Amino acids and their derivatives are common biomarkers for human physiological processes. In this work, we report a metabolome profiling technique for analyzing metabolites containing amines and phenolic hydroxyls or phenols based on SCIEX Triple QuadTM 4500 System .A chemical derivatization strategy based on dansylation reaction for increasing the retention capacity of amines in reversed-phase chromatography and improving the ionization efficiency in mass spectrometry in a complex sample. We developed a fast quantitative method to detect 90 amine-containing metabolites (including amino acids, their methylated and acetylated products, etc.) in 15 minutes. Our results demonstrated that 72 amine metabolites can be detected in mouse tissues, which were used for target metabonomics analysis to find out the potential markers. In addition, we detected 72 amine metabolites in plasma and 88 metabolites in urine with this method. As amines and phenols are important groups of metabolites, profiling these metabolites using the current technique should already be useful for biomarker discovery and biological studies.