Table 1: Dose-dependence of tissue and body fluid concentrations of K 117 injected intramuscularly to rats.
Sample (tissue or body fluid) |
Concentration (µg/ml± SD) Determined by HPLC-UV |
Tissue Concentration (ng/ml) |
Tissue concentration related to the serum concentration (%) |
Concentration. related to the dose of 1 µmol |
Dose: 0.1 µmol |
Serum |
0.011±0.005 |
110 |
100.0 |
0.567 |
Brain |
0.011±0.005 |
55 |
50.00 |
3.235 |
CSF |
0.010±0.000 |
50 |
45.45 |
5.880 |
Eyes |
0.010±0.002 |
50 |
45.45 |
0.990 |
Lung |
0.055±0.004 |
275 |
250.0 |
2.350 |
Testis |
0.006±0.004 |
30 |
27.27 |
5.450 |
Liver |
0.043±0.005 |
215 |
195.5 |
39.09 |
Kidney |
0.340±0.012 |
1700 |
1545 |
42.50 |
Inner ear |
0.079±0.005 |
395 |
359.0 |
3.361 |
Dose: 0.3 µmol |
Serum |
0.022±0.008 |
220 |
100.0 |
0.378 |
Brain |
0.015±0.004 |
75 |
34.09 |
1.470 |
CSF |
0.012±0.003 |
60 |
27.27 |
2.352 |
Eyes |
0.014±0.005 |
70 |
31.82 |
0.460 |
Lung |
0.051±0.002 |
255 |
115.9 |
0.720 |
Testis |
0.009±0.004 |
45 |
20.45 |
2.727 |
Liver |
0.077±0.027 |
385 |
175.0 |
3.208 |
Kidney, |
0.768±0.009 |
3840 |
1745 |
0.920 |
Inner ear |
0.088±0.010 |
440 |
200.0 |
0.838 |
Dose: 1.0 µmol |
Serum |
0.194±0.003 |
1940 |
100.0 |
1.00 |
Brain |
0.034±0.003 |
170 |
8.762 |
1.00 |
CSF |
0.017±0.011 |
85 |
4.381 |
1.00 |
Eyes |
0.101±0.013 |
505 |
26.03 |
1.00 |
Lung |
0.234±0.006 |
1170 |
60.30 |
1.00 |
Testis |
0.011±0.004 |
55 |
2.835 |
1.00 |
Liver |
0.080±0.010 |
400 |
20.61 |
1.00 |
Kidney, |
2.781±0.026 |
13905 |
716.7 |
1.00 |
Inner ear |
0.235±0.006 |
1175 |
60.56 |
1.00 |
Dose: 3.0 µmol |
Serum |
0.576±0.013 |
5760 |
100.0 |
0.989 |
Brain |
0.083±0.006 |
415 |
7.204 |
0.813 |
CSF |
0.023±0.016 |
115 |
1.996 |
0.451 |
Eyes |
0.222±0.005 |
1111 |
19.28 |
0.733 |
Lung |
0.601±0.013 |
3005 |
52.17 |
0.856 |
Testis |
0.093±0.009 |
465 |
8.072 |
2.818 |
Liver |
0.194±0.020 |
970 |
16.84 |
0.808 |
Kidney |
4.698±0.159 |
23490 |
407.8 |
0.563 |
Inner ear |
0.442±0.064 |
2210 |
38.36 |
0.626 |
Dose: 10.0 µmol |
Serum |
2.289±0.121 |
22890 |
100.0 |
1.179 |
Brain |
0.360±0.004 |
1800 |
7.863 |
1.058 |
CSF |
0.075±0.004 |
375 |
1.638 |
0.441 |
Eyes |
0.763±0.035 |
3815 |
16.66 |
0.755 |
Lung |
1.788±0.033 |
8940 |
39.05 |
1.770 |
Testis |
0.484±0.003 |
2420 |
10.57 |
4.400 |
Liver |
0.153±0.002 |
765 |
3.342 |
0.190 |
Kidney |
11.219±0.099 |
56095 |
245.06 |
0.403 |
Inner ear |
1.246±0.047 |
6230 |
27.21 |
0.530 |