Table 1.
Tissue: blood area under curve (AUC) ratio of radioactivity (T:B) | Calculated from quantitative whole body autoradiography studies (QWBA) studies by dividing the AUC of drug radioactivity concentration in tissues by that in blood |
Tissue: plasma ratio (T:P) | Calculated from rat metabolism studies by dividing tissue concentrations of either parent drug or radioactivity by the corresponding plasma concentration at the same sample time |
Base pKa | Basic pKa predicted using proprietary software |
Acid pKa | Acidic pKa predicted using proprietary software |
Predicted tissue/plasma partition coefficient (Kp) | Predicted using Lukacova option in Gastroplus software version 8.6 |
Chromatographic hydrophobicity index – immobilized artificial membrane (CHI-IAM) | A measure of phospholipid binding derived from high-performance liquid chromatography (HPLC) retention using an immobilized artificial membrane stationary phase |
cLogP | A measure of lipophilicity. cLogP is the logarithm of the partition coefficient between n-octanol and water log(coctanol/cwater) predicted from structure |