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Synthesis and pharmacological characterization of new histamine H1-/H4-receptor ligands derived from the atypical antipsychotic drug Clozapine

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Gobleder, Susanne
Date of publication of this fulltext: 25 May 2016 11:51

Abstract (English)

The combined application of mepyramine (H1R-antagonist) and JNJ7777120 (H4R-antagonist) evoked a synergistic inhibitory effect on the eosinophil accumulation in the bronchoalveolar lavage fluid in the acute murine asthma model, pointing out that the H1R as well as the H4R is involved in type-I-allergic diseases. Molecules bearing pharmacophores that address both receptors could therefore be ...


Translation of the abstract (German)

Die gemeinsame Applikation von Mepyramin (H1-Antagonist) und JNJ7777120 (H4-Antagonist) bewirkte einen synergistisch-inhibitorischen Effekt auf die Ansammlung der Eosinophilen in der bronchoalveolären Lavage im akuten Asthma Modell an der Maus, was darauf hinweist, dass sowohl der H1R als auch der H4R an Typ-I-Allergien beteiligt ist. Moleküle die Pharmakophore für diese beiden Rezeptoren ...


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