The first highly potent and selective non-peptide neuropeptide Y Y1 receptor antagonist: BIBP3226
European Journal of PharmacologyPublished 1 December 1994
K Rudolf, Wolfgang Eberlein, Wolfhard Engel, H. Wieland, Klaus D. Willim, Michael Entzeroth
Citations373
SJR quartileQ1
SJR score1.20
SNIP0.98
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TL;DR
BIBP3226 displayed potent antagonistic properties both in in vitro and in vivo models and thus represents the first selective non-peptide neuropeptides Y Y1 receptor antagonist.
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.
Keywords
NeuroscienceBiochemistry, Genetics and Molecular Biology
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