نتایج جستجو برای: histamine h3 receptor
تعداد نتایج: 614993 فیلتر نتایج به سال:
Hemodynamic responses to histamine were investigated in the anesthetized rabbit. Intravenous injections of histamine induced dose-dependent decreases in systemic arterial pressure that were blocked by the H1-receptor antagonist pyrilamine but not the H2 antagonist cimetidine. Injections of histamine and the H1 agonist 6-[2-(4-imidazolyl)ethylamine]- N-(4-trifuormethylphenyl)-heptanecardoxamide ...
Abbreviations: A1R: Adenosine A1 Receptor; A2AR: Adenosine A2A Receptor; A2BR: Adenosine A2B Receptor; A3R: Adenosine A3 Receptor; Cpd: Compound; D2R: Dopamine D2 Receptor; Emax: Efficacy; gp: Guinea-pig; GPCR: G-Protein Coupled Receptor; h: Human; H1R: Histamine H1 Receptor; H3R: Histamine H3 Receptor; r: rat; 5-HT1AR: Serotonine 5-HT1A Receptor; βR: β-Adrenergic Receptors; β2R: Adrenergic β2 ...
We studied the actions of Sch 50971, a novel histamine H3 receptor agonist, in an experimental neurogenic model of migraine and characterized its sedative and respiratory actions. Sch 50971 (i.v. and p.o) inhibited plasma protein extravasation in the dura mater of guinea pigs after electrical stimulation of the trigeminal ganglia. The minimum effective doses of Sch 50971 were 3.0 mg/kg i.v. and...
Histamine H3 receptor antagonists are being developed to treat a variety of neurological and cognitive disorders that may be ameliorated by enhancement of central neurotransmitter release. Here, we present the in vitro pharmacological and in vivo pharmacokinetic profiles for the nonimidazole, benzofuran ligand ABT-239 [4-(2-{2-[(2R)-2-methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile] and ...
We have used alanine scanning mutagenesis to identify residues in transmembrane domain 5 of the histamine H3 receptor that are important for agonist binding. All of the mutants generated were functionally expressed as demonstrated by their ability to bind [(125)I]iodoproxyfan with comparable affinity to the wild-type receptor and their ability to inhibit forskolin-stimulated cAMP formation when...
restraint-induced stress (rs) increases histamine concentration in the brain. there is no previous report regarding the role of histamine receptors in immunomodulatory effect of rs. in the present study the role of brain histamine receptors on reduction of humoral and cellular immune function induced by rs was evaluated. for this purpose male wistar rats (200-250 g) were immunized with sheep re...
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