The in vitro biological characterisation of the first potent and selective
non-peptide neuropeptide Y Y-2 receptor antagonist, (S)-N-2-[[1-[2-[4-[(R,S
)-5,11-dihydro-6(6h)-oxodibenz[b,e]azepin-11-yl]-1-piperazinyl]-2-oxoethyl]
cylopentyl] acetyl-N-[2-[1,2-dihydro-3,5(4H)-dioxo-1,2-diphenyl-3H-1,2,4-t
riazol-4-yl]ethyl]-argininamid (BIIE0246) is reported. BIIE0246 displaced [
I-125]neuropeptide Y with high affinity (IC50 = 3.3 nM) from the human neur
opeptide Y Y-2 receptor and proved to be highly selective. BIIE0246 display
ed antagonistic properties and thus represents the first selective non-pept
ide neuropeptide Y Y-2 receptor antagonist. (C) 1999 Elsevier Science B.V.
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