期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 80, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2022.129120
关键词
GPR88; [3H]RTI-33; Radioligand binding
This study synthesized and characterized the first GPR88 radio-ligand, [3H]RTI-33, derived from a synthetic agonist RTI-13951-33. [3H]RTI-33 showed specific and saturable binding (KD of 85 nM) in membranes prepared from stable PPLS-HA-hGPR88-CHO cells, and 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.
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 radio-ligand, [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.
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