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BIIE0246: A selective and high affinity neuropeptide Y Y2 receptor antagonist

1999; Elsevier BV; Volume: 384; Issue: 2-3 Linguagem: Inglês

10.1016/s0014-2999(99)00650-0

1879-0712

Henri Doods, Wolfram Gaida, H. Wieland, Horst Dollinger, Gerd Schnorrenberg, Franz Esser, Wolfhard Engel, Wolfgang Eberlein, K Rudolf,

Pharmacological Receptor Mechanisms and Effects

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-triazol-4-yl]ethyl]-argininamid (BIIE0246) is reported. BIIE0246 displaced [125I]neuropeptide Y with high affinity (IC(50)=3.3 nM) from the human neuropeptide Y Y(2) receptor and proved to be highly selective. BIIE0246 displayed antagonistic properties and thus represents the first selective non-peptide neuropeptide Y Y(2) receptor antagonist.