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

The design and subsequent in vitro and in vivo biological characterisa tion of the first potent and selective non-peptide neuropeptide Y Y-1 receptor antagonist, BIBP3226 lacetyl)-N-[(4-hydroxyphenyl)methyl]-arg ininamide) is reported. BIBP3226 displaced I-125-labelled neuropeptide Y with high affinity (K-i = 7 nM) from the human neuropeptide Y Y-1 r eceptor and proved to be highly selective. BIBP3226 displayed potent a ntagonistic properties both in in vitro and in vivo models and thus re presents the first selective non-peptide neuropeptide Y Y-1 receptor a ntagonist.