Metabolomics, as a promising and powerful approach, refers to comprehensive assessment and identification of small molecule endogenous metabolites in a biological system which is capable of further understanding the mechanisms of diseases for early diagnosis, effective treatment and prognosis. Acute kidney injury (AKI) induced by contrast is a serious complication in patients undergoing administration of iodinated contrast media. It is becoming a major health concern in clinic, however, the molecular mechanisms of contrast-induced acute kidney injury (CI-AKI) have not been well characterized. In this study, we used serum metabolomics based on liquid chromatography-mass spectrometry (LC-MS) combined with pattern recognition to explore and characterize potential metabolites and metabolic pathway in an experimental model for CI-AKI. Seventeen differentiating metabolites in the serum were identified involving the pivotal metabolic pathways related to tryptophan metabolism, glycerophospholipid metabolism, steroid hormone biosynthesis, pyrimidine metabolism, sphingolipid metabolism, aminoacyl-tRNA biosynthesis. Our study provides novel insight into pathophysiologic mechanisms of AKI by changing biomarkers and pathways.