The first highly potent and selective non-peptide neuropeptide Y Y1 receptor antagonist: BIBP3226

  • Eur J Pharmacol. 1994 Dec 27;271(2-3):R11-3. doi: 10.1016/0014-2999(94)90822-2.
K Rudolf  1 ,  W Eberlein ,  W Engel ,  H A Wieland ,  K D Willim ,  M Entzeroth ,  W Wienen ,  A G Beck-Sickinger ,  H N Doods
Affiliations
  • 1. Division of Pharma Research, Dr. Karl Thomae GmbH, Biberach, Germany.
PMID: 7705422 DOI: 10.1016/0014-2999(94)90822-2
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.