Objective:To study changes of PRA, AngⅡ and NE during metoprolol therapy in patients with congestive heart failure(CHF).Methods:All patients received baseline therapy(digitalis, diuretic and ACEI) were randomly assigned to control group and treatment group. Plasma levels of norepinephrine (NE), plasma renin activity(PRA), angiotensinⅡ(AngⅡ) were measured before and 1 month,3 months, 6 months after initiation of metoprolol treatment.Results:Metoprolol group had a lower activation of neuroendocrine, especially in PRA and NE , compared with pretreatment, both had significant differences (P 0.01,P 0.01). In the meantime, left ventrvicular ejection fraction(LVEF) was elevated. While the levels of PRA, AngⅡ, NE had dramatic elevation (P 0.01,P 0.01,P 0.05) in the control group.Conclusion:There still exists activation of neuroendocrine during ACEI medication in CHF patients, and it can be suppressed by adiministration of metoprolol and in the meantime, LVEF was elevated.