THE FIRST HIGHLY POTENT AND SELECTIVE NONPEPTIDE NEUROPEPTIDE-Y Y-1-RECEPTOR ANTAGONIST - BIBP3226

The design and subsequent in vitro and in vivo biological characterisation of the first potent and selective non-peptide neuropeptide Y Y-1 receptor antagonist, BIBP3226 ((R)-N-2-(diphenylacetyl)-N-[(4-hydroxyphenyl)methyl]-argininamide) is reported. BIBP3226 displaced I-125-labelled neuropeptide Y with high affinity (K-i = 7 nM) from the human neuropeptide Y Y-1 receptor and proved to be highly selective. BIBP3226 displayed potent antagonistic properties both in in vitro and in vivo models and thus represents the first selective non-peptide neuropeptide Y Y-1 receptor antagonist.