Structure-activity relationships of neuropeptide Y Y1 receptor antagonists related to BIBP 3226
Analogues of BIBP 3226, (R)-N(α)-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 N(G)-phenylpropyl arginine and a N(α)-p-biphenylylacetyl moiety shifted the NPY receptor selectivity towards Y5. (C) 2000 Elsevier Science Ltd. All rights reserved.