Results 171 to 180 of about 38,061 (191)
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Histamine receptors, agonists, and antagonists in health and disease
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 ...
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Amselamine, a new selective histamine H2-receptor agonist
Bioorganic & Medicinal Chemistry Letters, 1994Abstract 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 +3 more
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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 +4 more
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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 +4 more
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H2 histaminic receptors in rat cerebral cortex. 3. Inhibition of [3H]histamine by H2 agonists
Biochemistry, 1985The binding of [3H]histamine to H2 receptors in homogenates of rat cerebral cortex is inhibited by 11 H2 agonists in a characteristic and unique manner. At low concentrations of the radioligand (less than 1.5 nM), the inhibitory profiles of individual agonists (A) are distinctly biphasic; specific binding is well described in most cases by the ...
G H, Steinberg +3 more
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A Novel Pyrrolidine Analog of Histamine as a Potent, Highly Selective Histamine H3 Receptor Agonist
Journal of Medicinal Chemistry, 1995Employing classical conformational analysis on a known H3 agonist, (R)-alpha-methylhistamine (1), a series of conformationally constrained H3 agonists were proposed and synthesized. Pyrrolidine (+/-)-4a, a compound proposed to mimic the anti-conformation of (R)-alpha-methylhistamine (1), was found to be a potent and selective H3 agonist.
N Y, Shih +9 more
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Discovery of novel steroidal histamine H3 receptor antagonists/inverse agonists
Bioorganic & Medicinal Chemistry Letters, 2017Emerging from an HTS campaign, novel steroid-based histamine H3 receptor antagonists were identified and characterized. Structural moieties of the hit compounds were combined to improve binding affinities which resulted in compound 4 as lead molecule.
Istvan, Ledneczki +11 more
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European Journal of Medicinal Chemistry, 1995
Summary In search for potential histamine H3-receptor agonists a series of mono- and dialkyl-substituted histamine derivatives was synthesized. All target compounds were tested in vitro for their agonist activity at H3-, H2-, and H1-receptors. Introduction of one ethyl or two methyl residues into histamine led to compounds with decreased histamine H3-
R Lipp +5 more
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Summary In search for potential histamine H3-receptor agonists a series of mono- and dialkyl-substituted histamine derivatives was synthesized. All target compounds were tested in vitro for their agonist activity at H3-, H2-, and H1-receptors. Introduction of one ethyl or two methyl residues into histamine led to compounds with decreased histamine H3-
R Lipp +5 more
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Die Pharmazie, 1993
Piperidinoalkyl-, morpholinoalkyl- or [(pyrid-2-yl)methylthio]alkyl-substituents were introduced into position 2 of the essential histamine structure. These 2-substituted histamine derivatives were prepared via reaction of imidate hydrochlorides in liquid ammonia under pressure with 1,3-dihydroxypropanone followed by a stepwise build-up of the side ...
V, Zingel, S, Elz, W, Schunack
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Piperidinoalkyl-, morpholinoalkyl- or [(pyrid-2-yl)methylthio]alkyl-substituents were introduced into position 2 of the essential histamine structure. These 2-substituted histamine derivatives were prepared via reaction of imidate hydrochlorides in liquid ammonia under pressure with 1,3-dihydroxypropanone followed by a stepwise build-up of the side ...
V, Zingel, S, Elz, W, Schunack
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Routes to Histamine H2‐Agonists
Quantitative Structure-Activity Relationships, 1992AbstractIn this paper the design, synthesis and primary biological testing of several new H2‐agonists are presented. The existing agonists dimaprit and impromidine have been used as starting points.Dimaprit seems to be the only member of its class which is an H2‐agonist; close analogues of dimaprit proved to be inactive as H2‐agonists.In impromidine ...
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The evolution of histamine H₃ antagonists/inverse agonists.
Current topics in medicinal chemistry, 2011This article describes our efforts along with recent advances in the development, biological evaluation and clinical proof of concept of small molecule histamine H₃ antagonists/inverse agonists. The H3 receptor is a presynaptic autoreceptor within the Class A GPCR family, but also functions as a heteroreceptor modulating levels of neurotransmitters ...
Evan P, Lebois +2 more
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