Nociceptin receptor
Also known as: OOR, OPRL1, ORL1
Function
G protein-coupled opioid receptor that functions as a receptor for the endogenous neuropeptide nociceptin. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Signaling via G proteins mediates inhibition of adenylate cyclase activity and calcium channel activity. Arrestins modulate signaling via G proteins and mediate the activation of alternative signaling pathways that lead to the activation of MAP kinases. Plays a role in modulating nociception and the perception of pain. Plays a role in the regulation of locomotor activity by the neuropeptide nociceptin.
Classification
- Family (Pfam)
- PF00001 7tm_1
- InterPro
- GPCR_Rhodpsn, GPCR_Rhodpsn_7TM, Opioid_rcpt, X_opioid_rcpt
- Functional cluster
- Membrane Transporters & GPCRs
Experimental structures · PDB · 4
A predicted model is available from AlphaFold.
Gene Ontology · 14
- GO:0031410 cytoplasmic vesicle
- GO:0043005 neuron projection
- GO:0005886 plasma membrane
- GO:0097060 synaptic membrane
- GO:0004930 G protein-coupled receptor activity
- GO:0042923 neuropeptide binding
- GO:0001626 nociceptin receptor activity
- GO:0007193 adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway
- GO:0019722 calcium-mediated signaling
- GO:0007270 neuron-neuron synaptic transmission
- GO:0007218 neuropeptide signaling pathway
- GO:0007200 phospholipase C-activating G protein-coupled receptor signaling pathway
- GO:0007600 sensory perception
- GO:0019233 sensory perception of pain
Drugs targeting this protein · 3
- CEBRANOPADOL agonist
- LY-2940094 antagonist
- SCH-486757 agonist
Related proteins · sequence + function similarity
- Nociceptin receptor 1.00
- Nociceptin receptor 1.00
- Nociceptin receptor 1.00
- Nociceptin receptor 0.99
- Delta-type opioid receptor 0.95
- Delta-type opioid receptor 0.94
- Kappa-type opioid receptor 0.93
- Kappa-type opioid receptor 0.92
- Delta-type opioid receptor 0.92
- Kappa-type opioid receptor 0.92
- Kappa-type opioid receptor 0.91
- Somatostatin receptor type 5 0.91
Literature · 8 cited papers
- Serine 363 is required for nociceptin/orphanin FQ opioid receptor (NOPR) desensitization, internalization, and arrestin signaling. J. Biol. Chem. · 2012
- Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic. Nature · 2012
- The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
- Agonist-induced internalization and desensitization of the human nociceptin receptor expressed in CHO cells. Cell. Mol. Life Sci. · 2002
- The DNA sequence and comparative analysis of human chromosome 20. Nature · 2001
- Nociceptin stimulates neutrophil chemotaxis and recruitment: Inhibition by aspirin-triggered-15-Epi-lipoxin A4. J. Immunol. · 2001
- ORL1, a novel member of the opioid receptor family. Cloning, functional expression and localization. FEBS Lett. · 1994
- Expression of alternate forms of brain opioid 'orphan' receptor mRNA in activated human peripheral blood lymphocytes and lymphocytic cell lines. Brain Res. Mol. Brain Res. · 1995