κ-opioid receptor
The κ-opioid receptor or kappa opioid receptor, abbreviated KOR or KOP for its ligand ketazocine, is a G protein-coupled receptor that in humans is encoded by the OPRK1 gene. The KOR is coupled to the G protein Gi/G0 and is one of four related receptors that bind opioid-like compounds in the brain and are responsible for mediating the effects of these compounds. These effects include altering nociception, consciousness, motor control, and mood. Dysregulation of this receptor system has been implicated in alcohol and drug addiction.[5][6]
The KOR is a type of opioid receptor that binds the opioid peptide dynorphin as the primary endogenous ligand (substrate naturally occurring in the body).[7] In addition to dynorphin, a variety of natural alkaloids, terpenes and synthetic ligands bind to the receptor. The KOR may provide a natural addiction control mechanism, and therefore, drugs that target this receptor may have therapeutic potential in the treatment of addiction .
There is evidence that distribution and/or function of this receptor may differ between sexes.[8][9][10][11]
- ^ a b c GRCh38: Ensembl release 89: ENSG00000082556 – Ensembl, May 2017
- ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000025905 – Ensembl, May 2017
- ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ Anderson RI, Becker HC (August 2017). "Role of the Dynorphin/Kappa Opioid Receptor System in the Motivational Effects of Ethanol". Alcoholism: Clinical and Experimental Research. 41 (8): 1402–1418. doi:10.1111/acer.13406. PMC 5522623. PMID 28425121.
- ^ Karkhanis A, Holleran KM, Jones SR (2017). "Dynorphin/Kappa Opioid Receptor Signaling in Preclinical Models of Alcohol, Drug, and Food Addiction". International Review of Neurobiology. 136: 53–88. doi:10.1016/bs.irn.2017.08.001. ISBN 9780128124734. PMID 29056156.
- ^ James IF, Chavkin C, Goldstein A (1982). "Selectivity of dynorphin for kappa opioid receptors". Life Sciences. 31 (12–13): 1331–4. doi:10.1016/0024-3205(82)90374-5. PMID 6128656.
- ^ Chartoff EH, Mavrikaki M (2015). "Sex Differences in Kappa Opioid Receptor Function and Their Potential Impact on Addiction". Frontiers in Neuroscience. 9: 466. doi:10.3389/fnins.2015.00466. PMC 4679873. PMID 26733781.
- ^ Rasakham K, Liu-Chen LY (January 2011). "Sex differences in kappa opioid pharmacology". Life Sciences. 88 (1–2): 2–16. doi:10.1016/j.lfs.2010.10.007. PMC 3870184. PMID 20951148.
- ^ Siciliano CA, Calipari ES, Yorgason JT, Lovinger DM, Mateo Y, Jimenez VA, Helms CM, Grant KA, Jones SR (April 2016). "Increased presynaptic regulation of dopamine neurotransmission in the nucleus accumbens core following chronic ethanol self-administration in female macaques". Psychopharmacology. 233 (8): 1435–43. doi:10.1007/s00213-016-4239-4. PMC 4814331. PMID 26892380.
- ^ Johnson BN, Kumar A, Su Y, Singh S, Sai KK, Nader SH, et al. (September 2022). "PET imaging of kappa opioid receptors and receptor expression quantified in neuron-derived extracellular vesicles in socially housed female and male cynomolgus macaques". Neuropsychopharmacology. 48 (2): 410–417. doi:10.1038/s41386-022-01444-9. PMC 9751296. PMID 36100655.