The neuropeptide YY1 receptor selective radioligand, [I-125][Leu(31),Pro(34)]peptide YY, is also a high affinity radioligand for human pancreatic polypeptide 1 receptors

被引：24

作者：

Gehlert, DR ^{[1
]}

Gackenheimer, SL ^{[1
]}

Schober, DA ^{[1
]}

Beavers, L ^{[1
]}

Gadski, R ^{[1
]}

Burnett, JP ^{[1
]}

Mayne, N ^{[1
]}

Lundell, I ^{[1
]}

Larhammar, D ^{[1
]}

机构：

[1] UPPSALA UNIV,DEPT MED PHARMACOL,S-75124 UPPSALA,SWEDEN

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1996年 / 318卷 / 2-3期

关键词：

neuropeptide Y; pancreatic polypeptide; peptide YY; Leu(31); Pro(34)]peptide YY;

D O I：

10.1016/S0014-2999(96)00797-2

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

A number of receptors for the pancreatic polypeptide-fold peptides are proposed based on findings from pharmacology and molecular biology studies. Neuropeptide Y and peptide YY have similar affinity for neuropeptide Y Y-1 and neuropeptide Y Y-2 while pancreatic polypeptide has highest affinity for pancreatic polypeptide 1. Pro(34)-substituted analogs of neuropeptide Y and peptide YY have selectivity for neuropeptide Y Y-1 over neuropeptide Y Y-2 receptors. In the present study, we found that one such 'neuropeptide Y Y-1-selective' radioligand, [I-125][Leu(31),pro(34)]peptide YY, also binds with high affinity to the pancreatic polypeptide 1 receptor. Therefore, caution needs to be exercised when using Pro(34)-analogs to define the neuropeptide Y Y-1 receptor in vivo and using tissue preparations.

引用

页码：485 / 490

页数：6

共 13 条

[1] CLONING AND FUNCTIONAL EXPRESSION OF A HUMAN Y4 SUBTYPE RECEPTOR FOR PANCREATIC-POLYPEPTIDE, NEUROPEPTIDE-Y, AND PEPTIDE YY [J].

BARD, JA ;

WALKER, MW ;

BRANCHEK, TA ;

WEINSHANK, RL .

JOURNAL OF BIOLOGICAL CHEMISTRY, 1995, 270 (45) :26762-26765

[2] DIFFERENT NEUROPEPTIDE-Y RECEPTOR SUBTYPES IN RAT AND RABBIT VAS-DEFERENS [J].

DOODS, HN ;

KRAUSE, J .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1991, 204 (01) :101-103

[3]

DUMONT Y, 1995, J PHARMACOL EXP THER, V272, P673

[4] PEPTIDE YY DERIVATIVES AS SELECTIVE NEUROPEPTIDE-Y PEPTIDE YY Y-1 AND Y-2 AGONISTS DEVOIDED OF ACTIVITY FOR THE Y-3 RECEPTOR SUB-TYPE [J].

DUMONT, Y ;

CADIEUX, A ;

PHENG, LH ;

FOURNIER, A ;

STPIERRE, S ;

QUIRION, R .

MOLECULAR BRAIN RESEARCH, 1994, 26 (1-2) :320-324

[5] [LEU31,PRO34]NEUROPEPTIDE-Y - A SPECIFIC Y-1 RECEPTOR AGONIST [J].

FUHLENDORFF, J ;

GETHER, U ;

AAKERLUND, L ;

LANGELANDJOHANSEN, N ;

THOGERSEN, H ;

MELBERG, SG ;

OLSEN, UB ;

THASTRUP, O ;

SCHWARTZ, TW .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1990, 87 (01) :182-186

[6]

Gehlert DR, 1996, MOL PHARMACOL, V50, P112

[7] SUBTYPES OF RECEPTORS FOR NEUROPEPTIDE-Y - IMPLICATIONS FOR THE TARGETING OF THERAPEUTICS [J].

GEHLERT, DR .

LIFE SCIENCES, 1994, 55 (08) :551-562

[8]

GEHLERT DR, 1995, CURR PHARM DESIGN, V1, P295

[9] The cloned rat pancreatic polypeptide receptor exhibits profound differences to the orthologous human receptor [J].

Lundell, I ;

Statnick, MA ;

Johnson, D ;

Schober, DA ;

Starback, P ;

Gehlert, DR ;

Larhammar, D .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1996, 93 (10) :5111-5115

[10] CLONING OF A HUMAN RECEPTOR OF THE NPY RECEPTOR FAMILY WITH HIGH-AFFINITY FOR PANCREATIC-POLYPEPTIDE AND PEPTIDE YY [J].

LUNDELL, I ;

BLOMQVIST, AG ;

BERGLUND, MM ;

SCHOBER, DA ;

JOHNSON, D ;

STATNICK, MA ;

GADSKI, RA ;

GEHLERT, DR ;

LARHAMMAR, D .

JOURNAL OF BIOLOGICAL CHEMISTRY, 1995, 270 (49) :29123-29128

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