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Pharmacological profile of astemizole-derived compounds at the histamine H1 and H4 receptor - H1/H4 receptor selectivity

Wager, Eva ; Wittmann, Hans-Joachim ; Elz, Sigurd ; Strasser, Andrea



Abstract

Astemizole, a H1R antagonist shows high affinity to the histamine H1 receptor but only a moderate affinity to the histamine H4 receptor. This study aims to modify the astemizole to keep high affinity to the histamine H1 receptor and to increase affinity to the histamine H4 receptor. Therefore, 13 astemizole-derived compounds and astemizole-JNJ7777120-derived hybrid compounds were synthesized and ...

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