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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.