Neuropeptide FF receptor explained

neuropeptide FF receptor 1
Hgncid:17425
Symbol:NPFFR1
Altsymbols:GPR147
Entrezgene:64106
Omim:607448
Refseq:NM_022146
Uniprot:Q9GZQ6
Chromosome:10
Arm:q
Band:21-q22
neuropeptide FF receptor 2
Hgncid:4525
Symbol:NPFFR2
Altsymbols:GPR74
Entrezgene:10886
Omim:607449
Refseq:NM_004885
Uniprot:Q9Y5X5
Chromosome:4
Arm:q
Band:21

The neuropeptide FF receptors[1] are members of the G-protein coupled receptor superfamily of integral membrane proteins which bind the pain modulatory neuropeptides AF and FF.[2] The Neuropeptide FF receptor family is a member of the G protein-coupled receptor superfamily containing two subtypes, NPFF1 and NPFF2, which exhibit a high affinity for Neuropeptide FF (NPFF) peptides. NPFF1 is broadly distributed in the central nervous system with the highest levels found in the limbic system and the hypothalamus. NPFF2 is present in high density, particularly in mammals in the superficial layers of the spinal cord where it is involved in nociception and modulation of opioid functions. These receptors participate to the modulation of opioid receptor function in the brain and spinal cord, and can either reduce or increase opioid receptor function depending which tissue they are released in, reflecting a complex role for neuropeptide FF in pain responses.[3] [4] [5] [6] [7]

NPFF receptors are coupled to G proteins and regulate adenylyl cyclase in recombinant cell lines (CHO, HEK 293, SH-SY5Y). NPFF receptors are also coupled to voltage-gated N-type Ca2+ channels.

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Notes and References

  1. Parker RM, Copeland NG, Eyre HJ, Liu M, Gilbert DJ, Crawford J, Couzens M, Sutherland GR, Jenkins NA, Herzog H . Grant Robert Sutherland . Molecular cloning and characterisation of GPR74 a novel G-protein coupled receptor closest related to the Y-receptor family . Brain Res. Mol. Brain Res. . 77 . 2 . 199–208 . 2000 . 10837915 . 10.1016/S0169-328X(00)00052-8.
  2. Elshourbagy NA, Ames RS, Fitzgerald LR, Foley JJ, Chambers JK, Szekeres PG, Evans NA, Schmidt DB, Buckley PT, Dytko GM, Murdock PR, Milligan G, Groarke DA, Tan KB, Shabon U, Nuthulaganti P, Wang DY, Wilson S, Bergsma DJ, Sarau HM . Receptor for the pain modulatory neuropeptides FF and AF is an orphan G protein-coupled receptor . J. Biol. Chem. . 275 . 34 . 25965–71 . 2000 . 10851242 . 10.1074/jbc.M004515200 . free .
  3. Yang HY, Iadarola MJ . Modulatory roles of the NPFF system in pain mechanisms at the spinal level . Peptides . 27 . 5 . 943–52 . May 2006 . 16443306 . 10.1016/j.peptides.2005.06.030 . 2197210 .
  4. Roumy M, Lorenzo C, Mazères S, Bouchet S, Zajac JM, Mollereau C . Physical association between neuropeptide FF and micro-opioid receptors as a possible molecular basis for anti-opioid activity . The Journal of Biological Chemistry . 282 . 11 . 8332–42 . March 2007 . 17224450 . 10.1074/jbc.M606946200 . free .
  5. Yang HY, Tao T, Iadarola MJ . Modulatory role of neuropeptide FF system in nociception and opiate analgesia . Neuropeptides . 42 . 1 . 1–18 . February 2008 . 17854890 . 10.1016/j.npep.2007.06.004 . 20901853 .
  6. Betourne A, Familiades J, Lacassagne L, Halley H, Cazales M, Ducommun B, Lassalle JM, Zajac JM, Frances B . Decreased motivational properties of morphine in mouse models of cancerous- or inflammatory-chronic pain: implication of supraspinal neuropeptide FF(2) receptors . Neuroscience . 157 . 1 . 12–21 . November 2008 . 18804517 . 10.1016/j.neuroscience.2008.08.045 . 31899256 .
  7. Cline MA, Mathews DS . Anoretic effects of neuropeptide FF are mediated via central mu and kappa subtypes of opioid receptors and receptor ligands . General and Comparative Endocrinology . 159 . 2–3 . 125–9 . 2008 . 18823989 . 10.1016/j.ygcen.2008.09.001 .
  8. Mollereau C, Mazarguil H, Marcus D, Quelven I, Kotani M, Lannoy V, Dumont Y, Quirion R, Detheux M, Parmentier M, Zajac JM . Pharmacological characterization of human NPFF(1) and NPFF(2) receptors expressed in CHO cells by using NPY Y(1) receptor antagonists . Eur. J. Pharmacol. . 451 . 3 . 245–56 . 2002 . 12242085 . 10.1016/S0014-2999(02)02224-0.
  9. Fang Q, Guo J, He F, Peng YL, Chang M, Wang R . In vivo inhibition of neuropeptide FF agonism by BIBP3226, an NPY Y1 receptor antagonist . Peptides . 27 . 9 . 2207–13 . September 2006 . 16762456 . 10.1016/j.peptides.2006.04.002 . 34414256 .
  10. Fang Q, Wang YQ, He F, Guo J, Guo J, Chen Q, Wang R . Inhibition of neuropeptide FF (NPFF)-induced hypothermia and anti-morphine analgesia by RF9, a new selective NPFF receptors antagonist . Regulatory Peptides . 147 . 1–3 . 45–51 . April 2008 . 18276024 . 10.1016/j.regpep.2007.12.007 . 37436256 .
  11. Wang YQ, Guo J, Wang SB, Fang Q, He F, Wang R . Neuropeptide FF receptors antagonist, RF9, attenuates opioid-evoked hypothermia in mice . Peptides . 29 . 7 . 1183–90 . July 2008 . 18406009 . 10.1016/j.peptides.2008.02.016 . 10797657 .

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