V. Melanotropin release inhibiting activity of neuropeptide Y: Structure-activity relationships
V. Melanotropin release inhibiting activity of neuropeptide Y: Structure-activity relationships
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V. 神经肽 Y 的促黑素释放抑制活性：结构-活性关系
DOI：
10.1016/0024-3205(87)90045-2
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发表时间：
1987
期刊：
影响因子：
6.1
通讯作者：
H. Vaudry
中科院分区：
文献类型：
--
作者：
J. Danger;M. Tonon;M. Lamacz;J. Martel;S. Saint;G. Pelletier;H. Vaudry
我们最近发现，神经肽Y（neuropeptide Y，NPY）可抑制蛙垂体中叶α-MSH的释放。本研究采用灌流技术，比较了NPY、各种NPY短链类似物以及胰多肽家族的另外两个成员肽YY（PYY）和禽胰多肽（APP）对α-MSH释放的抑制活性。其生物学效价顺序为：NPY > NPY[2-36]> NPY[16-36] > NPY[25-36] > NPY[1-15]。在测试的两种胰腺多肽中，PYY似乎几乎与NPY一样有效，而APP的活性比NPY低6倍。NPY[1-15]和NPY[16-36]均不能对抗NPY对α-MSH释放的抑制作用。构效关系研究表明，NPY的生物活性决定簇位于分子的C-末端部分。
We have recently shown that the release of α-MSH by the intermediate lobe of the frog pituitary is inhibited by neuropeptide Y (NPY). Using the perifusion technique, we have compared in the present study, the α-MSH release inhibiting activities of NPY, various NPY short chain analogues and two other members of the pancreatic polypeptide family, peptide YY (PYY) and avian pancreatic polypeptide (APP). The order of biological potency was NPY > NPY[2–36] > NPY[16–36] > NPY[25–36] > NPY[1–15]. Among the two pancreatic polypeptides tested, PYY appeared to be almost as potent as NPY while APP was 6 times less active than NPY. Neither NPY[1–15] nor NPY[16–36] could antagonize the inhibitory effect of NPY on α-MSH release. The structure-activity relationship study suggests that the bioactive determinant of NPY is located in the C-terminal part of the molecule.