Biology:Neuropeptide FF receptor

From HandWiki
neuropeptide FF receptor 1
Identifiers
SymbolNPFFR1
Alt. symbolsGPR147
NCBI gene64106
HGNC17425
OMIM607448
RefSeqNM_022146
UniProtQ9GZQ6
Other data
LocusChr. 10 q21-q22
neuropeptide FF receptor 2
Identifiers
SymbolNPFFR2
Alt. symbolsGPR74
NCBI gene10886
HGNC4525
OMIM607449
RefSeqNM_004885
UniProtQ9Y5X5
Other data
LocusChr. 4 q21

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.

Ligands

Agonists

  • Neuropeptide AF
  • Neuropeptide FF - similar high affinity at both NPFF1 and NPFF2
  • Neuropeptide SF (RFRP-1)
  • Gonadotropin-inhibitory hormone (Neuropeptide VF / RFRP-3) - selective for NPFF1 over NPFF2
  • Prolactin-releasing peptide (PrRP) - endogenous agonist for GPR10 but also agonist at NPFF2 with only weak activity at NPFF1[8]
  • Kisspeptins - endogenous agonist for GPR54 but longer chain versions are also agonists at NPFF1 and NPFF2.[9]
  • AC-263093 - synthetic small molecule agonist at NPFF2 but antagonist at NPFF1 [10]

Antagonists

See also

References

  1. ↑ "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. doi:10.1016/S0169-328X(00)00052-8. PMID 10837915. 
  2. ↑ "Receptor for the pain modulatory neuropeptides FF and AF is an orphan G protein-coupled receptor". J. Biol. Chem. 275 (34): 25965–71. 2000. doi:10.1074/jbc.M004515200. PMID 10851242. 
  3. ↑ "Modulatory roles of the NPFF system in pain mechanisms at the spinal level". Peptides 27 (5): 943–52. May 2006. doi:10.1016/j.peptides.2005.06.030. PMID 16443306. https://zenodo.org/record/1259305. 
  4. ↑ "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. doi:10.1074/jbc.M606946200. PMID 17224450. 
  5. ↑ "Modulatory role of neuropeptide FF system in nociception and opiate analgesia". Neuropeptides 42 (1): 1–18. February 2008. doi:10.1016/j.npep.2007.06.004. PMID 17854890. https://zenodo.org/record/1259273. 
  6. ↑ "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. doi:10.1016/j.neuroscience.2008.08.045. PMID 18804517. https://hal.archives-ouvertes.fr/hal-00319865/file/Betourne_Manuscript_REVISED_FINAL.pdf. 
  7. ↑ "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. 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. PMID 23404625. 
  9. ↑ Oishi, Shinya; Misu, Ryosuke; Tomita, Kenji; Setsuda, Shohei; Masuda, Ryo; Ohno, Hiroaki; Naniwa, Yousuke; Ieda, Nahoko et al. (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 et al. (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. ↑ "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. doi:10.1016/S0014-2999(02)02224-0. PMID 12242085. 
  12. ↑ "In vivo inhibition of neuropeptide FF agonism by BIBP3226, an NPY Y1 receptor antagonist". Peptides 27 (9): 2207–13. September 2006. doi:10.1016/j.peptides.2006.04.002. PMID 16762456. 
  13. ↑ "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. doi:10.1016/j.regpep.2007.12.007. PMID 18276024. 
  14. ↑ "Neuropeptide FF receptors antagonist, RF9, attenuates opioid-evoked hypothermia in mice". Peptides 29 (7): 1183–90. July 2008. doi:10.1016/j.peptides.2008.02.016. PMID 18406009. 
  15. ↑ Quillet, Raphaëlle; Schneider, Séverine; Utard, Valérie; Drieu La Rochelle, Armand; Elhabazi, Khadija; Henningsen, Jo Beldring; Gizzi, Patrick; Schmitt, Martine et al. (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. https://hal.science/hal-03363456. 
  16. ↑ Lentschat, Hannah; Liessmann, Fabian; Tydings, Claiborne; Schermeng, Tina; Stichel, Jan; Urban, Nicole; Schaefer, Michael; Meiler, Jens et al. (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). doi:10.1002/anie.202417786. Bibcode: 2025ACIE...64E7786L. 
  17. ↑ King, Tamara I.; Roewekamp, Ann-Cathrin; Sharma, Abhisheak; Harrison, Sydney; Mesangeau, Christophe; Mottinelli, Marco; Kamble, Shyam H.; McCurdy, Christopher R. et al. (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. doi:10.1016/j.jchromb.2019.121875. PMID 31790916. 



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