Mepyramine–JNJ7777120-hybrid compounds show high affinity to hH 1 R, but low affinity to hH 4 R

E Wagner, HJ Wittmann, S Elz, A Strasser

Index: Wagner, Eva; Wittmann, Hans-Joachim; Elz, Sigurd; Strasser, Andrea Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 21 p. 6274 - 6280

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Citation Number: 7

Abstract

In literature, a synergism between histamine H1 and H4 receptor is discussed. Furthermore, it was shown, that the combined application of mepyramine, a H1 antagonist and JNJ7777120, a H4 receptor ligand leads to a synergistic effect in the acute murine asthma model. Thus, the aim of this study was to develop new hybrid ligands, containing one H1 and one H4 pharmacophor, connected by an appropriate spacer, in order to address both, ...