[I-125]Leu(31), Pro(34)-PYY is a high affinity radioligand for rat PP1/Y4 and Y1 receptors: Evidence for heterogeneity in pancreatic polypeptide receptors

被引:56
作者
Gehlert, DR [1 ]
Schober, DA [1 ]
Gackenheimer, SL [1 ]
Beavers, L [1 ]
Gadski, R [1 ]
Lundell, I [1 ]
Larhammar, D [1 ]
机构
[1] UPPSALA UNIV,DEPT MED PHARMACOL,S-75124 UPPSALA,SWEDEN
关键词
I-125]Leu(31); Pro(34)-PYY; radioligand; peptides; neuropeptide Y; pancreatic polypeptide;
D O I
10.1016/S0196-9781(96)00346-4
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Cloned receptors for the PP-fold peptides are subdivided into Y1, Y2, PP1/Y4, Y5 and Y6. NPY and PYY have similar affinity for Y1, Y2, Y5 and Y6 receptors while PP has highest affinity for PP1. Pro(34)-substituted analogs of NPY and PYY have selectivity for Y1 and Y1-like receptors over Y2 receptors. In the present study, we found the putative Y1-selective radioligand, [I-125]Leu(31), Pro(34)-PYY, also binds with high affinity to the rat PP1 receptor in cell lines expressing the receptor. However, in rat brain sections, [I-125]Leu(31), Pro(34)-PYY does not appear to bind to the interpeduncular nucleus, a brain region containing a high density of [I-125]-bPP binding sites. Therefore, it appears there is additional heterogeneity in receptors recognizing PP. (C) 1997 Elsevier Science Inc.
引用
收藏
页码:397 / 401
页数:5
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