Product Description

The Cholecystokinin B receptor (CCK2 or CCK-B) is a G protein-coupled receptor with high affinity for both cholecystokinin and gastrin. It is widely expressed in the central nervous system (e.g., cerebral cortex, limbic system) and the gastrointestinal tract (e.g., gastric parietal cells, certain intestinal cells). Its primary functions involve mediating neuromodulatory effects in the CNS, regulating anxiety, pain perception, memory, and dopaminergic neuron activity. Peripherally, it potently stimulates gastric acid secretion from parietal cells and may influence cell proliferation. Consequently, the CCK2 receptor is a significant therapeutic target for anxiety disorders, analgesia, and gastric acid-related conditions such as gastrinoma.

ScreeningBio’s HEK293 Mouse CCK2 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.