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Chlorpheniramine plasma concentration and histamine H1-receptor occupancy*

Clinical Pharmacology & Therapeutics, 1995
The 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.
Paul Likhari   +4 more
openaire   +3 more sources

Site-directed mutagenesis of the histamine H1-receptor reveals a selective interaction of asparagine207 with subclasses of H1-receptor agonists.

Biochemical and Biophysical Research Communications - BBRC, 1994
In this study we investigated the role of the threonine203 and the asparagine207 residues in the fifth transmembrane domain of the guinea-pig histamine H1-receptor by site-directed mutagenesis to non-functional alanines.
R. Leurs   +4 more
semanticscholar   +1 more source

Pharmacokinetic Optimisation of Histamine H1-Receptor Antagonist Therapy

Clinical Pharmacokinetics, 1991
Second-generation, relatively nonsedating histamine H1-receptor antagonists (H1-RA) are extensively used worldwide for the symptomatic treatment of allergic rhinoconjunctivitis and chronic urticaria. Information about the pharmacokinetics and pharmacodynamics of these medications, while still incomplete, is now sufficient to permit optimisation of ...
Keith J. Simons, F. Estelle, R. Simons
openaire   +3 more sources

Antagonism of central histamine H1 receptors by antipsychotic drugs

European Journal of Pharmacology, 1978
The activity of 8 widely antipsychotic drugs as antagonists of central histamine H1 receptors was determined from the inhibition of the binding of 3H-mepyramine to a membrane fraction from guinea-pig brain. The phenothiazines examined, clorpromazine, fluphenazine, thioridazine and trifluoperazine, were all potent H1 antagonists.
Michael Young, Stephen J. Hill
openaire   +3 more sources

Clinical comparison of histamine H1–receptor antagonist drugs

Journal of Allergy and Clinical Immunology, 1996
Nearly 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.
openaire   +2 more sources

Histamine H1- and H2-receptors in coronary arteries of pigs

Agents and Actions, 1979
Histamine exerts its action in smooth muscle via in two types of receptors. In coronary arteries of pigs both types of receptors are also involved in responses to histamine. Histamine initiates by an interaction with H1-receptors a contraction and with H2-receptors a relaxation.
I. Paegelow, M. Hagen
openaire   +2 more sources

Histamine H1 receptors in the brain and spinal cord of the cat

Brain Research, 1982
The regional distribution of histamine H1 receptors in the feline brain and spinal cord was determined in vitro using the radioactively labeled histamine H1 antagonist, [3H]pyrilamine. This distribution of H1 receptors, which was different from that reported for other species, was highest in the hypothalamus and mammillary bodies.
Tony L. Yaksh   +2 more
openaire   +3 more sources

3. Molecular and chemical aspects of the histamine receptors

Inflammation Research, 2005
S Yoshimura   +7 more
openaire   +3 more sources

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