Nω-Carbamoylation of the argininamide moiety: an avenue to insurmountable NPY Y1 receptor antagonists and a radiolabeled selective high-affinity molecular tool ([ …

…, G Bernhardt, B Konig, A Buschauer

Index: Keller, Max; Pop, Nathalie; Hutzler, Christoph; Beck-Sickinger, Annette G.; Bernhardt, Guenther; Buschauer, Armin Journal of Medicinal Chemistry, 2008 , vol. 51, # 24 p. 8168 - 8172

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Citation Number: 2

Abstract

Analogues of the argininamide-type NPY Y1 receptor (Y1R) antagonist BIBP3226, bearing carbamoyl moieties at the guanidine group, revealed subnanomolar K i values and caused depression of the maximal response to NPY (calcium assay) by up to 90% in a concentration- and time-dependent manner, suggesting insurmountable antagonism. To gain insight into the mechanism of binding of the synthesized compounds, a tritiated antagonist,(R)-N α- ...