Histamine H-3 Receptor Antagonists. in Frontiers in Neuroscience Frontiers Media Sa, Lausanne., 10. https://doi.org/10.3389/fnins.2016.00201
Khanfar MA, Affini A, Lutsenko K, Nikolić K, Butini S, Stark H. Multiple Targeting Approaches on Histamine H-3 Receptor Antagonists. in Frontiers in Neuroscience. 2016;10. doi:10.3389/fnins.2016.00201 .
Khanfar, Mohammad A., Affini, Anna, Lutsenko, Kiril, Nikolić, Katarina, Butini, Stefania, Stark, Holger, "Multiple Targeting Approaches on Histamine H-3 Receptor Antagonists" in Frontiers in Neuroscience, 10 (2016), https://doi.org/10.3389/fnins.2016.00201 . .