选择性神经肽Y Y(2)受体拮抗剂BIIE0246对神经肽Y释放的影响。
Effect of a selective neuropeptide Y Y(2) receptor antagonist, BIIE0246 on neuropeptide Y release.
作者信息
King P J, Williams G, Doods H, Widdowson P S
机构信息
Diabetes and Endocrinology Research Group, Department of Medicine, University of Liverpool, Duncan Building, Daulby Street, L69 3GA, Liverpool, UK.
出版信息
Eur J Pharmacol. 2000 May 12;396(1):R1-3. doi: 10.1016/s0014-2999(00)00230-2.
We have examined the selective 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]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 Y(2) receptors in regulating rat hypothalamic neuropeptide Y release in the rat.
我们已经在体外研究了选择性神经肽Y Y(2)受体拮抗剂(S)-N(2)-[[1-[2-[4-[(R,S)-5,11-二氢-6(6H)-氧代二苯并[b,e]氮杂卓-11-基]-1-哌嗪基]-2-氧代乙基]环戊基]乙酰基]-N-[2-[1,2-二氢-3,5(4H)-二氧代-1,2-二苯基-3-H-1,2,4-三唑-4-基]乙基]-精氨酰胺(BIIE0246)对大鼠下丘脑切片神经肽释放的影响。BIIE0246可防止神经肽Y-(13-36)诱导的基础和K(+)刺激的神经肽Y释放减少。单独添加BIIE0246可增强K(+)刺激的神经肽释放，而不影响基础释放。这些数据与解剖学和功能研究一致，表明神经肽Y Y(2)受体在调节大鼠下丘脑神经肽Y释放中具有突触前作用。
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