GPR88 is an orphan G protein-coupled receptor which has been implicated in a number of striatal-associated disorders. Herein we describe the synthesis and pharmacological characterization of the first GPR88 radioligand, [3H]RTI-33, derived from a synthetic agonist RTI-13951-33. [3H]RTI-33 has a specific activity of 83.4 Ci/mmol and showed one-site, saturable binding (KD of 85 nM) in membranes prepared from stable PPLS-HA-hGPR88-CHO cells. A competition binding assay was developed to determine binding affinities of several known GPR88 agonists. This radioligand represents a powerful tool for future mechanistic and cell-based ligand-receptor interaction studies of GPR88.
Synthesis and pharmacological validation of a novel radioligand for the orphan GPR88 receptor
Decker, A. M., Rahman, M. T., Kormos, C. M., Hesk, D., Darcq, E., Kieffer, B. L., & Jin, C. (2023). Synthesis and pharmacological validation of a novel radioligand for the orphan GPR88 receptor. Bioorganic and Medicinal Chemistry Letters, 80, 129120. . https://doi.org/10.1016/j.bmcl.2022.129120
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