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N(G)-Acyl-argininamides as NPY Y (1) receptor antagonists: Influence of structurally diverse acyl substituents on stability and affinity

Weiss, Stefan ; Keller, Max ; Bernhardt, G. ; Buschauer, Armin ; König, Burkhard



Abstract

N-G-Acylated argininamides, covering a broad range of lipophilicity (calculated log D values: -1.8-12.5), were synthesized and investigated for NPY Y-1 receptor (Y1R) antagonism, Y1R affinity and stability in buffer (N-G-deacylation, yielding BIBP 3226). Broad structural variation of substituents was tolerated. The K-i (binding) and K-b values (Y1R antagonism) varied from low nM to one-digit mu ...

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