Product Description

The kappa opioid receptor (κ-OR) is one of the three principal members of the opioid receptor family, belonging to the class of G protein-coupled receptors. It is widely distributed within the central nervous system, including the hypothalamus, nucleus accumbens, periaqueductal gray, and spinal cord, and is also expressed in some peripheral tissues such as the gastrointestinal tract. Its primary functions, upon activation by endogenous ligands like dynorphins, include mediating analgesia (particularly effective against visceral pain), producing sedation and diuresis, and modulating mood (often associated with dysphoria). Unlike mu receptor agonists, kappa agonists do not typically produce euphoria and carry a lower risk of respiratory depression, making the κ-OR a potential target for developing non-addictive analgesics. However, challenges such as the dysphoric and psychotomimetic side effects associated with its activation remain to be addressed.

ScreeningBio’s HEK293T/Human κ 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.