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Towards labeled argininamide-type NPY Y1 receptor antagonists: Identification of a favorable propionylation site in BIBO3304

Keller, Max ; Schindler, Lisa ; Bernhardt, Günther ; Buschauer, Armin


Aiming at molecular tools for the neuropeptide Y Y1 receptor (Y1R), three types of derivatives of the argininamide-type Y1R antagonist BIBO3304 were prepared by (1) propionylation at the guanidine group (3), (2) substitution at the urea moiety with a propionamidobutyl residue (4) and (3) replacement of ureidomethyl by a propionylaminomethyl group (5). With Ki and Kb values in the range of 1.5-4.3 ...


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