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Molecular determinants for the high constitutive activity of the human histamine H4 receptor: Functional studies on orthologs and mutants

Wifling, David ; Löffel, Karolin ; Nordemann, Uwe ; Strasser, Andrea ; Bernhardt, Günther ; Dove, Stefan ; Seifert, Roland ; Buschauer, Armin



Abstract

BACKGROUND AND PURPOSE & para;& para;Some histamine H-4 receptor ligands act as inverse agonists at the human H-4 receptor (hH(4)R), a receptor with exceptionally high constitutive activity, but as neutral antagonists or partial agonists at the constitutively inactive mouse H-4 receptor (mH(4)R) and rat H-4 receptor (rH(4)R). To study molecular determinants of constitutive activity, H-4 receptor ...

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