title: The first highly potent and selective non-peptide neuropeptide Y Y1 receptor antagonist: BIBP3226.
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.
authors.affiliation: Division of Pharma Research, Dr. Karl Thomae GmbH, Biberach, Germany.
authors.forename: K
authors.initials: K
authors.lastname: Rudolf
authors.forename: W
authors.initials: W
authors.lastname: Eberlein
authors.forename: W
authors.initials: W
authors.lastname: Engel
authors.forename: H A
authors.initials: HA
authors.lastname: Wieland
authors.forename: K D
authors.initials: KD
authors.lastname: Willim
authors.forename: M
authors.initials: M
authors.lastname: Entzeroth
authors.forename: W
authors.initials: W
authors.lastname: Wienen
authors.forename: A G
authors.initials: AG
authors.lastname: Beck-Sickinger
authors.forename: H N
authors.initials: HN
authors.lastname: Doods
mesh_terms: D000818:Animals; D001120:Arginine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects; D002118:Calcium / Q000378:metabolism; D010477:Perfusion; D051381:Rats; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors*
chemical_list: C092926:BIBP 3226; D017476:Receptors, Neuropeptide Y; D001120:Arginine; D002118:Calcium