2. Academic Validation
  3. The first highly potent and selective non-peptide neuropeptide Y Y1 receptor antagonist: BIBP3226

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

Affiliation

  • 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.

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