The first highly potent and selective non-peptide neuropeptide Y Y1 receptor antagonist: BIBP3226.
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.
Rudolf
K
K
Division of Pharma Research, Dr. Karl Thomae GmbH, Biberach, Germany.
Eberlein
W
W
Engel
W
W
Wieland
H A
HA
Willim
K D
KD
Entzeroth
M
M
Wienen
W
W
Beck-Sickinger
A G
AG
Doods
H N
HN
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*
C092926:BIBP 3226; D017476:Receptors, Neuropeptide Y; D001120:Arginine; D002118:Calcium