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2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor - H1/H4-receptor selectivity

Hammer, Sebastian ; Gobleder, Susanne ; Naporra, Franziska ; Wittmann, Hans-Joachim ; Elz, Sigurd ; Heinrich, Markus ; Strasser, Andrea


Distinct diaminopyrimidines, for example, 4-(4-methylpiperazin-1-yl)-5,6-dihydrobenzo[h]quinazolin-2-amine are histamine H-4 receptor (H4R) antagonists and show high affinity to the H4R, but only a moderate affinity to the histamine H-1 receptor (H1R). Within previous studies it was shown that an aromatic side chain with a distinct distance to the basic amine and aromatic core is necessary for ...


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