Academic literature on the topic 'Histamine H3 receptor ligands'

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Journal articles on the topic "Histamine H3 receptor ligands"

1

Wágner, Gábor, Tamara A. M. Mocking, Albert J. Kooistra, et al. "Covalent Inhibition of the Histamine H3 Receptor." Molecules 24, no. 24 (2019): 4541. http://dx.doi.org/10.3390/molecules24244541.

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Covalent binding of G protein-coupled receptors by small molecules is a useful approach for better understanding of the structure and function of these proteins. We designed, synthesized and characterized a series of 6 potential covalent ligands for the histamine H3 receptor (H3R). Starting from a 2-amino-pyrimidine scaffold, optimization of anchor moiety and warhead followed by fine-tuning of the required reactivity via scaffold hopping resulted in the isothiocyanate H3R ligand 44. It shows high reactivity toward glutathione combined with appropriate stability in water and reacts selectively
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2

Díaz, Néstor F., Héctor Flores-Herrera, Guadalupe García-López, and Anayansi Molina-Hernández. "Central Histamine, the H3-Receptor and Obesity Therapy." CNS & Neurological Disorders - Drug Targets 18, no. 7 (2019): 516–22. http://dx.doi.org/10.2174/1871527318666190703094846.

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The brain histaminergic system plays a pivotal role in energy homeostasis, through H1- receptor activation, it increases the hypothalamic release of histamine that decreases food intake and reduces body weight. One way to increase the release of hypothalamic histamine is through the use of antagonist/inverse agonist for the H3-receptor. Histamine H3-receptors are auto-receptors and heteroreceptors located on the presynaptic membranes and cell soma of neurons, where they negatively regulate the synthesis and release of histamine and other neurotransmitters in the central nervous system. Althoug
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3

Singh, Mahaveer, and Hemant R. Jadhav. "Histamine H3 Receptor Function and Ligands: Recent Developments." Mini Reviews in Medicinal Chemistry 13, no. 1 (2013): 47–57. http://dx.doi.org/10.2174/138955713804484695.

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4

Singh, Mahaveer, and Hemant R. Jadhav. "Histamine H3 Receptor Function and Ligands: Recent Developments." Mini-Reviews in Medicinal Chemistry 13, no. 1 (2012): 47–57. http://dx.doi.org/10.2174/1389557511307010047.

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5

Sander, Kerstin, Tim Kottke, Lilia Weizel, and Holger Stark. "Kojic Acid Derivatives as Histamine H3 Receptor Ligands." CHEMICAL & PHARMACEUTICAL BULLETIN 58, no. 10 (2010): 1353–61. http://dx.doi.org/10.1248/cpb.58.1353.

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6

Watanabe, Mizuki, Takaaki Kobayashi, Yoshihiko Ito, Shizuo Yamada, and Satoshi Shuto. "Conformational Restriction of Histamine with a Rigid Bicyclo[3.1.0]hexane Scaffold Provided Selective H3 Receptor Ligands." Molecules 25, no. 16 (2020): 3562. http://dx.doi.org/10.3390/molecules25163562.

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We designed and synthesized conformationally rigid histamine analogues with a bicyclo[3.1.0]hexane scaffold. All the compounds were selectively bound to the H3 receptor subtype over the H4 receptor subtype. Notably, compound 7 showed potent binding affinity and over 100-fold selectivity for the H3 receptors (Ki = 5.6 nM for H3 and 602 nM for H4). These results suggest that the conformationally rigid bicyclo[3.1.0]hexane structure can be a useful scaffold for developing potent ligands selective for the target biomolecules.
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7

Pallardo-Fernández, Iñigo, José Ramón Muñoz-Rodríguez, Carmen González-Martín, and Luis F. Alguacil. "Histamine H3 receptor gene variants associated with drug abuse in patients with cocaine use disorder." Journal of Psychopharmacology 34, no. 11 (2020): 1326–30. http://dx.doi.org/10.1177/0269881120961253.

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Background: Preclinical work revealed significant interactions between ligands of the histamine H3 receptor and different drugs of abuse. In the case of psychostimulants, the results reported are somewhat controversial and human data are still scarce, despite the fact that an inverse agonist of the H3 receptor (pitolisant) has reached the market after approval for the treatment of narcolepsy. Aims: We have studied associations between histamine H3 receptor gene variants and cocaine use disorder to increase the knowledge of the possible involvement of histamine H3 receptor in drug abuse. Method
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8

Kuder, Kamil J., Magdalena Kotańska, Katarzyna Szczepańska, et al. "Discovery of Potential, Dual-Active Histamine H3 Receptor Ligands with Combined Antioxidant Properties." Molecules 26, no. 8 (2021): 2300. http://dx.doi.org/10.3390/molecules26082300.

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In an attempt to find new dual acting histamine H3 receptor (H3R) ligands, we designed a series of compounds, structurally based on previously described in our group, a highly active and selective human histamine H3 receptor (hH3R) ligand KSK63. As a result, 15 obtained compounds show moderate hH3R affinity, the best being the compound 17 (hH3R Ki = 518 nM). Docking to the histamine H3R homology model revealed two possible binding modes, with key interactions retained in both cases. In an attempt to find possible dual acting ligands, selected compounds were tested for antioxidant properties. C
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9

Dimitriadou, V., A. Rouleau, M. Dam Trung Tuong, et al. "Functional Relationship between Mast Cells and C-Sensitive Nerve Fibres Evidenced by Histamine H3-Receptor Modulation in Rat Lung and Spleen." Clinical Science 87, no. 2 (1994): 151–63. http://dx.doi.org/10.1042/cs0870151.

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1. Mast cell populations in rat lung and spleen were characterized by the presence of two specific protease markers, rat mast cell protease I and II, using both histochemical and radioimmunoassay techniques. Three mast cell populations with different size, morphology and localization were found in lung and spleen and were identified according to the expression of rat mast cell protease I (RMCPI+) or rat mast cell protease II (RMCPII+) or of both proteases (RMCPI/II+). 2. All three mast cell types were in the vicinity of calcitonin-gene-related-peptide-immunoreactive (CGRP+) nerve fibres in con
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10

Amon, Michael, Xavier Ligneau, Jean-Claude Camelin, Isabelle Berrebi-Bertrand, Jean-Charles Schwartz, and Holger Stark. "Highly Potent Fluorescence-Tagged Nonimidazole Histamine H3 Receptor Ligands." ChemMedChem 2, no. 5 (2007): 708–16. http://dx.doi.org/10.1002/cmdc.200600270.

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