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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: Some histamine H4 receptor (H4R) ligands act as inverse agonists at the human H4R (hH4R), a receptor with exceptionally high constitutive activity, but as neutral antagonists or partial agonists at the constitutively inactive mouse H4R (mH4R) and rat H4R (rH4R). To study molecular determinants of constitutive activity, H4R reciprocal mutants were constructed: single ...

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