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Gene Review

Npffr1  -  neuropeptide FF receptor 1

Mus musculus

Synonyms: Gm236, Gpr147, LOC237362, NPFF1, OT7T022
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Disease relevance of Npffr1

  • The present results suggest that NPFF-induced hypothermia depends on the stimulation of Gs (but not Gi) proteins [1].
  • In mice pretreated intracerebroventricularly (i.c.v.) with pertussis or cholera toxins, effects of neuropeptide FF (NPFF), on hypothermia and morphine-induced analgesia, were assessed [1].

High impact information on Npffr1

  • The brain substrates involved in the pharmacological effects of neuropeptide FF (NPFF, Phe-Leu-Phe-Gln-Pro-Gln-Arg-Phe-NH2) including interactions with opioid systems, were investigated with the [14C]-2-deoxyglucose ([14C]-2-DG) autoradiography technique in mouse [2].
  • The pharmacological effects of Neuropeptide FF (NPFF) analogs exhibiting different selectivities towards Neuropeptide FF1 (NPFF1) and Neuropeptide FF2 (NPFF2) receptors were investigated after supraspinal administration in mice [3].
  • Pre-treatment with the putative NPFF antagonist, BIBP3226 (30 microM) abolished the contractile responses to the two neuropeptides (3 microM) [4].
  • To assess the peripheral effects of NPFF receptors in the gastrointestinal tract motility, NPFF and NPVF were tested in the mouse isolated distal colon [4].
  • The responses to NPFF (5 microM) and NPVF (5 microM) were not modified by atropine or naloxone (1 microM) [4].

Biological context of Npffr1


Anatomical context of Npffr1

  • Rodent strain differences in the NPFF1 and NPFF2 receptor distribution and density in the central nervous system [5].
  • The NPFF1 binding levels were nearly the same in telencephalic structures while distinct in the forebrain [5].
  • NPFF, a FMRF-NH2-like peptide, blocks opiate effects on ileum contractions [8].
  • NPFF and a potent NPFF agonist, 1DMe (0.005-22 nmol) injected into the lateral ventricle decreased morphine analgesia and produced naloxone (2.5 mg x kg(-1), s.c.)-resistant hypothermia after administration into the third ventricle [1].
  • NPFF was cleaved preferentially into an inactive metabolite, Gln-Arg-Phe-NH2, in the cerebrum slices [9].

Associations of Npffr1 with chemical compounds

  • Furthermore, NPFF (1 microM) and NPVF (1 microM) did not influence the contractive responses to acetylcholine (0.1-10 microM), morphine (1 microM) or nociceptin (0.1 microM) [4].
  • Antinociceptive and hypothermic effects of 1DMe (D.Tyr-Leu-(n.Me)Phe-Gln-Pro-Gln-Arg-Phe-NH(2)), an NPFF agonist, and of L-NAME (N(omega)nitro-L-arginine methyl ester), an inhibitor of nitric oxide synthase, were investigated in mice [10].
  • An NPFF analog, 1 DMe, reduced the analgesic effect of DAGO and [D.Ala2]deltorphin-I, mu and delta selective agonists respectively [11].

Analytical, diagnostic and therapeutic context of Npffr1

  • The present study evaluates the putative differences between NPFF1 and NPFF2 receptor distribution and density throughout the central nervous system between rat and mouse strains by using in vitro quantitative autoradiography [5].
  • In addition, the isolated bioassay may be applied as a simple parameter to characterize the potential NPFF agonists and antagonists [4].
  • In contrast, anti-opioid effects resulting from NPFF-receptor stimulation do not involve a cholera toxin-sensitive transducer protein [1].
  • Degradation of neuropeptide FF (NPFF) and SQA-neuropeptide FF (SQA-NPFF) by mouse brain sections was investigated by using capillary electrophoresis with UV detection for the separation and the identification of the degradation products [9].


  1. Cholera and pertussis toxins inhibit differently hypothermic and anti-opioid effects of neuropeptide FF. Francés, B., Lahlou, H., Zajac, J.M. Regul. Pept. (2001) [Pubmed]
  2. Functional consequences of neuropeptide FF receptors stimulation in mouse: a cerebral glucose uptake study. Quelven, I., Roussin, A., Zajac, J.M. Neuroscience (2004) [Pubmed]
  3. Comparison of pharmacological activities of Neuropeptide FF1 and Neuropeptide FF2 receptor agonists. Quelven, I., Roussin, A., Zajac, J.M. Eur. J. Pharmacol. (2005) [Pubmed]
  4. Neuropeptide FF receptors exert contractile activity via inhibition of nitric oxide release in the mouse distal colon. Fang, Q., Guo, J., Chang, M., Chen, L.X., Chen, Q., Wang, R. Peptides (2005) [Pubmed]
  5. Rodent strain differences in the NPFF1 and NPFF2 receptor distribution and density in the central nervous system. Gouardères, C., Faura, C.C., Zajac, J.M. Brain Res. (2004) [Pubmed]
  6. Sex differences in the effects of neuropeptide FF and IgG from neuropeptide FF on morphine- and stress-induced analgesia. Kavaliers, M., Innes, D. Peptides (1992) [Pubmed]
  7. Hypothermic effects of neuropeptide FF analogues in mice. Desprat, C., Zajac, J.M. Pharmacol. Biochem. Behav. (1997) [Pubmed]
  8. NPFF, a FMRF-NH2-like peptide, blocks opiate effects on ileum contractions. Demichel, P., Rodriguez, J.C., Roquebert, J., Simonnet, G. Peptides (1993) [Pubmed]
  9. Enzymatic degradation of neuropeptide FF and SQA-neuropeptide FF in the mouse brain. Sol, J.C., Roussin, A., Proto, S., Mazarguil, H., Zajac, J.M. Peptides (1999) [Pubmed]
  10. Opposing interplay between Neuropeptide FF and nitric oxide in antinociception and hypothermia. Zajac, J.M., Latapie, J.P., Francés, B. Peptides (2000) [Pubmed]
  11. Differential modulation of mu- and delta-opioid antinociception by neuropeptide FF receptors in young mice. Desprat, C., Zajac, J.M. Neuropeptides (1997) [Pubmed]
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