G protein-coupled receptors (GPCRs) are a large family of transmembrane receptors that are significant drug targets. They function as enzymes that activate G-proteins. GPCRs couple to three main families of Gα subunits: Gαi/o, Gαs, and Gαq.

The coupling specificity depends on the GPCR and its cellular environment. Gαs and Gαi subunits operate through the cAMP pathway, either activating or inhibiting adenylate cyclase, which converts ATP to cAMP.

In this application note, the AlphaScreen™-based cAMP detection technology has been used to study Gαi-coupled receptors, specifically the 5-hydroxytryptamine-1A (5-HT1A) serotonergic receptor. The note demonstrates the utility of the AlphaScreen-based cAMP Assay kit for the pharmacological characterization and potential high-throughput screening of Gαi-coupled receptors.

For research use only. Not for use in diagnostic procedures.