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Nociceptin

Nociceptin
Names
Other names
Orphanin FQ
Identifiers
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
MeSH nociceptin
UNII
  • InChI=1S/C79H129N27O22/c1-41(2)33-54(72(122)95-44(5)66(116)103-56(36-59(84)110)73(123)102-53(77(127)128)27-28-58(83)109)104-70(120)49(23-13-15-29-80)100-69(119)52(26-18-32-90-79(87)88)99-65(115)43(4)96-75(125)57(40-107)105-71(121)50(24-14-16-30-81)101-68(118)51(25-17-31-89-78(85)86)98-64(114)42(3)94-61(112)39-93-76(126)63(45(6)108)106-74(124)55(35-47-21-11-8-12-22-47)97-62(113)38-91-60(111)37-92-67(117)48(82)34-46-19-9-7-10-20-46/h7-12,19-22,41-45,48-57,63,107-108H,13-18,23-40,80-82H2,1-6H3,(H2,83,109)(H2,84,110)(H,91,111)(H,92,117)(H,93,126)(H,94,112)(H,95,122)(H,96,125)(H,97,113)(H,98,114)(H,99,115)(H,100,119)(H,101,118)(H,102,123)(H,103,116)(H,104,120)(H,105,121)(H,106,124)(H,127,128)(H4,85,86,89)(H4,87,88,90)/t42-,43-,44-,45+,48-,49-,50-,51-,52-,53-,54-,55-,56-,57-,63-/m0/s1 ☒N
    Key: PULGYDLMFSFVBL-SMFNREODSA-N ☒N
  • C[C@H]([C@@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CCC(=O)N)C(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@H](Cc2ccccc2)N)O
Properties
C79H129N27O22
Molar mass 1809.04
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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prepronociceptin
Identifiers
SymbolPNOC
NCBI gene5368
HGNC9163
OMIM601459
RefSeqNM_006228
UniProtQ13519
Other data
LocusChr. 8 p21
Search for
StructuresSwiss-model
DomainsInterPro

Nociceptin/orphanin FQ (N/OFQ), a 17-amino acid neuropeptide, is the endogenous ligand for the nociceptin receptor (NOP, ORL-1). Nociceptin acts as a potent anti-analgesic, effectively counteracting the effect of pain-relievers; its activation is associated with brain functions such as pain sensation and fear learning.

The gene coding for prepronociceptin is located on Ch8p21 in humans.[1] Nociceptin is derived from the prepronociceptin protein, as are a further two peptides, nocistatin and NocII, both of which inhibit N/OFQ receptor function.[2] Nociceptin is the first example of reverse pharmacology; the NOP receptor was discovered before the endogenous ligand which was discovered by two separate groups in 1995.[3][4]

  1. ^ Mollereau C, Simons MJ, Soularue P, Liners F, Vassart G, Meunier JC, Parmentier M (August 1996). "Structure, tissue distribution, and chromosomal localization of the prepronociceptin gene". Proceedings of the National Academy of Sciences of the United States of America. 93 (16): 8666–70. Bibcode:1996PNAS...93.8666M. doi:10.1073/pnas.93.16.8666. PMC 38730. PMID 8710928.
  2. ^ Okuda-Ashitaka E, Minami T, Tachibana S, Yoshihara Y, Nishiuchi Y, Kimura T, Ito S (March 1998). "Nocistatin, a peptide that blocks nociceptin action in pain transmission". Nature. 392 (6673): 286–9. Bibcode:1998Natur.392..286O. doi:10.1038/32660. PMID 9521323. S2CID 4414426.
  3. ^ Cite error: The named reference Meunier et al. Isolation of N/OFQ was invoked but never defined (see the help page).
  4. ^ Reinscheid, R. K.; Nothacker, H.-P.; Bourson, A.; Ardati, A.; Henningsen, R. A.; Bunzow, J. R.; Grandy, D. K.; Langen, H.; Monsma, F. J.; Civelli, O. (1995-11-03). "Orphanin FQ: A Neuropeptide That Activates an Opioidlike G Protein-Coupled Receptor". Science. 270 (5237): 792–794. Bibcode:1995Sci...270..792R. doi:10.1126/science.270.5237.792. ISSN 0036-8075. PMID 7481766. S2CID 38117854.
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