Results 161 to 170 of about 38,061 (191)

Design of histamine H3-receptor agonists and antagonists

European Journal of Drug Metabolism and Pharmacokinetics, 1994
The development of highly potent and selective ligands for the characterization of histamine H3-receptors is reviewed. In the field of agonists stereoselectively methylated derivatives of the natural ligand are found to have the desired pharmacodynamic properties. Pharmacokinetic properties could be improved by forming bioreversible azomethine prodrugs
W, Schunack, H, Stark
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Structure-Activity Relationships of Histamine H1-Receptor Agonists

Mini-Reviews in Medicinal Chemistry, 2004
Significant progress in the development of potent and selective histamine H1-receptor agonists has been achieved since 1990. Optimisation of the class of 2-phenylhistamines has furnished 2-[3-(trifluoromethyl)phenyl]histamine and its Nalpha-methyl derivative. The discovery of histaprodifen (2-[2-(3,3-diphenylpropyl)-1H-imidazol-4-yl]ethanamine) and the
Heinz H, Pertz, Sigurd, Elz, Walter, Schunack   +2 more
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Linking agonist binding to histamine H1 receptor activation

Nature Chemical Biology, 2005
G protein-coupled receptors (GPCRs) constitute a large and functionally diverse family of transmembrane proteins. They are fundamental in the transfer of extracellular stimuli to intracellular signaling pathways and are among the most targeted proteins in drug discovery.
Jongejan, Aldo, Bruysters, Martijn, Ballesteros, Juan A., Haaksma, Eric, Bakker, Remko A., Pardo, Leonardo, Leurs, Rob   +6 more
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A modulation of the anaphylactic basophil histamine release by selective H2 histamine agonists

Agents and Actions, 1981
Two 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, K, Szczepaniak, K, Bańkowska   +2 more
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Histamine analogues. 33rd communication: 2-phenylhistamines with high histamine H1-agonistic activity

European Journal of Medicinal Chemistry, 1990
Abstract 2-Phenylhistamines with various substituents at the phenyl ring were synthesized and the influence of substitution in ortho, meta or para position on histamine H1-agonistic activity was investigated. Compounds with high activity occurred in the meta phenyl series.
V Zingel, S Elz, W Schunack
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Visualization of Agonist-Induced Internalization of Histamine H2 Receptors

Biochemical and Biophysical Research Communications, 1995
Histamine H2 receptors were tagged at the N-terminus with the eight amino acid Flag epitope to allow the immunological identification of the receptor peptide with the monoclonal anti-Flag M2 antibody. The introduction of the epitope did not modify the binding of several H2 ligands to the H2 receptor, nor the ability of histamine to stimulate the H2 ...
M J, Smit, H, Timmerman, A E, Alewijnse, M, Punin, I, van den Nieuwenhof, J, Blauw, J, van Minnen, R, Leurs   +7 more
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Mesenteric vascular reactivity to histamine receptor agonists and antagonists

Digestive Diseases and Sciences, 1981
Response patterns of intestinal blood flow, oxygen extraction and consumption, blood flow distribution, and motility were assessed during intraarterial infusions of histamine, histamine after H1 or H2 blockade, dimaprit or dimaprit after H2 blockade. Histamine produced an initial peak response of blood flow with a slow decrease thereafter.
K M, Walus, J D, Fondacaro, E D, Jacobson   +2 more
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Chemical differentiation of histamine H1- and H2-receptor agonists

Journal of Medicinal Chemistry, 1975
Histamine 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 Inverse Agonists as Novel Antipsychotics

Central Nervous System Agents in Medicinal Chemistry, 2009
Schizophrenia (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.
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Interactions of Histamine H1-Receptor Agonists and Antagonists with the Human Histamine H4-Receptor

Molecular Pharmacology, 2009
The 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, Silke, Beermann, Detlef, Neumann, Andrea, Strasser, Roland, Seifert   +4 more
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