Opioid Receptor-Like 1 (OPRL1) ACTOne Stable Cell Line
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Catalog Number:
CL-11-OPRL1
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In Stock
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Price: Please inquire order@eEnzyme.com
Detailed Description
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CL-11-OPRL1
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Name
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Opioid Receptor-Like 1 (OPRL1) ACTOneTM Stable Cell Line |
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Description
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This cell line is a HEK-293-CNG cell line that expresses a recombinant human OPRL1. HEK-293-CNG cells express a modified CNG (Cyclic Nucleotide Gated) channel that opens in response to elevated intracellular cAMP levels and consequently result in ion flux and cell membrane depolarization. The assay allows both end-point and kinetic measurement of intracellular cAMP changes with a FDSS, FLIPR, or a fluorescence microplate reader.
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Application
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cAMP dependent assay for Gi-coupled human OPRL1;
Cell-based high-throughput screening of human OPRL1 agonists/antagonists.
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Size
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1x 106 cells
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Detection
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FlexStation or Microplate reader
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For Downloading
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==>> DATA SHEET ==>> MSDS
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Synonym: Opioid Related Nociceptin Receptor 1, KOR-3, ORL1, OOR, Orphanin FQ Receptor, NOCIR, PNOCR, NOPr, Nociceptin/Orphanin FQ Receptor, Kappa3-Related Opioid Receptor, Kappa-Type 3 Opioid Receptor, Opiate Receptor-Like 1, Nociceptin Receptor, LC132 Receptor-Like, KOR3, OPRL, NOP
About Human Kappa Opioid Receptor (OPRK1/KOR) Stable Cell Line
Kappa Opioid Receptor (OPRK1), also known as KOR or Kappa-type Opioid Receptor, is a Class A G protein-coupled receptor (GPCR) that is activated primarily by the endogenous opioid peptides dynorphins. OPRK1 predominantly couples to Gi/o proteins, resulting in inhibition of adenylate cyclase activity, reduced intracellular cAMP production, modulation of calcium and potassium channels, and regulation of neuronal excitability. The receptor is widely expressed throughout the brain, spinal cord, and peripheral nervous system, where it plays important roles in pain perception, stress responses, mood regulation, and reward signaling.
OPRK1 is an important therapeutic target for pain management, pruritus, substance use disorders, depression, and other neuropsychiatric diseases. Unlike the μ-opioid receptor, activation of KOR produces potent analgesia with a lower risk of respiratory depression but is also associated with dysphoria and sedation, driving the development of selective agonists, antagonists, and biased ligands with improved therapeutic profiles.
eEnzyme's Human OPRK1 Stable Cell Line provides a reliable platform for investigating KOR-mediated signaling and evaluating agonists, antagonists, and biased ligands using cAMP and other GPCR functional assays. The cell line is well suited for receptor characterization, compound profiling, potency determination, and high-throughput drug screening.
Applications
• OPRK1 (KOR) receptor pharmacology studies
• Opioid signaling research
• Agonist and antagonist screening
• Pain and analgesic drug discovery
• Addiction and substance use disorder research
• Depression and stress-related disorder studies
• cAMP and GPCR functional assays
• High-throughput screening (HTS)
Biological Significance of OPRK1
OPRK1 is a major regulator of opioid signaling in the central and peripheral nervous systems. Activation of the receptor by dynorphins modulates nociception, stress responses, mood, reward pathways, and neurotransmitter release through Gi/o-mediated signaling. The receptor has attracted considerable interest for the development of safer analgesics and novel therapies for opioid use disorder, chronic pruritus, depression, and other CNS disorders. In addition, selective KOR agonists, antagonists, and G protein-biased ligands continue to be actively investigated to maximize therapeutic efficacy while minimizing undesirable central nervous system side effects. The OPRK1 Stable Cell Line provides a valuable tool for studying opioid receptor biology and accelerating the discovery of next-generation KOR-targeted therapeutics.
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