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N1-(3-Cyclohexylbutanoyl)-N2-[3-(1H-imidazol-4-
yl)propyl]guanidine (UR-AK57), a Potent Partial Agonist for the Human Histamine H1- and H2- Receptors

Xie, Sheng-Xue ; Kraus, Anja ; Ghorai, Prasanta ; Ye, Qi-Zhuang ; Elz, Sigurd ; Buschauer, Armin ; Seifert, Roland
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Date of publication of this fulltext: 05 Aug 2009 13:21


Abstract

Both the histamine H1-receptor (H1R) and H2-receptor (H2R) exhibit pronounced species selectivity in their pharmacological properties; i.e., bulky agonists possess higher potencies and efficacies at guinea pig (gp) than at the corresponding human (h) receptor isoforms. In this study, we examined the effects of NG-acylated imidazolylpropylguanidines substituted with a single phenyl or cyclohexyl ...

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