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Updated: Sep 26, 2026

Peptide-based Identification of Functional Motifs and their Binding Partners
Published on: July 1, 2013
The first highly potent and selective non-peptide neuropeptide Y Y1 receptor antagonist: BIBP3226
K Rudolf1, W Eberlein, W Engel
1Division of Pharma Research, Dr. Karl Thomae GmbH, Biberach, Germany.
Abstract:
The design and subsequent in vitro and in vivo biological characterisation of the first potent and selective non-peptide neuropeptide Y Y1 receptor antagonist, BIBP3226 ((R)-N2-(diphenylacetyl)-N-[(4-hydroxyphenyl)methyl]-argininami de) is reported. BIBP3226 displaced 125I-labelled neuropeptide Y with high affinity (Ki = 7 nM) from the human neuropeptide Y Y1 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 Y1 receptor antagonist.
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