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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



Abstract

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 H-2 receptor (H2R) agonism ( guinea pig (gp) right atrium, GTPase assay on recombinant gp and human (h)H2R) and for hH(2)R selectivity compared to hH(1)R, hH(3)R and hH(4)R. In contrast to previous studies on ...

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