Screening of GPCR-antagonists using the calcium mobilisation assay

The nucleotide receptor family P2Y comprises of G protein-coupled receptors that show potential as drug targets for various disorders. Targeting the P2Y2 subtype is particularly promising, since antagonists could be effective against tumour metastasis, excessive inflammatory reactions, atherosclerosis, kidney disorders, and osteoporosis [1-3]. The precise role of the P2Y2 receptor in these conditions is often not clear, which can be partially attributed to the limited availability of potent and selective antagonists that are required for pharmacological studies [4]. To characterise potential antagonists, three commercially available compounds were screened for P2Y2 receptor inhibition using the calcium mobilisation assay with two different fluorescent dyes measured on a TriStar² LB 942 plate reader. Reliable and consistent results were obtained.