2-(3,4-Dichlorophenoxy) triethylamine (DCPTA) regulates plant development; however, the molecular basis of this regulation is poorly understood. In this study, RNA sequencing (RNA-seq) analysis and physiological indexes of maize seedlings (three-leaf stage) treated with 15% polyethylene glycol (PEG) with/without DCPTA were investigated to explore the possible mechanism of exogenous DCPTA-improved drought tolerance. In the library pair comparisons of DCPTA vs. the control, PEG vs. the control, and PEG + DCPTA vs. PEG, totals of 19, 38 and 20 differentially expressed genes (DEGs) were classified as being involved in metabolic processes, respectively; totals of 5, 11, and 6 DEGs were enriched in the nitrogen (N) metabolic pathway, respectively. The genes encoding nicotinamide adenine dinucleotide-nitrate reductase (NADH-NR), ferredoxin-nitrite reductase (Fd-NiR), reduced ferredoxin-glutamate synthase (Fd-GOGAT), and chloroplastic glutamine synthetase (GS 2) were common in response to PEG-simulated drought stress with/without DCPTA treatment. Moreover, DCPTA maintained stable gene relative expression levels and protein abundances of NADH-NR, Fd-NiR, GS2, and Fd-GOGAT. Moreover, exogenous DCPTA partially mitigated PEG-simulated drought-induced reductions in the enzymatic activities of NR, nitrite reductase (NiR), glutamine synthase (GS), glutamine oxoglutarate aminotransferase (GOGAT), and transaminase, as well as in the contents of nitrate (NO 3 − ), nitrite (NO 2 − ) and soluble proteins and increases in the contents of ammonium (NH 4 + ) and free amino acids. Together, our results indicate that exogenous DCPTA improved plant growth and drought tolerance by regulating N-mechanism enzymatic activities involved in transcription and enzymatic protein synthesis.