Results 261 to 270 of about 467,605 (318)
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Histamine receptors, agonists, and antagonists in health and disease
Handbook of Clinical Neurology, 2021Histamine in the brain is produced by a group of tuberomamillary neurons in the posterior hypothalamus and a limited number of mast cells in different parts of the brain. Four G-protein-coupled receptors mediate the effects of histamine. Two of these receptors, H3 and H4 receptors, are high-affinity receptors in the brain and immune system ...
P. Panula
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INHIBITION OF ACETYLCHOLINESTERASE BY HISTAMINE AGONISTS AND ANTAGONISTS
Clinical and Experimental Pharmacology and Physiology, 1985SUMMARY1. The histamine H1 and/or H2‐receptor agonists showed weak acetylcholinesterase inhibitory activity. Their dissociation constants (Kis and/or Kii) were 2‐methyl histamine (Kis= 1751 μmol/1, s.e. = 163) < 4‐methyl histamine (Kis= 3551 μmol/1, s.e. = 414) < dimaprit (Kis= 2931 μmol/1, s.e. = 605; Kii= 3668 μmol/1, s.e. = 901) < histamine
Lee, H.S., Cheah, L.S., Gwee, M.C.E.
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Histamine H4 receptor agonists
Bioorganic & Medicinal Chemistry Letters, 2010Since its discovery 10 years ago the histamine H(4) receptor (H(4)R) has attracted attention as a potential drug target, for instance, for the treatment of inflammatory and allergic diseases. Potent and selective ligands including agonists are required as pharmacological tools to study the role of the H(4)R in vitro and in vivo.
Patrick, Igel +2 more
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A modulation of the anaphylactic basophil histamine release by selective H2 histamine agonists
Agents and Actions, 1981Two selective H2-histamine agonists, dimaprit and impromidine, have been tested for their action on histamine release from human basophils and rat mast cells. IgE-mediated basophil histamine release was inhibited by stimulation of histamine H2-receptors. However, differences between the actions of both dimaprit and impromidine were noticed.
W, Kazimierczak +2 more
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Histamine H3-Receptor Inverse Agonists as Novel Antipsychotics
Central Nervous System Agents in Medicinal Chemistry, 2009Schizophrenia (SZ) that is resistant to treatment with dopamine (DA) D2 antagonists may involve changes other than those in the dopaminergic system. Recently, histamine (HA), which regulates arousal and cognitive functions, has been suggested to act as a neurotransmitter in the central nervous system.
C. Ito
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Interactions of Histamine H1-Receptor Agonists and Antagonists with the Human Histamine H4-Receptor
Molecular Pharmacology, 2009The human histamine H(4)-receptor (hH(4)R) possesses high constitutive activity and, like the human H(1)-receptor (hH(1)R), is involved in the pathogenesis of type-I allergic reactions. The study aims were to explore the value of dual H(1)/H(4)R antagonists as antiallergy drugs and to address the question of whether H(1)R ligands bind to hH(4)R.
Karl-Friedrich, Deml +4 more
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Chemical differentiation of histamine H1- and H2-receptor agonists
Journal of Medicinal Chemistry, 1975Histamine exists predominantly as the NT-H tautomer of the monocation (IIa) at a physiological pH of 7.4 and structure-activity studies indicate that this tautomer is likely to be the pharmacologically active species for both H1 and H2 receptors. Effective H2-receptor agonists appear to require a prototropic tautomeric system whereas H1-receptor ...
G J, Durant, C R, Ganellin, M E, Parsons
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Histamine H3 Receptor Agonists
Mini-Reviews in Medicinal Chemistry, 2004The SAR of H3 ligands has been difficult to evaluate because of species differences, multiple isoforms and constitutive activity, among other complicating factors. A review is given of the sometimes-conflicting affinity, activity and efficacy data of H3 agonists that has been described in literature to date.
I J P, De Esch, K J, Belzar
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Cardiac Effects of Novel Histamine H2 Receptor Agonists
The Journal of Pharmacology and Experimental Therapeutics, 2021In an integrative approach, we studied cardiac effects of recently published novel H2 receptor agonists in the heart of mice that overexpress the human H2 receptor (H2-TG mice) and littermate wild type (WT) control mice and in isolated electrically driven muscle preparations from patients undergoing cardiac surgery.
Ulrich, Gergs +11 more
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The Evolution of Histamine H3 Antagonists/Inverse Agonists
Current Topics in Medicinal Chemistry, 2011Evan P. Lebois +2 more
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