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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



Abstract

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

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