TABLE 1

Ki values and inhibition types for the imidaprilat formation

Data generated by nonlinear regression analysis are expressed as mean ± S.E. The concentrations of imidapril ranged from 100 to 500 μM for HLM and HLC, from 25 to 150 μM for RLM, from 15 to 90 μM for RLC, from 20 to 80 μM for RJM, and from 25 to 100 μM for RJC. The concentrations of inhibitors ranged as follows: for carvedilol, 1 to 6 μM for RLM, 1 to 6 μM for RLC, 4 to 24 μM for RJM, and 5 to 30 μM for RJC; for NDGA, 10 to 40 μM for HLM, 2 to 7 μM for HLC, 0.2 to 2 μM for RLM, 0.2 to 1.5 μM for RLC, 3 to 15 μM for RJM, and 2 to 12 μM for RJC; and for procainamide, 25 to 150 μM for HLM and 25 to 100 μM for HLC.


Enzyme Source

Inhibitor

Ki

Inhibition Type
μM
HLM NDGA 13.3 ± 1.5 Mixed
Procainamide 29.3 ± 4.8 Competitive
HLC NDGA 2.9 ± 0.5 Uncompetitive
Procainamide 34.5 ± 2.2 Competitive
RLM Carvedilol 1.6 ± 0.2 Competitive
NDGA 0.4 ± 0.0 Uncompetitive
RLC Carvedilol 2.3 ± 0.3 Mixed
NDGA 0.4 ± 0.0 Uncompetitive
RJM Carvedilol 8.8 ± 0.5 Competitive
NDGA 11.0 ± 2.2 Mixed
RJC Carvedilol 5.1 ± 1.0 Competitive

NDGA
3.2 ± 0.3
Uncompetitive