TABLE 2.
Compartment | Druga | % Dose/compartment at the following timesb:
|
||||
---|---|---|---|---|---|---|
3 h | 6 h | 18 h | 24 h | 48 h | ||
Liver | AQ | 4.3 ± 1.2 | 3.5 ± 1.0 | 9.2 ± 8.5 | 2.9 ± 1.1 | 0.9 ± 0.2 |
5′-ClPAQ | 13.8 ± 2.7** | 13.6 ± 2.5*** | 17.8 ± 1.6 | 14.8 ± 3.7*** | 10.7 ± 1.6*** | |
CYC | 12.9 ± 5.9** | 12.4 ± 2.0*** | 10.8 ± 1.8 | 10.4 ± 2.2*** | 13.3 ± 1.3***,†† | |
Kidney | AQ | 1.5 ± 0.1 | 1.3 ± 0.4 | 0.6 ± 0.1 | 0.5 ± 0.2 | 0.7 ± 1.3 |
5′-ClPAQ | 3.8 ± 1.1** | 4.5 ± 1.2*** | 9.0 ± 0.6*** | 4.4 ± 1.2*** | 6.0 ± 1.1*** | |
CYC | 2.2 ± 0.9† | 1.8 ± 0.2††† | 1.7 ± 0.1***,††† | 1.7 ± 0.5*,††† | 2.3 ± 0.3*,††† | |
Lung | AQ | 0.7 ± 0.2 | 0.5 ± 0.1 | 0.3 ± 0.1 | 0.2 ± 0.1 | 0.1 ± 0.01 |
5′-ClPAQ | 1.4 ± 0.4 | 2.1 ± 0.7*** | 4.5 ± 0.6*** | 2.7 ± 0.9*** | 2.1 ± 0.4*** | |
CYC | 1.3 ± 0.7 | 1.0 ± 0.2*,† | 0.4 ± 0.1††† | 0.4 ± 0.3**,††† | 0.8 ± 0.2***,††† | |
Spleen | AQ | 0.4 ± 0.1 | 0.4 ± 0.1 | 0.3 ± 0.1 | 0.05 ± 0.1 | 0.01 ± 0.05 |
5′-ClPAQ | 0.9 ± 0.2* | 1.9 ± 0.5*** | 2.3 ± 0.2*** | 2.7 ± 0.7*** | 1.3 ± 0.2*** | |
CYC | 0.6 ± 0.3† | 0.6 ± 0.1††† | 0.4 ± 0.1*,††† | 0.6 ± 0.1††† | 0.7 ± 0.1***,††† | |
Gastrointestinal tract | AQ | 1.4 ± 1.9 | 18.9 ± 4.5 | 24.3 ± 13.6 | 21.7 ± 9.6 | 3.4 ± 2.7 |
5′-ClPAQ | 19.6 ± 4.5** | 18.3 ± 3.4 | 34.1 ± 3.3 | 19.4 ± 4.7 | 10.5 ± 1.2 | |
CYC | 22.4 ± 7.6*** | 17.3 ± 0.9 | 18.7 ± 4.8 | 21.2 ± 3.3 | 5.9 ± 3.8 | |
Blood | AQ | 0.4 ± 0.5 | 1.3 ± 0.2 | 0.2 ± 0.2 | 0.7 ± 0.1 | 0.3 ± 0.01 |
5′-ClPAQ | 0.3 ± 0.1 | 5.2 ± 3.8 | 1.0 ± 0.1 | 1.0 ± 0.05 | 0.4 ± 0.05 | |
CYC | 0.3 ± 0.1 | 0.4 ± 0.0 | 0.3 ± 0.0 | 0.4 ± 0.1 | 0.3 ± 0.1 |
The drug doses are given in the text. AQ, [3H]amodiaquine; 5′-ClPAQ, [3H]5′-ClPAQ; CYC, [3H]cycloquine.
Data are means ± SDs (n = four mice per time point). *, P < 0.05; **, P < 0.01; ***, P < 0.001 compared with amodiaquine; †, P < 0.05; ††, P < 0.01; †††, P < 0.001 for cycloquine compared with 5′-ClPAQ.