TABLE 2.
Radioactivity concentrations (μg equivalents/g) determined by quantitative whole-body autoradiography in tissues and blood through 168 h after a single oral dose of [14C]PPI-1011 to Group 1 Sprague-Dawley male rats (Nominal Dose Levels: 200 μCi/kg and 100 mg/kg).
| Rat Identification: | 01M | 02M | 03M | 04M | 05M | 06M |
|---|---|---|---|---|---|---|
| Time (Post-Dose): | 8 h | 12 h | 18 h | 24 h | 48 h | 168 h |
| Adipose - Brown | 171 | 426 | 66.0 | 133 | 132 | 89.0 |
| Adipose - Brown (Vessel Wall) | 301 | 383 | 94.2 | 110 | 98.6 | 76.7 |
| Adipose - Visceral | 83.1 | 170 | 75.6 | 71.6 | 111 | 90.7 |
| Adipose - Subcutaneous | 74.0 | 242 | 73.9 | 70.1 | 82.1 | 89.3 |
| Adrenal Glanda | 195 | 367 | 185 | 155 | 201 | 142 |
| Bladder Wall | 86.0 | 19.3 | 14.5 | 7.69 | 10.7 | nd |
| Blood - QWBA | 35.4 | 16.4 | 9.62 | 5.62 | 4.19 | 2.56 |
| Bone Marrow | 23.5 | 23.0 | 22.3 | 18.3 | 15.7 | 4.69 |
| Bone Surface | 2.30 | 1.15 | 1.25 | 0.513 | 0.508 | nd |
| Diaphragm | 55.6 | 59.9 | 40.4 | 37.4 | 23.0 | 11.7 |
| Exorbital Lacrimal Gland | 28.7 | 34.5 | 8.74 | 9.66 | 6.13 | 7.36 |
| Harderian Gland | 14.4 | 10.8 | 14.7 | 10.5 | 11.1 | 3.67 |
| Intra-Orbital Lacrimal Gland | 10.4 | 8.89 | 8.91 | 7.56 | 6.64 | 5.01 |
| Kidney | 42.9 | 45.3 | 36.1 | 24.7 | 24.6 | 14.5 |
| Renal Cortex | 41.4 | 46.6 | 38.1 | 26.8 | 24.3 | 15.3 |
| Renal Medulla | 51.0 | 53.2 | 23.0 | 25.8 | 22.7 | 11.8 |
| Liver | 313 | 269 | 121 | 73.4 | 40.0 | 7.50 |
| Lung | 74.0 | 51.9 | 45.4 | 30.2 | 22.9 | 11.2 |
| Lymph Node | 22.7 | 22.6 | 22.5 | 17.4 | 20.0 | 12.3 |
| Muscle | 10.3 | 12.6 | 9.63 | 7.57 | 8.42 | 7.01 |
| Myocardium | 92.0 | 72.6 | 42.4 | 31.0 | 26.6 | 13.4 |
| Nasal Turbinates | 16.0 | 10.6 | 6.43 | 4.81 | 5.03 | 4.29 |
| Pancreas | 66.3 | 52.7 | 39.8 | 24.8 | 28.0 | 18.2 |
| Parotid Gland | 39.1 | 30.4 | 35.2 | 20.5 | 20.9 | 12.3 |
| Salivary Gland | 53.3 | 31.4 | 28.8 | 21.3 | 22.9 | 15.4 |
| Skin - Non-Pigmented | 15.0 | 18.0 | 12.0 | 9.26 | 13.4 | 10.2 |
| Spleen | 105 | 111 | 71.3 | 46.3 | 33.1 | 9.36 |
| Thymus | 10.7 | 12.2 | 11.8 | 9.79 | 9.58 | 7.84 |
| Thyroid | 49.9 | 43.1 | 38.5 | 27.7 | 27.2 | 18.9 |
| Ocular - Lens | nd | nd | nd | nd | nd | nd |
| Ocular - Uveal Tract | 6.97 | 6.57 | 5.32 | 4.27 | 4.78 | 6.48 |
| Ocular - Vitreous Body | nd | nd | nd | nd | nd | nd |
| Ocular - Whole Eye | 1.83 | 2.03 | 1.65 | 1.14 | 1.30 | 1.55 |
| Cerebellum | 2.70 | 2.69 | 3.03 | 2.08 | 2.60 | 3.59 |
| Cerebrum | 2.39 | 2.22 | 2.49 | 1.61 | 2.23 | 2.94 |
| Choroid Plexus | 14.9 | 17.1 | 12.8 | 9.85 | 14.4 | 10.4 |
| Colliculus | 3.50 | 3.03 | 2.94 | 2.06 | 3.30 | 3.97 |
| Medulla Oblongata | 2.40 | 2.44 | 2.23 | 1.98 | 2.45 | 3.13 |
| Olfactory Bulb | 2.16 | 2.01 | 1.75 | 2.07 | 2.01 | 2.25 |
| Pineal Gland | 11.9 | 12.1 | 16.2 | 10.8 | 16.4 | 12.0 |
| Pituitary Gland | 21.2 | 21.2 | 22.0 | 16.7 | 19.2 | 12.9 |
| Spinal Cord | 2.71 | 2.76 | 3.20 | 1.75 | 2.56 | 3.33 |
| Thalamus | 2.27 | 2.31 | 2.20 | 1.71 | 1.91 | 2.78 |
| Whole Brain | 2.60 | 2.48 | 2.70 | 1.95 | 2.45 | 3.08 |
| Epididymis | 39.8 | 70.9 | 67.7 | 40.4 | 6.81 | 7.75 |
| Preputial Gland | 33.6 | 214 | 78.0 | 112 | 76.5 | 69.0 |
| Prostate | 49.6 | 11.8 | 28.0 | 56.7 | 7.15 | 4.44 |
| Seminal Vesicles | 12.8 | 2.99 | as | 5.38 | 9.12 | nd |
| Testis | 2.65 | 4.12 | 5.09 | 4.31 | 4.02 | 3.08 |
| Cecum | as | 450 | 177 | 231 | 34.3 | as |
| Esophagus | 17.4 | 16.9 | 15.0 | 9.46 | 10.8 | 5.34 |
| Gastric Mucosa | 91.2 | 67.8 | 70.1 | 48.7 | 37.5 | 14.5 |
| Large Intestines | 12.5 | 209 | 154 | 180 | 19.1 | 14.0 |
| Small Intestines | 609 | 347 | 239 | 247 | 43.3 | 139 |
| Stomach | 22.6 | 22.9 | 21.6 | 10.8 | 8.01 | 4.97 |
aas: tissue was soaked with adipose. nd: radioactivity was not detectable