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Influence of the N-terminus and the E2-loop onto the binding kinetics of the antagonist mepyramine and the partial agonist phenoprodifen to H1R

Wittmann, Hans-Joachim ; Seifert, Roland ; Strasser, Andrea



Abstract

Numerous competitive radioligand binding studies revealed significant differences between human and guinea pig histamine H-1-receptors (hH(1)R and gpH(1)R), e.g. for the partial H1R agonist phenoprodifen. But until now, there are only few studies with regard to binding kinetics at H1R. Previous studies from our group revealed an influence of the exchange of N-terminus and E2-loop between hH(1)R ...

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