OPRK1
OPRK1 (opioid receptor kappa 1, also known as KOR or OPRK) is a G protein-coupled opioid receptor that responds to endogenous dynorphins and alpha-neoendorphins. It inhibits adenylate cyclase and neurotransmitter release, and contributes to the perception of pain. Browse Assay Genie's current range of OPRK1 research reagents below, or read on for the biology behind the target.
OPRK1 is a G protein-coupled opioid receptor that acts as a receptor for the endogenous peptides alpha-neoendorphins and dynorphins, and has low affinity for beta-endorphins. It also responds to various synthetic opioids and to the psychoactive diterpene salvinorin A. Ligand binding causes a conformational change that triggers signalling through guanine nucleotide-binding proteins (G proteins) and modulates downstream effectors such as adenylate cyclase. The result is inhibition of adenylate cyclase activity. OPRK1 also inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance.
The OPRK1 gene encodes a seven-transmembrane-spanning receptor of the G protein-coupled receptor 1 family, and the protein is found at the cell membrane. HGNC places it in the opioid receptors gene group. Mouse and rat both carry an ortholog named Oprk1. The gene produces alternatively spliced transcript variants that encode different isoforms, and a recent study provided evidence for translational readthrough, giving an additional C-terminally extended isoform through an alternative in-frame termination codon.
Functionally, the kappa-type opioid receptor plays a role in the perception of pain and in mediating the hypolocomotor, analgesic and aversive actions of synthetic opioids. It is also involved in reduced physical activity and in the regulation of salivation after synthetic opioid treatment, and may contribute to arousal and the regulation of autonomic and neuroendocrine functions. Variations in the OPRK1 gene have been associated with alcohol dependence and opiate addiction. The previous name was opioid receptor, kappa 1.
OPRK1 contributes to the perception of pain and to the analgesic actions of synthetic opioids, making it a focus for pain signalling studies.
Variations in the OPRK1 gene have been associated with alcohol dependence and opiate addiction, linking the receptor to substance-use research.
Ligand binding triggers G protein signalling and inhibition of adenylate cyclase, offering a model for opioid receptor signal transduction.
OPRK1 reduces calcium currents, increases potassium conductance and inhibits neurotransmitter release, and may influence autonomic and neuroendocrine regulation.
OPRK1 is a G protein-coupled receptor for dynorphins and alpha-neoendorphins. Ligand binding triggers G protein signalling that inhibits adenylate cyclase, reduces calcium currents, increases potassium conductance and inhibits neurotransmitter release. It plays a role in pain perception and in the effects of synthetic opioids.
OPRK1 is also called KOR and OPRK, and its UniProt name is kappa-type opioid receptor. The previous HGNC name was opioid receptor, kappa 1. The gene produces alternatively spliced variants encoding different isoforms, including a C-terminally extended isoform produced by translational readthrough.
Mouse and rat both have an ortholog called Oprk1, so the receptor can be studied in common rodent models; check the datasheet of any product for its validated reactivity. Variations in the human OPRK1 gene have been associated with alcohol dependence and opiate addiction.
Other opioid receptors, their peptide ligands and related G protein-coupled receptor targets studied in pain and neuroscience research.
Gene and protein annotations from HGNC, NCBI Gene and UniProt P41145; product specifications from Assay Genie datasheets.