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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 logD values: -1.8-12.5), were synthesized and investigated for NPY Y(1) receptor (Y(1)R) antagonism, Y(1)R 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 (Y(1)R antagonism) varied from low nM to ...

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