U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
Orphanin FQ (OFQ, Nociceptin) is a recently discovered 17-amino acid neuropeptide that is structurally related to the opioid peptides but does not bind opioid receptors. OFQ selectively binds its own receptor (OFQR), which is also sequentially related to the opioid receptors, yet does not bind opioid ligands. OFQ has been proposed to act as an anti-opioid peptide, but its widespread sites of action in the brain suggest that it may have more general functions. Nociceptin acts as an anxiolytic to attenuate behavioral responses to stress. In vivo experiments have demonstrated that Nociceptin modulates a variety of biological functions ranging from nociception to food intake, from memory processes to cardiovascular and renal functions, from spontaneous locomotor activity to gastrointestinal motility, from anxiety to the control of neurotransmitter release at peripheral and central sites. Nociceptin has being shown to directly inhibit an adaptive immune response, i.e., antibody formation, both in vitro and in vivo.

Approval Year

TargetsConditions

Conditions

PubMed

PubMed

TitleDatePubMed
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.
2011-10-13
Orphanin FQ/nociceptin not only blocks but also reverses behavioral adaptive changes induced by repeated cocaine in mice.
2010-08-01
Distinct effects of nociceptin analogs on scopolamine-induced memory impairment in mice.
2009-01-14
Pharmacological characterisation of [(pX)Phe4]nociceptin(1-13)amide analogues. 1. In vitro studies.
2002-06
Orphanin FQ/nociceptin but not Ro 65-6570 inhibits the expression of cocaine-induced conditioned place preference.
2002-05
Comparison of the effects of [Phe1psi(CH2-NH)Gly2]nociceptin(1-13)NH2 in rat brain, rat vas deferens and CHO cells expressing recombinant human nociceptin receptors.
1999-05
Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.
1997-11
Relationship between binding affinity and functional activity of nociceptin/orphanin FQ.
1997-10
Patents

Sample Use Guides

Rats: Intrathecal (i.t.) administration of Nociceptin (0.2--20 nmoles) dose-dependently reversed mechanical allodynic-like behavior
Route of Administration: Other
Suspension muscle strips test in vitro showed Nociceptin (OFQ) (10(-9)-10(-6) mol/L) concentration dependently caused an immediate tonic contraction in the isolated rat colon.
Substance Class Protein
Created
by admin
on Wed Apr 02 20:12:54 GMT 2025
Edited
by admin
on Wed Apr 02 20:12:54 GMT 2025
Protein Type PEPTIDE
Protein Sub Type
Sequence Origin HUMAN
Sequence Type COMPLETE
Record UNII
7AYI9N34FF
Record Status FAILED
Record Version
  • Download
Name Type Language
NOCICEPTIN
MI  
Common Name English
NOCICEPTIN [MI]
Preferred Name English
OFQ
Common Name English
L-GLUTAMINE, L-PHENYLALANYLGLYCYLGLYCYL-L-PHENYLALANYL-L-THREONYLGLYCYL-L-ALANYL-L-ARGINYL-L-LYSYL-L-SERYL-L-ALANYL-L-ARGINYL-L-LYSYL-L-LEUCYL-L-ALANYL-L-ASPARAGINYL-
Systematic Name English
ORPHANIN FQ (SWINE)
Common Name English
ORPHANIN FQ
Common Name English
PHE-GLY-GLY-PHE-THR-GLY-ALA-ARG-LYS-SER-UNK-ALA-ARG-LYS-LEU-ALA-ASN-GLN
Systematic Name English
Code System Code Type Description
EPA CompTox
DTXSID60168933
Created by admin on Wed Apr 02 20:12:54 GMT 2025 , Edited by admin on Wed Apr 02 20:12:54 GMT 2025
PRIMARY
UNIPROT
Q13519
Created by admin on Wed Apr 02 20:12:54 GMT 2025 , Edited by admin on Wed Apr 02 20:12:54 GMT 2025
PRIMARY
PUBCHEM
16131448
Created by admin on Wed Apr 02 20:12:54 GMT 2025 , Edited by admin on Wed Apr 02 20:12:54 GMT 2025
PRIMARY
CAS
170713-75-4
Created by admin on Wed Apr 02 20:12:54 GMT 2025 , Edited by admin on Wed Apr 02 20:12:54 GMT 2025
PRIMARY
FDA UNII
7AYI9N34FF
Created by admin on Wed Apr 02 20:12:54 GMT 2025 , Edited by admin on Wed Apr 02 20:12:54 GMT 2025
PRIMARY
MERCK INDEX
m8024
Created by admin on Wed Apr 02 20:12:54 GMT 2025 , Edited by admin on Wed Apr 02 20:12:54 GMT 2025
PRIMARY Merck Index
CHEBI
80266
Created by admin on Wed Apr 02 20:12:54 GMT 2025 , Edited by admin on Wed Apr 02 20:12:54 GMT 2025
PRIMARY
WIKIPEDIA
Nociceptin
Created by admin on Wed Apr 02 20:12:54 GMT 2025 , Edited by admin on Wed Apr 02 20:12:54 GMT 2025
PRIMARY
Related Record Type Details
TARGET -> AGONIST
[35S]GTP?S Binding
EC50
TARGET -> AGONIST
Ki
Related Record Type Details
ACTIVE MOIETY
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.
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:NUMBER(CALCULATED) CHEMICAL
Molecular Formula CHEMICAL