Drug radioequivalent concentrations (microgram equivalents per gram) in tissues of Long-Evans male and female rats administered an oral dose (13.8 mg/kg) of [14C]LAS
The LLOQ was 0.6 μg Eq/g.
Tissue | 1 h | 3 h | 8 h | 12 h | 168 h | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| M | F | M | F | M | F | M | F | M | F | ||||||
| Adipose: brown | 5.6 | 6.3 | 4.0 | 3.8 | 2.2 | 1.7 | —a | — | — | — | |||||
| Adrenal gland | 24 | N.D. | 13 | 11 | 6.4 | 4.1 | — | — | — | — | |||||
| Blood: systemic | 1.7 | 1.2 | 0.8 | — | — | — | — | — | — | — | |||||
| Bone marrow | 7.1 | 5.8 | 4.6 | 4.4 | 3.3 | 2.5 | — | — | — | — | |||||
| Contents: gastric | 572 | 490 | 288 | 320 | 124 | — | — | — | — | — | |||||
| Contents: intestinal | 261 | 313 | 320 | 375 | 231 | 79 | 48 | 22 | 3.4 | ||||||
| CNS tissuesb | 1.8 | 1.6 | 1.2 | 0.9 | 0.7 | 0.7 | — | — | — | — | |||||
| Kidney | 8.6 | 8.3 | 6.7 | 4.9 | 2.3 | 1.5 | 0.9 | — | — | — | |||||
| Lacrimal gland | 8.2 | 6.3 | 11 | 8.5 | 20 | 19 | 16 | 15 | — | — | |||||
| Liver | 23 | 27 | 20 | 16 | 6.7 | 4.6 | 3.2 | 2.1 | — | — | |||||
| Lung | 21 | 16 | 14 | 16 | 6.8 | 10 | 2.8 | 1.6 | — | — | |||||
| Myocardium | 7.1 | 6.0 | 4.4 | 3.4 | 1.5 | 1.1 | — | — | — | — | |||||
| Pancreas | 16 | 15 | 15 | 12 | N.D. | 6.0 | 2.5 | 2.1 | — | — | |||||
| Salivary gland | 11 | 8.8 | 9.2 | 8.0 | 6.5 | 7.5 | 0.9 | — | — | — | |||||
| Skeletal muscle | 2.5 | 2.6 | 2.3 | 1.7 | 0.9 | — | — | — | — | — | |||||
| Spleen | 17 | 16 | 11 | 8.7 | 4.5 | 4.1 | 1.5 | 0.9 | — | — | |||||
| Testis or ovary | 0.8 | 8.5 | 1.0 | N.D. | 1.8 | 2.7 | 1.8 | — | — | — | |||||
| Thymus | 4.0 | 3.8 | 3.8 | 3.0 | 2.7 | 2.5 | 0.9 | 0.7 | — | — | |||||
| Uvea | 12 | 8.8 | 12 | 10 | 21 | 15 | 14 | 13 | 7.1 | 4.6 | |||||
| Whole-body | 16 | 22 | 15 | 24 | 18 | 10 | 6.0 | 2.4 | — | — | |||||
M, male; F, female; N.D., sample was not obtained at this time point.
↵ a Tissue [14C]LAS radioequivalents either declined below the LLOQ, or the tissue was indistinguishable from background (—).
↵ b Noncircumventricular central nervous system (CNS) tissues (e.g. cerebellum, cerebrum, medulla oblongata, mesencephalon, olfactory bulb, and pons) were collectively assessed for [14C]LAS radioequivalent concentrations due to the low amounts of distributed radioactivity into the brain.