Functional properties of PFR(Tic)amide and BIBP3226 at human neuropeptide FF2 receptors

被引：19

作者：

Engström, M

Wurster, S

Savola, JM

Panula, P

机构：

[1] Juvantia Pharma Ltd, Pharm, FIN-20520 Turku, Finland

[2] Abo Akad Univ, Inst Biol, Dept Biol, FIN-20520 Turku, Finland

来源：

PEPTIDES | 2003年 / 24卷 / 12期

关键词：

neuropeptide FF; antagonist; PFR(Tic)amide; BIBP3226; neuropeptides; S-35]GTP gamma S binding assay; NPFF2; receptor; super-agonist;

D O I：

10.1016/j.peptides.2003.10.009

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：

The functional characteristics of two putative neuropeptide FF (NPFF) antagonists, BIBP3226 and PFR(Tic)amide, on the human neuropeptide FF receptor subtype 2 (hNPFF2) were investigated. Surprisingly, PFR(Tic)amide was shown to exhibit agonist properties in the [S-35]guanosine-5'-O-(3-thio)triphosphate ([S-35]GTPgammaS) binding assay. The efficacy of PFR(Tic)amide was significantly greater than that of (1DMe)Y8Fa, a stable analog of NPFF, and PFR(Tic)amide can therefore be classified as a 'super-agonist'. BIBP3226 did act as a reversible competitive antagonist on the hNPFF2 receptor. However, high concentrations of BIBP3226 also non-specifically increased [S-35]GTPgammaS binding. The usefulness of BIBP3226 as an antagonist tool on the NPFF receptor is thus limited. (C) 2003 Elsevier lnc. All rights reserved.

引用

页码：1947 / 1954

页数：8

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