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Molecular basis for the selective interaction of synthetic agonists with the human histamine H1-receptor compared with the guinea-pig H1-receptor

Strasser, Andrea ; Wittmann, Hans-Joachim ; Kunze, Marc ; Elz, Sigurd ; Seifert, Roland


Previous studies revealed that phenylhistamines and histaprodifens possess higher potency and affinity at guinea pig histamine H(1)-receptor (gpH(1)R) than at human histamine H(1)-receptor (hH(1)R). However, we recently identified an imidazolylpropylguanidine [N(1)-(3-cyclohexylbutanoyl)-N(2)-[3-(1H-imidazol-4-yl)-propyl]guanidine (UR-AK57)] with higher potency and efficacy at hH(1)R compared ...


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