Product Description

The mu opioid receptor (μ-OR) is the most clinically significant subtype within the opioid receptor family, belonging to the G protein-coupled receptor class. It is widely and densely expressed in the central nervous system, primarily in brain regions involved in pain modulation and reward, such as the periaqueductal gray, spinal cord dorsal horn, thalamus, striatum, and locus coeruleus, and is also found on peripheral nerves and some immune cells. As the primary target for most clinical opioid analgesics, its activation produces potent analgesia, euphoria, and sedation. However, it simultaneously leads to characteristic side effects like respiratory depression, constipation, tolerance, and addiction. Consequently, it is the central target for powerful pain relief, while its high addictive potential also underpins the biological basis of the global opioid crisis.

ScreeningBio’s HEK293T/Human μ 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.