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Structure-Activity Relationships of Neuropeptide Y Y_1 Receptor Antagonists Related to BIBP 3226,

Aiglstorfer, Iris ; Hendrich, Ingo ; Moser, Christiane ; Bernhardt, Günther ; Dove, Stefan ; Buschauer, Armin


Analogues of BIBP 3226, (R)-Nα-diphenylacetyl-N-(4-hydroxybenzyl)argininamide, were synthesized and investigated for Y1 antagonism (Ca2+-assay, HEL cells) and binding on Y1, Y2 and Y5 receptors. Replacing the benzylamino by a tetrahydrobenzazepinyl group preserves most of the Y1 activity. Combination with a NG-phenylpropyl arginine and a Nα-p-biphenylylacetyl moiety shifted the NPY receptor selectivity towards Y5.

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