Neuropeptide FF receptor

Last updated
neuropeptide FF receptor 1
Identifiers
SymbolNPFFR1
Alt. symbolsGPR147
NCBI gene 64106
HGNC 17425
OMIM 607448
RefSeq NM_022146
UniProt Q9GZQ6
Other data
Locus Chr. 10 q21-q22
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Structures Swiss-model
Domains InterPro
neuropeptide FF receptor 2
Identifiers
SymbolNPFFR2
Alt. symbolsGPR74
NCBI gene 10886
HGNC 4525
OMIM 607449
RefSeq NM_004885
UniProt Q9Y5X5
Other data
Locus Chr. 4 q21
Search for
Structures Swiss-model
Domains InterPro

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]

Contents

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.

Ligands

Agonists

Antagonists

See also

References

  1. ↑ Parker RM, Copeland NG, Eyre HJ, Liu M, Gilbert DJ, Crawford J, Couzens M, Sutherland GR, Jenkins NA, Herzog H (2000). "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. doi:10.1016/S0169-328X(00)00052-8. PMID   10837915.
  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 (2000). "Receptor for the pain modulatory neuropeptides FF and AF is an orphan G protein-coupled receptor". J. Biol. Chem. 275 (34): 25965–71. doi: 10.1074/jbc.M004515200 . PMID   10851242.
  3. ↑ Yang HY, Iadarola MJ (May 2006). "Modulatory roles of the NPFF system in pain mechanisms at the spinal level". Peptides. 27 (5): 943–52. doi:10.1016/j.peptides.2005.06.030. PMID   16443306. S2CID   2197210.
  4. ↑ Roumy M, Lorenzo C, Mazères S, Bouchet S, Zajac JM, Mollereau C (March 2007). "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. doi: 10.1074/jbc.M606946200 . PMID   17224450.
  5. ↑ Yang HY, Tao T, Iadarola MJ (February 2008). "Modulatory role of neuropeptide FF system in nociception and opiate analgesia". Neuropeptides. 42 (1): 1–18. doi:10.1016/j.npep.2007.06.004. PMID   17854890. S2CID   20901853.
  6. ↑ Betourne A, Familiades J, Lacassagne L, Halley H, Cazales M, Ducommun B, Lassalle JM, Zajac JM, Frances B (November 2008). "Decreased motivational properties of morphine in mouse models of cancerous- or inflammatory-chronic pain: implication of supraspinal neuropeptide FF(2) receptors" (PDF). Neuroscience. 157 (1): 12–21. doi:10.1016/j.neuroscience.2008.08.045. PMID   18804517. S2CID   31899256.
  7. ↑ Cline MA, Mathews DS (2008). "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. doi:10.1016/j.ygcen.2008.09.001. PMID   18823989.
  8. ↑ Jhamandas, Jack H.; Goncharuk, Valeri (2013). "Role of neuropeptide FF in central cardiovascular and neuroendocrine regulation". Frontiers in Endocrinology. 4: 8. doi: 10.3389/fendo.2013.00008 . PMC   3566396 . PMID   23404625.
  9. ↑ Oishi, Shinya; Misu, Ryosuke; Tomita, Kenji; Setsuda, Shohei; Masuda, Ryo; Ohno, Hiroaki; Naniwa, Yousuke; Ieda, Nahoko; Inoue, Naoko; Ohkura, Satoshi; Uenoyama, Yoshihisa; Tsukamura, Hiroko; Maeda, Kei-Ichiro; Hirasawa, Akira; Tsujimoto, Gozoh; Fujii, Nobutaka (2011). "Activation of Neuropeptide FF Receptors by Kisspeptin Receptor Ligands". ACS Medicinal Chemistry Letters. 2: 53–57. doi:10.1021/ml1002053. PMID   24900254.
  10. ↑ Malin, David H.; Henceroth, Mallori M.; Izygon, Jonathan J.; Nghiem, Duyen M.; Moon, Will D.; Anderson, Andrea P.; Madison, Caitlin A.; Goyarzu, Pilar; Ma, Jian-Nong; Burstein, Ethan S. (2015). "Reversal of morphine tolerance by a compound with NPFF receptor subtype-selective actions". Neuroscience Letters. 584: 141–145. doi:10.1016/j.neulet.2014.10.018. PMID   25459291.
  11. ↑ Mollereau C, Mazarguil H, Marcus D, Quelven I, Kotani M, Lannoy V, Dumont Y, Quirion R, Detheux M, Parmentier M, Zajac JM (2002). "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. doi:10.1016/S0014-2999(02)02224-0. PMID   12242085.
  12. ↑ Fang Q, Guo J, He F, Peng YL, Chang M, Wang R (September 2006). "In vivo inhibition of neuropeptide FF agonism by BIBP3226, an NPY Y1 receptor antagonist". Peptides. 27 (9): 2207–13. doi:10.1016/j.peptides.2006.04.002. PMID   16762456. S2CID   34414256.
  13. ↑ Fang Q, Wang YQ, He F, Guo J, Guo J, Chen Q, Wang R (April 2008). "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. doi:10.1016/j.regpep.2007.12.007. PMID   18276024. S2CID   37436256.
  14. ↑ Wang YQ, Guo J, Wang SB, Fang Q, He F, Wang R (July 2008). "Neuropeptide FF receptors antagonist, RF9, attenuates opioid-evoked hypothermia in mice". Peptides. 29 (7): 1183–90. doi:10.1016/j.peptides.2008.02.016. PMID   18406009. S2CID   10797657.
  15. ↑ Quillet, Raphaëlle; Schneider, Séverine; Utard, Valérie; Drieu La Rochelle, Armand; Elhabazi, Khadija; Henningsen, Jo Beldring; Gizzi, Patrick; Schmitt, Martine; Kugler, Valérie; Simonneaux, Valérie; Ilien, Brigitte; Simonin, Frédéric; Bihel, Frédéric (2021). "Identification of an N -acylated-DArg-Leu-NH2 Dipeptide as a Highly Selective Neuropeptide FF1 Receptor Antagonist That Potently Prevents Opioid-Induced Hyperalgesia". Journal of Medicinal Chemistry. 64 (11): 7555–7564. doi:10.1021/acs.jmedchem.1c00256. PMID   34008968.
  16. ↑ Lentschat, Hannah; Liessmann, Fabian; Tydings, Claiborne; Schermeng, Tina; Stichel, Jan; Urban, Nicole; Schaefer, Michael; Meiler, Jens; Beck-Sickinger, Annette G. (2025). "Hederagenin is a Highly Selective Antagonist of the Neuropeptide FF Receptor 1 that Reveals Mechanisms for Subtype Selectivity". Angewandte Chemie International Edition. 64 (6) e202417786. Bibcode:2025ACIE...64E7786L. doi:10.1002/anie.202417786.
  17. ↑ King, Tamara I.; Roewekamp, Ann-Cathrin; Sharma, Abhisheak; Harrison, Sydney; Mesangeau, Christophe; Mottinelli, Marco; Kamble, Shyam H.; McCurdy, Christopher R.; Avery, Bonnie A. (2019). "Bioanalytical method development and validation of MES207, a neuropeptide FF receptor antagonist, and its application in preclinical pharmacokinetics". Journal of Chromatography B. 1134–1135 121875. doi:10.1016/j.jchromb.2019.121875. PMC   7027589 . PMID   31790916.
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