Objective: To investigate the effects of desmopressin acetate and pituitrin on the proliferation, contraction, and secretion of hepatic stellate cells (HSCs). Methods: The human HSC cell line LX-2 was selected as the research model. And three groups were designed: blank control group, desmopressin acetate group (three subgroups: 1×10-10mol/L, 1×10-9mol/L, and 1×10-8mol/L desmopressin acetate), and pituitrin group (three subgroups: 0.1 U/L, 1.0 U/L, and 10.0 U/L pituitrin). Water-soluble tetrazolium salt (WST)-1 assay was used to evaluate cell proliferation; collagen gel contraction assay was used to assess cell contraction; enzyme-linked immunosorbent assay (ELISA) was used to identify cell secretion. The data was subjected to one-way analysis of variance. Results: (1) The results of WST-1 assay showed that the values of A450in three desmopressin acetate subgroups (1×10-10mol/L, 1×10-9mol/L, and 1×10-8mol/L) were 0.459±0.017, 0.467±0.024, and 0.436±0.015, respectively. And the values of A450 in three pituitrin subgroups (0.1 U/L, 1.0 U/L, and 10.0 U/L) were 0.495±0.011, 0.507±0.015, and 0.501±0.009, respectively. Compared with the control group, the desmopressin acetate at high concentration significantly inhibited the cell proliferation (P< 0.05), but the pituitrin at three different concentrations significantly promoted the cell proliferation (P< 0.05). (2) The collagen gel area ratios in three desmopressin acetate subgroups (1×10-10mol/L, 1×10-9mol/L, and 1×10-8mol/L) were 77.07±4.42, 75.85±3.70, and 72.74±3.92, respectively. And the collagen gel area ratios in three pituitrin subgroups (0.1 U/L, 1.0 U/L, and 10.0 U/L) were 57.83±3.96, 50.28±6.69, and 43.56±7.68, respectively. Compared with the control group, the pituitrin at three different concentrations significantly reduced the collagen gel area (P< 0.01). (3) The matrix metalloproteinase(MMP)-2 concentrations in three desmopressin acetate subgroups (1×10-10mol/L, 1×10-9mol/L, and 1×10-8mol/L) were 13.321±0.098, 12.230±0.153, and 12.061±0.126, respectively. And the MMP-2 concentrations in three pituitrin subgroups (0.1 U/L, 1.0 U/L, and 10.0 U/L) were 12.899±0.150, 13.662±0.152, and 13.698±0.119, respectively. Compared with the control group, the desmopressin acetate at low concentration significantly increased the secretion of MMP-2 (P< 0.01); the desmopressin acetate at high concentration significantly decreased the MMP-2 concentration (P< 0.05); the pituitrin at three different concentrations significantly increased the MMP-2 concentration (P< 0.01). The transforming growth factor-beta 1 (TGF-β1) concentrations in three desmopressin acetate subgroups (1×10-10mol/L, 1×10-9mol/L, and 1×10-8mol/L) were 5.233±0.102, 17.749±0.188, and 36.060±0.227, respectively. And the TGF-β1 concentrations in three pituitrin subgroups (0.1 U/L, 1.0 U/L, and 10.0 U/L) were 15.615±0.099, 38.460±0.209, and 49.053±0.115, respectively. Compared with the control group, desmopressin acetate and pituitrin significantly promoted the secretion of TGF-β1 in a concentration-dependent manner (P< 0.01) and pituitrin had a stronger effect than desmopressin acetate (P< 0.01). Desmopressin acetate and pituitrin had no effect on the secretion of the collagenase type I and III (P> 0.05). Conclusion: Desmopressin acetate and pituitrin can induce the changes in the function and morphology of HSCs and may increase vascular resistance in the hepatic sinus. However, desmopressin acetate has less influence on HSCs than pituitrin.