TABLE 2.
Effects of various esterase inhibitors on the conversion of CS-8958 to R-125489 in mouse trachea and lung S9 fractionsa
Condition | CS-8958 hydrolase activity (% of control) in S9 fractionsb |
|
---|---|---|
Trachea | Lung | |
Control | 100.0 | 100.0 |
DFP | 44.1 | 13.6 |
Eserine | — | 31.9 |
BNPP | — | 21.0 |
DTNB | — | 42.0 |
EDTA | — | 130.7 |
PCMB | — | 106.5 |
Various esterase inhibitors (final concentration, 1 mM) were each added to the trachea and lung S9 fractions 10 min before the addition of [14C]CS-8958 (final concentration, 10 μM) in order to examine their effects on its hydrolysis at 37°C. The experiment was performed in the presence of 1% dimethyl sulfoxide. The control values for the hydrolase activities were 4.51 and 1.01 pmol/min/mg in lung and trachea S9 fractions, respectively.
Values are means for duplicate experiments. —, not tested due to the limitations of the matrix.