|Opiate receptor-like 1|
|Symbols||; KOR-3; NOCIR; OOR; ORL1|
|External IDs||IUPHAR: ChEMBL: GeneCards:|
The nociceptin receptor or NOP also known as the orphanin FQ receptor or kappa-type 3 opioid receptor is a protein that in humans is encoded by the OPRL1 (opioid receptor-like 1) gene. The nociceptin receptor is a G protein-coupled receptor whose natural ligand is known as nociceptin or orphanin FQ, a 17 amino acid neuropeptide. This receptor is involved in the regulation of numerous brain activities, particularly instinctive and emotional behaviors.
Nociceptin is thought to be an endogenous antagonist of dopamine transport that may act either directly on dopamine or by inhibiting GABA to affect dopamine levels. Within the central nervous system its action can be either similar or opposite to those of opioids depending on their location. It controls a wide range 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.
Several commonly used opioid drugs including etorphine and buprenorphine have been demonstrated to bind to nociceptin receptors, but this binding is relatively insignificant compared to their activity at other opioid receptors. More recently a range of selective ligands for NOP have been developed, which show little or no affinity to other opioid receptors and so allow NOP-mediated responses to be studied in isolation.
- Buprenorphine (partial agonist, not selective for NOP, also partial agonist of µ-opioid and δ-opioid receptors, and competitive antagonist of κ-opioid receptors)
- Cebranopadol (full agonist at NOP, μ-opioid and δ-opioid receptors, partial agonist at κ-opioid receptor)
- Norbuprenorphine (full agonist; non-selective (also full agonist at the MOR and DOR and partial agonist at the KOR; peripherally-selective)
- NNC 63-0532
- SR-16435 (mixed MOR / NOP partial agonist)
- MCOPPB (full agonist, CAS# 1028969-49-4)
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- nociceptin receptor at the US National Library of Medicine Medical Subject Headings (MeSH)