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Chiral N(G)-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity

Ghorai, Prasanta ; Kraus, Anja ; Birnkammer, Tobias ; Geyer, Roland ; Bernhardt, Günther ; Dove, Stefan ; Seifert, Roland ; Elz, Sigurd ; Buschauer, Armin


A set of chiral imidazolylpropylguanidines and 2-aminothiazolylpropylguanidines bearing N(G)-3-phenyl- or N(G)-3-cyclohexylbutanoyl residues was synthesized and investigated for histamine H2 receptor (H2R) agonism (guinea pig (gp) right atrium, GTPase assay on recombinant gp and human (h) H2R) and for hH2R selectivity compared to hH1R, hH3R and hH4R. In contrast to previous studies on arpromidine ...


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