In vivo binding properties of non‐sedating antihistamines to CNS histamine receptors | Zendy

McQuade Robert D. | Zendy; Richlan Kimberly | Zendy; Duffy Ruth A. | Zendy; Chipkin Richard E. | Zendy; Barnett Allen | Zendy

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In vivo binding properties of non‐sedating antihistamines to CNS histamine receptors

Author(s) -

McQuade Robert D.,

Richlan Kimberly,

Duffy Ruth A.,

Chipkin Richard E.,

Barnett Allen

Publication year - 1990

Publication title -

drug development research

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.582

H-Index - 60

eISSN - 1098-2299

pISSN - 0272-4391

DOI - 10.1002/ddr.430200305

Subject(s) - terfenadine , mepyramine , loratadine , astemizole , in vivo , pharmacology , histamine h1 receptor , histamine , cetirizine , chemistry , antihistamine , histamine h1 antagonists , diphenhydramine , receptor , antagonist , medicine , biochemistry , biology , microbiology and biotechnology

A series of antihistamines were examined for their ability to inhibit the in vivo binding of 3 H‐mepyramine to mouse brain membranes. All of the seven antihistamines tested inhibited the in vitro binding of 3 H‐mepyramine, but loratadine and terfenadine were the only compounds which did not cause an inhibition of the in vivo binding. Conversely, diphenhydramine, chlorpheniramine, astemizole, mequitazine, and cetirizine all resulted in a significant ( P < 0.05) decrease in the binding of 3 H‐mepyramine, in vivo. These results suggest that loratadine and terfenadine are antihistamines which are unable to cross the blood‐brain barrier and therefore possess a low sedative liability.

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