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Multiple Targeting Approaches on Histamine H-3 Receptor Antagonists

Thumbnail
2016
2545.pdf (3.499Mb)
Authors
Khanfar, Mohammad A.
Affini, Anna
Lutsenko, Kiril
Nikolić, Katarina
Butini, Stefania
Stark, Holger
Article (Published version)
Metadata
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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.
Source:
Frontiers in Neuroscience, 2016, 10
Publisher:
  • 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
[ Google Scholar ]
35
34
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/2547
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Pharmacy
TY  - 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 . .

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