Product Description

The PAC1 receptor (pituitary adenylate cyclase-activating polypeptide type 1 receptor) is a class B G protein-coupled receptor encoded by the ADCYAP1R1 gene, with high selectivity for its endogenous ligands PACAP-27 and PACAP-38. It is primarily distributed in the central nervous system (e.g., hypothalamus, hippocampus, cerebellum, brainstem) and peripheral tissues (adrenal medulla, pancreas, testis, lungs, and immune cells). Its core function involves activating Gs and Gq proteins to stimulate cAMP production and calcium mobilization, thereby mediating neurotransmission regulation, neuroprotection, promotion of neuronal survival and synaptic plasticity, while also participating in hormone secretion, inflammatory responses, and vasodilation regulation. This receptor plays critical roles in migraine, post-traumatic stress disorder, and neurodegenerative diseases.

ScreeningBio’s CHO-K1/Human PAC1 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.