Neuropeptide FF analog RF9 is not an antagonist of NPFF receptor and decreases food intake in mice after its central and peripheral administration
Language English Country Netherlands Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
23291266
DOI
10.1016/j.brainres.2012.12.037
PII: S0006-8993(12)01972-5
Knihovny.cz E-resources
- MeSH
- Adamantane analogs & derivatives pharmacology MeSH
- Appetite Depressants pharmacology MeSH
- CHO Cells MeSH
- Cricetulus MeSH
- Dipeptides pharmacology MeSH
- Extracellular Signal-Regulated MAP Kinases metabolism MeSH
- Phosphorylation drug effects MeSH
- Binding, Competitive MeSH
- Rats MeSH
- Humans MeSH
- Mice, Inbred C57BL MeSH
- Cell Line, Tumor MeSH
- Oligopeptides metabolism MeSH
- Eating drug effects MeSH
- Receptors, Neuropeptide metabolism MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Humans MeSH
- Male MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Adamantane MeSH
- adamantylcarbonyl-arginyl-phenylalaninamide MeSH Browser
- Appetite Depressants MeSH
- Dipeptides MeSH
- Extracellular Signal-Regulated MAP Kinases MeSH
- neuropeptide FF receptor MeSH Browser
- neuropeptide FF, Tyr(1)-N-methyl-Phe(3)- MeSH Browser
- Oligopeptides MeSH
- Receptors, Neuropeptide 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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