The concentration and concanavalin A (ConA)-dependent microheterogeneity of serum and urinary α1-acid glycoprotein (AGP) were studied in patients with various degrees of renal impairment and compared with healthy control values. Serum concentrations of AGP were significantly higher in hemodialyzed and uremic patients than in the control subjects (1.54 ± 0.42 g/l, p < 0.05, and 1.20 ± 0.40 g/l, p < 0.05, respectively, versus 0.83 ± 0.17 g/l). There was a similar increase in serum α1-protease inhibitor and haptoglobin concentrations in the uremic patients (r = 0.87 and r = 0.70; p < 0.001). Urinary concentrations of AGP were also significantly higher in the hemodialyzed and uremic patients than in the control subjects, despite wide variability in the patients (20 ± 14 mg/24 h, p < 0.05, and 126 ± 160 mg/24 h, p < 0.05, respectively, versus 3 ± 1 mg/24 h). AGP clearance was significantly higher in the uremic patients than in the hemodialyzed patients (p < 0.01) and the control subjects (p < 0.01). The proportions of strongly ConA-reactive AGP fractions were higher in the serum of the hemodialyzed (18.6 ± 5.2%; p < 0.05) and uremic patients (18.1 ± 5.3%; p < 0.05) than in the control subjects (14.5 ± 2.5%). There was a similar difference in the urine samples (26.7 ± 8.2%, p < 0.01; 20.1 ± 6.2%, p < 0.0l, respectively, versus 10.3 ± 4.8%), with also a significant difference between the hemodialyzed and uremic patients (p < 0.05). Moreover, there was a correlation between serum and urinary levels of the strongly ConA-reactive AGP fractions in the uremic patients (r = 0.85). These results show that serum and urinary levels of biantennary AGP glycans are elevated in chronic renal failure not yet requiring hemodialysis, changes that did not seem to depend on the duration or the degree of renal failure. This reflects a chronic inflammatory state, probably due to altered cytokine secretion (principally interleukin-1, interleukin-6 and tumor necrosis factor-α).