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Chlorpheniramine plasma concentration and histamine H1-receptor occupancy*
Clinical Pharmacology & Therapeutics, 1995The plasma concentration-response relationship of the antihistamine chlorpheniramine is poorly characterized. This study examined concurrently the concentrations of chlorpheniramine and presence of H1-receptor antagonist in plasma after administration of 8 mg chlorpheniramine in normal volunteers.
S U, Yasuda +4 more
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The roles of histamine H1 receptors on cognition
Inflammation Research, 2008Histamine neurons are located exclusively in the posterior hypothalamus, from where they project diffusely to all regions of brain. Neuronal histamine has been implicated in a variety of brain functions including wakefulness, learning and memory [1].
K, Yanai +3 more
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Genomic Cloning of the Rat Histamine H1 Receptor
Biochemical and Biophysical Research Communications, 1993A rat histamine H1 receptor gene which lacked introns was isolated from a rat genomic library using recently cloned bovine histamine H1 receptor cDNA [Yamashita et al., Proc. Natl. Acad. Sci. USA, 88, 11515-11519 (1991)]. The receptor protein deduced from this isolated gene was composed of 486 amino acids and showed characteristic properties of G ...
K, Fujimoto +5 more
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Interactions between adenosine A1- and histamine H1-receptors
International Journal of Biochemistry, 1994The interactions or "cross-talk" between adenosine A1-receptors and receptors coupled to phospholipase C (leading to the hydrolysis of inositol phospholipids) have been well documented in the literature. For example, activating the A1-receptor selectively potentiates the histamine H1-receptor stimulated hydrolysis of inositol phospholipids in guinea ...
J M, Dickenson, S J, Hill
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Histamine H1 receptors in the CNS
Trends in Pharmacological Sciences, 1979Abstract Despite the explosion of activity in the receptor labelling field in recent years, the histamine H 1 receptor has been surprisingly neglected. The synthesis of a suitable H-ligand has filled this gap and provided the means to obtain information on the properties and distribution of histamine H 1 receptors in the CNS.
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Characteristics of histamine H1 receptors on HeLa cells
European Journal of Pharmacology: Molecular Pharmacology, 1993The affinities of antagonists at histamine H1 receptors on HeLa cells have been determined from inhibition of histamine-induced inositol phosphate formation in intact and from inhibition of [3H]mepyramine binding to HeLa cell membranes. The dissociation constants of mepyramine and (+)-chlorpheniramine were similar to values for binding to H1 receptors ...
J A, Arias-Montaño, J M, Young
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Nonsedating histamine H1-receptor antagonists.
Clinical pharmacy, 1989The chemistry, pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosages of the nonsedating histamine H1-receptor antagonists terfenadine, astemizole, loratadine, and acrivastine are reviewed. Terfenadine and astemizole are chemically unrelated to histamine H1-receptor antagonists such as diphenhydramine and chlorpheniramine ...
K V, Mann, J P, Crowe, K J, Tietze
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Structure-Activity Relationships of Histamine H1-Receptor Agonists
Mini-Reviews in Medicinal Chemistry, 2004Significant 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 +2 more
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Clinical comparison of histamine H1–receptor antagonist drugs
Journal of Allergy and Clinical Immunology, 1996Nearly 40 million Americans have symptoms of upper respiratory allergies, making antihistamines among the most frequently used pharmacologic agents. Although there are mediators of allergic symptoms in addition to histamine, therapy for allergic rhinitis and urticaria has focused upon the use of antihistamines.
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