Neuropeptide FF analog RF9 is not an antagonist of NPFF receptor and decreases food intake in mice after its central and peripheral administration
Jazyk angličtina Země Nizozemsko Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
23291266
DOI
10.1016/j.brainres.2012.12.037
PII: S0006-8993(12)01972-5
Knihovny.cz E-zdroje
- MeSH
- adamantan analogy a deriváty farmakologie MeSH
- anorektika farmakologie MeSH
- CHO buňky MeSH
- Cricetulus MeSH
- dipeptidy farmakologie MeSH
- extracelulárním signálem regulované MAP kinasy metabolismus MeSH
- fosforylace účinky léků MeSH
- kompetitivní vazba MeSH
- krysa rodu Rattus MeSH
- lidé MeSH
- myši inbrední C57BL MeSH
- nádorové buněčné linie MeSH
- oligopeptidy metabolismus MeSH
- přijímání potravy účinky léků MeSH
- receptory neuropeptidů metabolismus MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- lidé MeSH
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- adamantan MeSH
- adamantylcarbonyl-arginyl-phenylalaninamide MeSH Prohlížeč
- anorektika MeSH
- dipeptidy MeSH
- extracelulárním signálem regulované MAP kinasy MeSH
- neuropeptide FF receptor MeSH Prohlížeč
- neuropeptide FF, Tyr(1)-N-methyl-Phe(3)- MeSH Prohlížeč
- oligopeptidy MeSH
- receptory neuropeptidů MeSH
Neuropeptide FF (NPFF) belongs to the RF-amide family of peptides bearing the identical C-terminal amino acid sequence (R-F-NH2). In addition to NPFF, prolactin-releasing peptide (PrRP), another RF-amide, binds to NPFF receptors with high affinity. A selective antagonist of PrRP has not yet been identified, but a selective antagonist of NPFF, 1-adamantanecarbonyl-RF-NH2 (RF9), was recently reported to antagonize the hyperalgesic effect of NPFF after central administration to mice. In the present study, RF9 competed with NPFF analog D-Y-L-(N-Me)-F-Q-P-Q-R-F-NH2 (1DMe) in binding to CHO-K1 cell membranes transfected with the human NPFF2 receptor. In rat pituitary RC-4B/C cells, where the expression of the NPFF2 receptor was proved by immunodetection, RF9 did not reverse the phosphorylation of MAPK/ERK1/2 induced by [Tyr(1)]NPFF. In vivo experiments with fasted mice confirmed that centrally injected [Tyr(1)]NPFF significantly lowered food intake. However, RF9, a putative NPFF2 antagonist, did not reverse the anorectic effect of [Tyr(1)]NPFF. Paradoxically, RF9 itself exhibited an anorectic effect in fasted mice not only after intracerebroventricular but also after subcutaneous administration. This finding casts doubt on claims that RF9 is an NPFF antagonist.
Brain Res. 2013 Mar 29;1503:108 PubMed
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