Faculty Opinions recommendation of Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H3 receptor antagonists.

2018 ◽  
Author(s):  
Andrew Kruse
Keyword(s):  
Receptor Antagonists ◽  
Histamine H3 Receptor ◽  
Sigma 1 Receptor ◽  
Receptor Affinity ◽  
Receptor Kinetics ◽  
H3 Receptor ◽  
Sigma 1 ◽  
Drug Receptor ◽  
Histamine H3

Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H3 receptor antagonists

2019 ◽  
Vol 144 ◽  
pp. 244-255 ◽  
Author(s):  
Darren M. Riddy ◽  
Anna E. Cook ◽  
David M. Shackleford ◽  
Tracie L. Pierce ◽  
Elisabeth Mocaer ◽  
...  
Keyword(s):  
Receptor Antagonists ◽  
Histamine H3 Receptor ◽  
Sigma 1 Receptor ◽  
Receptor Affinity ◽  
Receptor Kinetics ◽  
H3 Receptor ◽  
Sigma 1 ◽  
Drug Receptor ◽  
Histamine H3

Dual-targeting approach on histamine H3 and sigma-1 receptor ligands as promising pharmacological tools in the treatment of CNS-linked disorders

2020 ◽  
Vol 27 ◽  
Author(s):  
Katarzyna Szczepańska ◽  
Kamil J. Kuder ◽  
Katarzyna Kieć-Kononowicz
Keyword(s):  
G Protein Coupled Receptors ◽  
Receptor Ligands ◽  
Receptor Antagonists ◽  
Histamine H3 Receptor ◽  
Sigma 1 Receptor ◽  
Biological Targets ◽  
H3 Receptor ◽  
Sigma 1 ◽  
G Protein Coupled ◽  
Histamine H3

: With the recent market approval of Pitolisant (Wakix®), the interest in clinical application for novel multifunctional histamine H3 receptor antagonists has clearly increased. Several combinations of different H3R pharmacophores with pharmacophoric elements of other G-protein coupled receptors, transporters or enzymes have been synthesized by numerous pharmaceutical companies and academic institutions. Since central nervous system disorders are characterized by diverse physiological dysfunctions and deregulations of a complex network of signaling pathways, optimal multipotent drugs should simultaneously and peculiary modulate selected groups of biological targets. Interestingly, very recent studies have shown that some of clinically evaluated histamine H3 receptor antagonists possess nanomolar affinity for sigma-1 receptor binding sites, suggesting that this property might play a role in their overall efficacy. The sigma-1 receptor, unusual and yet obscure protein, is supposed to be involved in numerous CNS pathologies through neuroprotection and neuroplasticity. These two different biological structures, histamine H3 and sigma-1 receptors, combined can represent potential fruitful target for therapeutic developments in tackling numerous human diseases.

ChemInform Abstract: 4-Chlorobenzyl Sulfonamide and Sulfamide Derivatives of Histamine Homologues: The Design of Potent Histamine H3 Receptor Antagonists.

ChemInform ◽  
2010 ◽  
Vol 31 (8) ◽  
pp. no-no
Author(s):  
Matthew J. Tozer ◽  
Ildiko M. Buck ◽  
Tracey Cooke ◽  
S. Barret Kalindjian ◽  
Iain M. McDonald ◽  
...  
Keyword(s):  
Receptor Antagonists ◽  
Histamine H3 Receptor ◽  
H3 Receptor ◽  
Derivatives Of ◽  
Histamine H3

ChemInform Abstract: Substituted N-Phenylcarbamates as Histamine H3 Receptor Antagonists with Improved in vivo Potency.

ChemInform ◽  
2010 ◽  
Vol 31 (24) ◽  
pp. no-no
Author(s):  
S. Reidemeister ◽  
H. Stark ◽  
X. Ligneau ◽  
C. R. Ganellin ◽  
J.-C. Schwartz ◽  
...  
Keyword(s):  
Receptor Antagonists ◽  
Histamine H3 Receptor ◽  
H3 Receptor ◽  
Histamine H3

Piperidine-Containing Histamine H3 Receptor Antagonists of the Carbamate Series: The Influence of the Additional Ether Functionality

ChemInform ◽  
2003 ◽  
Vol 34 (16) ◽  
Author(s):  
D. Lazewska ◽  
K. Kiec-Kononowicz ◽  
H. H. Pertz ◽  
S. Elz ◽  
H. Stark ◽  
...  
Keyword(s):  
Receptor Antagonists ◽  
Histamine H3 Receptor ◽  
H3 Receptor ◽  
Histamine H3

Keynote review: Histamine H3 receptor antagonists reach out for the clinic

2005 ◽  
Vol 10 (23-24) ◽  
pp. 1613-1627 ◽  
Author(s):  
Sylvain Celanire ◽  
Maikel Wijtmans ◽  
Patrice Talaga ◽  
Rob Leurs ◽  
Iwan J.P. de Esch
Keyword(s):  
Receptor Antagonists ◽  
Histamine H3 Receptor ◽  
H3 Receptor ◽  
Histamine H3
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