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Gene Review

NPFFR2  -  neuropeptide FF receptor 2

Homo sapiens

Synonyms: G-protein coupled receptor 74, G-protein coupled receptor HLWAR77, GPR74, HLWAR77, NPFF2, ...
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Disease relevance of NPFFR2


High impact information on NPFFR2


Biological context of NPFFR2


Anatomical context of NPFFR2

  • Characterization of the NPGP receptor and identification of a novel short mRNA isoform in human hypothalamus [1].
  • In situ hybridisation analysis of rat brain tissue confirms this result and identifies the hippocampus and amygdala nuclei as the brain areas with particular high expression of GPR74 mRNA [7].
  • Furthermore, immunohistochemically, NPFF receptor 2-protein was demonstrated to be increased in the primary afferents in the spinal cord of rats with peripheral inflammation [8].
  • At low levels, NPGPR message is detectable in several other tissues including spleen, prostate, brain, heart, ovary, colon, kidney, lung, liver, and pancreas [9].

Associations of NPFFR2 with chemical compounds

  • Therefore, we used binding studies to examine the interaction of NPFF, orexin and NPY with the NPGPR [1].
  • 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 [10].
  • The activities of these analogues were evaluated by their ability to both inhibit adenylate cyclase in NPFF2 receptor transfected CHO cells and to reverse the effect of nociceptin on acutely dissociated rat dorsal raphe neurons [11].

Analytical, diagnostic and therapeutic context of NPFFR2


  1. Characterization of the NPGP receptor and identification of a novel short mRNA isoform in human hypothalamus. Laemmle, B., Schindler, M., Beilmann, M., Hamilton, B.S., Doods, H.N., Wieland, H.A. Regul. Pept. (2003) [Pubmed]
  2. Regulation of endogenous human NPFF2 receptor by neuropeptide FF in SK-N-MC neuroblastoma cell line. Ankö, M.L., Panula, P. J. Neurochem. (2006) [Pubmed]
  3. A common haplotype in the G-protein-coupled receptor gene GPR74 is associated with leanness and increased lipolysis. Dahlman, I., Dicker, A., Jiao, H., Kere, J., Blomqvist, L., van Harmelen, V., Hoffstedt, J., Borch-Johnsen, K., Jorgensen, T., Hansen, T., Pedersen, O., Laakso, M., Arner, P. Am. J. Hum. Genet. (2007) [Pubmed]
  4. Neuropeptide AF and FF modulation of adipocyte metabolism. Primary insights from functional genomics and effects on beta-adrenergic responsiveness. Lefrere, I., De Coppet, P., Camelin, J.C., Le Lay, S., Mercier, N., Elshourbagy, N., Bril, A., Berrebi-Bertrand, I., Feve, B., Krief, S. J. Biol. Chem. (2002) [Pubmed]
  5. Neuropeptide FF (NPFF) analogs functionally antagonize opioid activities in NPFF2 receptor-transfected SH-SY5Y neuroblastoma cells. Mollereau, C., Mazarguil, H., Zajac, J.M., Roumy, M. Mol. Pharmacol. (2005) [Pubmed]
  6. The high throughput screening of neuropeptide FF2 receptor ligands from Korean herbal plant extracts. Do, E.U., Piao, L.Z., Choi, G., Choi, Y.B., Kang, T.M., Shin, J., Chang, Y.J., Nam, H.Y., Kim, H.J., Kim, S.I. Peptides (2006) [Pubmed]
  7. Molecular cloning and characterisation of GPR74 a novel G-protein coupled receptor closest related to the Y-receptor family. Parker, R.M., Copeland, N.G., Eyre, H.J., Liu, M., Gilbert, D.J., Crawford, J., Couzens, M., Sutherland, G.R., Jenkins, N.A., Herzog, H. Brain Res. Mol. Brain Res. (2000) [Pubmed]
  8. Modulatory roles of the NPFF system in pain mechanisms at the spinal level. Yang, H.Y., Iadarola, M.J. Peptides (2006) [Pubmed]
  9. Sequence and tissue distribution of a novel G-protein-coupled receptor expressed prominently in human placenta. Cikos, S., Gregor, P., Koppel, J. Biochem. Biophys. Res. Commun. (1999) [Pubmed]
  10. Functional properties of Pfr(Tic)amide and BIBP3226 at human neuropeptide FF2 receptors. Engström, M., Wurster, S., Savola, J.M., Panula, P. Peptides (2003) [Pubmed]
  11. Structure-activity relationships of neuropeptide FF: role of C-terminal regions. Mazarguil, H., Gouardères, C., Tafani, J.A., Marcus, D., Kotani, M., Mollereau, C., Roumy, M., Zajac, J.M. Peptides (2001) [Pubmed]
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