Effect of a selective neuropeptide Y Y2 receptor antagonist, BIIE0246 on neuropeptide Y release

PJ King, G Williams, H Doods… - European journal of …, 2000 - Elsevier
PJ King, G Williams, H Doods, PS Widdowson
European journal of pharmacology, 2000Elsevier
We have examined the selective neuropeptide Y Y2 receptor antagonist,(S)-N2-[[1-[2-[4-[(R,
S)-5, 11-dihydro-6 (6h)-oxodibenz [b, e] azepin-11-yl]-1-piperazinyl]-2-oxoethyl] cyclopentyl]
acetyl]-N-[2-[1, 2-dihydro-3, 5 (4H)-dioxo-1, 2-diphenyl-3-H-1, 2, 4-triazol-4-yl] ethyl]-
argininamid (BIIE0246) on neuropeptide release from rat hypothalamic slices in vitro.
BIIE0246 prevented neuropeptide Y-(13-36)-induced reduction in basal and K+-stimulated
neuropeptide Y release. Addition of BIIE0246 alone enhanced K+-stimulated neuropeptide …
We have examined the selective neuropeptide Y Y2 receptor antagonist, (S)-N2-[[1-[2-[4-[(R,S)-5,11-dihydro-6(6h)-oxodibenz[b,e]azepin-11-yl]-1-piperazinyl]-2-oxoethyl]cyclopentyl]acetyl]-N-[2-[1,2-dihydro-3,5(4H)-dioxo-1,2-diphenyl-3-H-1,2,4-triazol-4-yl]ethyl]-argininamid (BIIE0246) on neuropeptide release from rat hypothalamic slices in vitro. BIIE0246 prevented neuropeptide Y-(13-36)-induced reduction in basal and K+-stimulated neuropeptide Y release. Addition of BIIE0246 alone enhanced K+-stimulated neuropeptide release, without affecting basal release. These data are consistent with anatomical and functional studies suggesting a pre-synaptic role for neuropeptide Y Y2 receptors in regulating rat hypothalamic neuropeptide Y release in the rat.
Elsevier