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Bivalent argininamide-type neuropeptide Y Y1 antagonists do not support the hypothesis of receptor dimerisation

Keller, Max ; Teng, Shangjun ; Bernhardt, Günther ; Buschauer, Armin



Abstract

Bivalent ligands are potential tools to investigate the dimerisation of G-protein-coupled receptors. Based on the (R)-argininamide BIBP 3226, a potent and selective neuropeptide Y Y1 receptor (Y1R) antagonist, we prepared a series of bivalent Y1R ligands using a wide range of linker lengths (8 to 36 atoms). Exploiting the high eudismic ratio (>1000) of the parent compound we synthesized sets of ...

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