Abstract: The increasing attention to micropollutants including pharmaceuticals in the environment is driven by advancements in analytical techniques and the potential environmental risks.G protein-coupled receptor (GPCR) account for 40%of pharmaceutical targets.There are around 700 GPCR-acting pharmaceuticals with large consumptions.Wastewater treatment plants are unable to completely remove GPCR-acting pharmaceuticals from sewage, which leads to their eventual release into aquatic environment and posing potential risks to aquatic organisms.However, only limited GPCR-acting pharmaceuticals are investigated in the aquatic environment, and their ecological risks to aquatic organisms remain largely unknown.This review provides a summary of recent studies on GPCR-acting pharmaceuticals, analyzing their main sources, migration and transformation, methods for analysis and detection of GPCR-acting pharmaceuticals in the environment, pollution and ecotoxicity, and offers prospects for future research.