Table 1.
Summary of GUS Inhibitory Activity of Studied Drugs
| Drug | Drug Class | Currently Marketed |
E. coli GUS Enzyme Assaya |
B. taurus GUS Enzyme Assaya |
E. coli
Cell-Based Assaya |
|---|---|---|---|---|---|
| IC50 ± SD (nM) | IC50 ± SD (nM) | IC50 ± SD (nM) | |||
| Nialamide | Irreversible MAOI | No | 71 ± 32 | 74,813 ± 1,841 | 17 ± 2 |
| Isocarboxazid | Irreversible MAOI | Yes | 128 ± 56 | >100,000 | 336 ± 120 |
| Phenelzine | Irreversible MAOI | Yes | 2,282 ± 1041 | NDb | 7,123 ± 1650 |
| Amoxapine | Tricyclic Antidepressant | Yes | 388 ± 98 | >100,000 | 119 ± 61 |
| Loxapinec | Tricyclic Antidepressant | Yes | >100,000 | ND | >100,000 |
| Mefloquine | Antimalarial | Yes | 1,212 ± 234 | ND | 5,961 ± 1526 |
IC50 value determinations were performed at least three times, with average IC50 values and standard deviations (SD) shown. The range of average Hill slopes for all measurable IC50 curves (where at least 50% inhibition was obtained) was 0.84 to 1.26.
ND = not determined;
This drug was included as a study control