CHO-K1 Human Opioid Mu β Arrestin Stable Cell
Item | Cat# | Price |
Stable Cell Line | SNB-A-0175A | Inquiry |
Compound Testing Services | CT-001 | $1,850 per 384w plate (Up To 16 cpds Dose) |
Product Description
The opioid receptors are class A (rhodopsin-like) G protein-coupled receptors (GPCRs) that mediate the actions of endogenous opioid peptides and opiate drugs. They play essential roles in pain modulation, reward, mood regulation, and stress response. The three main subtypes—μ (MOR), δ (DOR), and κ (KOR)—differ in distribution and physiological function. MOR primarily mediates analgesia and euphoria; DOR contributes to mood control and emotional balance; and KOR is linked to stress and dysphoric effects.
These receptors are highly expressed in the central nervous system, including the brainstem, thalamus, spinal cord, and limbic regions, as well as in peripheral tissues such as the gut and immune cells. Upon activation by endogenous peptides like endorphins, enkephalins, and dynorphins, opioid receptors couple mainly to Gi/o proteins, inhibiting adenylyl cyclase, reducing intracellular cAMP, suppressing Ca²⁺ influx, and promoting neuronal hyperpolarization via K⁺ channels.
Through these pathways, opioid receptors inhibit nociceptive signaling and produce analgesic effects, while also influencing emotion and reward circuits. However, chronic activation can lead to tolerance, dependence, and addiction, highlighting their dual roles in therapeutic pain control and substance abuse.
ScreeningBio’s human opioid Mu β-arrestin cell line is an ideal tool for studying GPCR/β-arrestin interactions. In this system, the GPCR C-terminus is fused to a smallBiT tag, and the β2-arrestin N-terminus is fused to a largeBiT tag. Upon receptor activation, GPCR/β-arrestin interaction brings the two fragments together to reconstitute an active NanoLuc enzyme, which can be quantified using the NanoBiT substrate. This cell line is designed to evaluate a compound’s ability to activate the β-arrestin signaling pathway.
Product Specifications
Target Type | GPCR |
Species | Human |
HGNC Symbol | OPRM1 |
Accession Number | NM_000914 |
Parental Line | CHO-K1 |
Lot# | See Vial |
Storage | Liquid Nitrogen |
Data
Target Background
The μ-opioid receptor (MOR), also known as the mu-opioid receptor or OPRM1, is a class A G-protein-coupled receptor (GPCR) that mediates the analgesic and euphoric effects of endogenous opioid peptides and exogenous opiates. MOR is highly expressed in the central and peripheral nervous systems, including the brainstem, thalamus, spinal cord, and peripheral sensory neurons, as well as in the gastrointestinal tract and immune cells. This broad distribution reflects its diverse physiological and pharmacological actions.
Upon activation by endogenous ligands such as β-endorphin, enkephalins, or synthetic agonists like morphine and fentanyl, MOR couples predominantly to Gi/o proteins, leading to inhibition of adenylate cyclase, decreased intracellular cAMP levels, opening of G-protein–gated inwardly rectifying potassium (GIRK) channels, and closure of voltage-gated calcium channels. These effects result in hyperpolarization and reduced neuronal excitability, which underlie its potent analgesic and antinociceptive actions.
Clinically, MOR is the principal target of opioid analgesics used for moderate to severe pain management. However, chronic activation can lead to tolerance, physical dependence, respiratory depression, and addiction, posing major challenges in therapeutic use. In contrast, partial agonists (e.g., buprenorphine) and biased agonists that preferentially activate G-protein over β-arrestin pathways are being explored to achieve analgesia with fewer side effects. Due to its central role in pain modulation, reward, and stress response, MOR remains a critical focus in both neuroscience and pharmacological research aimed at developing safer opioid therapeutics.