Results 271 to 280 of about 467,605 (318)

New selective histamine H1 agonists

Pharmaceutisch Weekblad, 1990
In this article the synthesis and histaminergic H1 activity of a series of substituted 2-phenylhistamines are described. It appeared that substitution of the phenyl ring of these compounds influences the H1 activity substantially. In general, substitution in para position causes a decrease in H1 activity.
J G, Koper, A, Van der Vliet, H, Van der Goot, H, Timmerman   +3 more
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Developments in histamine H1-receptor agonists

1995
The story of histamine started in the early 1900’s with the fundamental investigations of Dale et al. [l–3], which recognized the remarkable physiological behavior of this biogenic amine. Scientific progress over the past decades has proved that histamine interacts with specific histamine receptors as a neurotransmitter and nearly all mammalian tissues
V, Zingel, C, Leschke, W, Schunack
openaire   +2 more sources

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
openaire   +2 more sources

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
openaire   +2 more sources

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
openaire   +1 more source

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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Amselamine, a new selective histamine H2-receptor agonist

Bioorganic & Medicinal Chemistry Letters, 1994
Abstract The synthesis of amselamine (2-amino-5(2-aminoethyl)-4-methyl-1,3-selenazole), a potent histamine H2-agonist, has been described. At the guinea pig right atrium amselamine revealed to be slightly more active than its sulfur analogue amthamine and histamine. Moreover negligible effects on H1 and H3-receptors were observed.
Henk van der Goot, John Ch. Eriks, Rob Leurs, Hendrik Timmerman   +3 more
openaire   +1 more source

The selective histamine H1-receptor agonist 2-(3-trifluoromethylphenyl)histamine increases waking in the rat

European Neuropsychopharmacology, 1994
The effects of the selective histamine H1-receptor agonist, 2-(3-trifluoromethylphenyl)histamine, were studied in rats implanted with electrodes for chronic sleep recordings. 2-(3-Trifluoromethylphenyl)histamine (80-120 micrograms) injected into the left lateral ventricle increased wakefulness, whereas slow wave sleep was reduced.
J M, Monti, H, Jantos, C, Leschke, S, Elz, W, Schunack   +4 more
openaire   +2 more sources