Somatostatin receptor 1 (SSTR1), a key GPCR, plays an essential role in regulating endocrine and nervous system functions by inhibiting adenylyl cyclase activity and decreasing intracellular cAMP levels. Dysregulated SSTR1 signaling is associated with various conditions, including neuroendocrine tumors, pituitary adenomas, and hormone-related disorders. Traditional methods for studying GPCRs often fail to fully capture the intricate signaling mechanisms of receptors like SSTR1.

The Screen Quest™ Live Cell Somatostatin Receptor 1 (SSTR1) cAMP Assay Service Pack is designed for real-time, high-throughput monitoring of intracellular cAMP changes associated with SSTR1 activation using transfected cell lines and Calbryte™ 520 wash-free calcium fluorescence detection methods. Unlike conventional assays that require cell lysis, this assay maintains cellular integrity, providing both temporal and spatial resolution of SSTR1-mediated signaling events. The assay uses cell lines engineered to express SSTR1 alongside a promiscuous G-protein Gα16. This co-expression enables SSTR1, which typically signals via inhibition of adenylyl cyclase, to couple to Gq signaling, leading to intracellular calcium mobilization. Activation of SSTR1 by specific ligands, such as somatostatin or its analogs, can be detected using calcium-sensitive dyes like Calbryte™ 520 AM, Cal-520® AM, Fluo-8® AM, Fluo-4™ AM, or other compatible no-wash calcium kits.

This service pack includes all components required for precise measurement of SSTR1-mediated cAMP changes using FLIPR, FDSS, or equivalent fluorescence microplate readers. It offers researchers a reliable tool to investigate SSTR1 signaling pathways and assess therapeutic compounds targeting this receptor, particularly in endocrine and neuroendocrine research.