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Chemistry of Anti-H1 Histamine Antagonists

1978
In this Chapter a survey and discussion of the chemistry of compounds which antagonize the effects of histamine at H1 receptors are presented. Ellis (1969) has compiled an extensive list of reviews on histamine, 5-hydroxytryptamine, and their antagonists, several of which include some account of the chemical aspects of antihistaminics.
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A dual antagonist for chemokine CCR3 receptor and histamine H1 receptor

European Journal of Pharmacology, 2007
Eosinophilic chemokines and histamine play distinct but important roles in allergic diseases. Inhibition of both eosinophilic chemokines and histamine, therefore, is an ideal strategy for the treatment of allergic inflammation, such as asthma, allergic rhinitis, and atopic dermatitis.
Keiko, Suzuki   +7 more
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Nonsedating histamine H1-receptor antagonists.

Clinical pharmacy, 1989
The 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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The histamine H1-antagonist chlorpheniramine facilitates learning in aged rats

Neuroscience Letters, 1997
The effect of the histamine H1-receptor antagonist chlorpheniramine on inhibitory avoidance conditioning was investigated in 31-month-old rats, using a one-trial step-through avoidance task. Immediately after the learning trial, old rats were injected intraperitoneally with 5 or 10 mg/kg d-chlorpheniramine.
C, Frisch, R U, Hasenöhrl, J P, Huston
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Trifluoperazine inhibits phosphoinositide hydrolysis as a histamine H1-receptor antagonist

European Journal of Pharmacology: Molecular Pharmacology, 1991
In human astrocytoma cells (1321N1), trifluoperazine potently inhibited histamine-induced phosphoinositide hydrolysis, while it slightly inhibited carbachol-induced phosphoinositide hydrolysis. Trifluoperazine as well as diphenhydramine inhibited [3H]mepyramine binding in astrocytoma cell membranes with Ki values of 0.052 microM and 0.005 microM ...
N, Nakahata   +4 more
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Determination of some histamine H1-receptor antagonists in dosage forms

Journal of Pharmaceutical and Biomedical Analysis, 2002
Three simple and accurate methods are presented for determination of Cetirizine, Fexofenadine, Loratadine and Acrivastine in pure form and commercial dosage forms. The first method is based on the reaction of the above cited drugs with bromocresol purple dye to form ion-pair complex extractable with chloroform and subsequently measured ...
Azza A, Gazy   +4 more
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Studies on the mode of action of histamine H1- and H2-receptor antagonists on gastric histamine methyltransferase

Agents and Actions, 1973
Histamine methyltransferase from pig antrum mucosa was inhibited by 33 H1-receptor antagonists, by the H2-receptor antagonists burimamide and metiamide and by the burimamide analogue 5-methylburimamide, which did neither act on H1-nor on H2-receptors.
H, Barth, I, Niemeyer, W, Lorenz
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Antagonists of H1 Receptors of Histamine: Recent Developments

1991
In the previous handbook of this series on this topic (Casy 1978), attention was drawn to the fact that most compounds known at that time which effectively antagonized histamine at H1-receptor sites could be described by the general structure (1) Open image in new window (1)
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