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N(omega)-carbamoylation of the argininamide moiety: an avenue to insurmountable NPY Y1 receptor antagonists and a radiolabeled selective high affinity molecular tool ([3H]UR-MK299) with extended residence time

Keller, Max ; Weiss, Stefan ; Hutzler, Christoph ; Kuhn, Kilian K. ; Mollereau, Catherine ; Dukorn, Stefanie ; Schindler, Lisa ; Bernhardt, Günther ; König, Burkhard ; Buschauer, Armin



Abstract

Analogues of the argininamide-type NPY Y-1 receptor (Y1R) antagonist BIBP3226, bearing carbamoyl moieties at the guanidine group, revealed subnanomolar Ki 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 ...

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