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Probing Ligand-Specific Histamine H1- and H2-Receptor
Conformations with NG-Acylated Imidazolylpropylguanidines

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


Abstract

Impromidine (IMP) and arpromidine (ARP)-derived guanidines are more potent and efficacious guinea pig (gp) histamine H2-receptor (gpH2R) than human (h) H2R agonists and histamine H1-receptor (H1R) antagonists with preference for hH1R relative to gpH1R. We examined NG-acylated imidazolylpropylguanidines (AIPGs), which are less basic than guanidines, at hH2R, gpH2R, rat H2R (rH2R), hH1R, and gpH1R ...

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