Results 31 to 40 of about 41,179 (270)

Homogeneous, Real-Time NanoBRET Binding Assays for the Histamine H3 and H4 Receptors on Living Cells

Molecular Pharmacology, 2018
Receptor-binding affinity and ligand-receptor residence time are key parameters for the selection of drug candidates and are routinely determined using radioligand competition-binding assays.
Tamara A. M. Mocking, E. Verweij, H. Vischer, R. Leurs   +3 more
semanticscholar   +1 more source

A Novel Potent and Selective Histamine H3 Receptor Antagonist Enerisant: In Vitro Profiles, In Vivo Receptor Occupancy, and Wake-Promoting and Procognitive Effects in Rodents

Journal of Pharmacology and Experimental Therapeutics, 2020
Histamine H3 receptor antagonists/inverse agonists are known to enhance the activity of histaminergic neurons in the brain, thereby promoting arousal and cognition. Here, we report the in vitro and in vivo pharmacological profiles for a newly synthesized
N. Hino, Toshiyuki Marumo, Makiko Kotani, T. Shimazaki, Ayaka Kaku-Fukumoto, H. Hikichi, J. Karasawa, Yasumitsu Tomishima, H. Komiyama, Emi Tatsuda, D. Nozawa, Toshio Nakamura, S. Chaki   +12 more
semanticscholar   +1 more source

Histamine receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database [PDF]

, 2019
Histamine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Histamine Receptors [75, 163]) are activated by the endogenous ligand histamine. Marked species differences exist between histamine receptor orthologues [75]. The human and rat
Chazot, Paul, Cowart, Marlon, Fukui, Hiroyuki, Ganellin, C. Robin, Gutzmer, Ralf, Haas, Helmut L., Hill, Stephen J., Hills, Rebecca, Leurs, Rob, Levi, Roberto, Liu, Steve, Panula, Pertti, Schunack, Walter, Schwartz, Jean-Charles, Seifert, Roland, Shankley, Nigel P., Stark, Holger, Thurmond, Robin, Timmerman, Henk, Young, J. Michael   +19 more
core   +2 more sources

Quantification methods for brain imaging with novel and repurposed PET tracers [PDF]

, 2021
The number of people suffering from brain disorders is annually increasing. Knowledge about the molecular processes in the healthy and diseased brain is essential for a better understanding of disease conditions, treatment selection, and drug development.
Ghazanfari, Nafiseh
core   +1 more source

Review: Vascular Effects of Histamine [PDF]

, 2015
Four subtypes of receptors (HFour subtypes of receptors (H1, H2, H3 and H4) mediate the actions of histamine. In the vascular wall, the effects of histamine are mediated via H1 and H2 receptors and the actions are modulated by H3 receptor subtype located
Ebeigbe, AB, Talabi, OO
core   +2 more sources

M/F-Theory as Mf-Theory [PDF]

Rev. Math. Phys., Vol. 35, No. 10, 2350028 (2023), 2021
In the quest for mathematical foundations of M-theory, the "Hypothesis H" that fluxes are quantized in Cohomotopy theory, implies, on flat but possibly singular spacetimes, that M-brane charges locally organize into equivariant homotopy groups of spheres.
arxiv   +1 more source

Histamine H1 and H2 Receptor Antagonists Accelerate Skin Barrier Repair and Prevent Epidermal Hyperplasia Induced by Barrier Disruption in a Dry Environment [PDF]

, 2001
Keratinocytes have histamine H1 and H2 receptors, but their functions are poorly understood. To clarify the role of histamine receptors in the epidermis, we examined the effects of histamine receptor antagonists and agonists applied epicutaneously on the
Ashida, Yutaka, Denda, Mitsuhiro, Hirao, Tetsuji   +2 more
core   +1 more source

Histamine H3 receptors and its antagonism as a novel mechanism for antipsychotic effect: a current preclinical & clinical perspective.

International Journal of Health Sciences, 2016
Histamine H3 receptors are present as autoreceptors on histaminergic neurons and as heteroreceptors on nonhistaminergic neurones. They control the release and synthesis of histamine and several other key neurotransmitters in the brain.
Danish Mahmood
semanticscholar   +1 more source

Short photoperiod-induced decrease of histamine H3 receptors facilitates activation of hypothalamic neurons in the Siberian Hamster [PDF]

, 2009
Nonhibernating seasonal mammals have adapted to temporal changes in food availability through behavioral and physiological mechanisms to store food and energy during times of predictable plenty and conserve energy during predicted shortage.
Bamshad, Barrett, Barrett, Brown, C. K. Song, D. Spanswick, D. Wilson, Doi, Enriori, Franklin, Franklin, Garcia, Gottsch, Inagaki, J. G. Mercer, Jamali, Jamali, Leurs, Liu, M. van den Top, Malmlöf, Morgan, Morgan, Morton, Nakamura, Nilaweera, Ookuma, P. Barrett, P. J. Morgan, Panula, Pillot, Prendergast, Revel, Ross, Sakata, Sallmen, Sallmen, Schneider, Song, Spanswick, Spanswick, T. J. Bartness, Top, Tups, Viguié, Yoshimoto, Yoshimura   +46 more
core   +1 more source

Plasticity of histamine H3 receptor expression and binding in the vestibular nuclei after labyrinthectomy in rat [PDF]

, 2004
Background: In rat, deafferentation of one labyrinth (unilateral labyrinthectomy) results in a characteristic syndrome of ocular and motor postural disorders (e.g., barrel rotation, circling behavior, and spontaneous nystagmus). Behavioral recovery (e.g.,
Aarnisalo, Antti A., Karlstedt, Kaj, Lozada, Adrian F., Panula, Pertti, Stark, Holger   +4 more
core   +2 more sources