Highly potent and small neuropeptide Y agonist obtained by linking NPY 1–4 via spacer to α‐helical NPY 25–36

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Abstract
Analogues of neuropeptide Y (NPY) containing small N‐ and C‐terminal segments linked via flexible spacer arms were found to exhibit receptor binding affinity constants almost as high as NPY as well as post‐ and presynaptic NPY‐agonistic activities. One of the most active analogues contains N‐terminal NPY segment 1–4 linked via ε‐aminocaproic acid (Aca) to the C‐terminal partially α‐helical peptide amide segment 25–36. NPY 1–4‐Aca‐25–36 is the first highly potent NPY agonist, which is of considerably reduced size in comparison to the native hormone. The analogues are accessible by solid‐phase synthesis using Fmoc strategy.