Table 7. In Vivo Pharmacokinetic Properties of Selected Compounds in Rats (0.3 mg/kg iv bolus and 1.0 mg/kg po).
compd | AUCnormiv [kg·h/L] | CL [L/h/kg] | Vss [L/kg] | MRTiv [h] | AUCnormpo [kg·h/L] | Fa [%] | fu [%] |
---|---|---|---|---|---|---|---|
rat/human/rabbit | |||||||
25 | 1.3 | 0.79 | 1.1 | 2.1 | 0.87 | 67 | 9.1/4.5/8.6 |
34 | 1.0 | 0.98 | 1.8 | 1.9 | 0.53 | 53 | 15/5.2/14 |
71 | 1.5 | 0.67 | 0.98 | 1.5 | 0.67 | 42 | n.d.b |
75 | n.d. | n.d. | n.d. | n.d. | 0.46 | n.d. | n.d. |
76 | n.d. | n.d. | n.d. | n.d. | 0.45 | n.d. | n.d. |
77 | n.d. | n.d. | n.d. | n.d. | 0.84 | n.d. | n.d. |
78 | 2.0 | 0.51 | 0.83 | 1.6 | 1.1 | 53 | 2.2/7.0/16 |
79 | n.d. | n.d. | n.d. | n.d. | 1.3 | n.d. | n.d. |
80 | 2.2 | 0.46 | 0.76 | 2.5 | 1.3 | 60 | 2.4/6.4/14 |
81 | 1.7 | 0.58 | 1.0 | 1.8 | 0.56 | 33 | n.d. |
82 | 1.2 | 0.83 | 1.5 | 1.8 | 0.72 | 60 | n.d. |
83 | 2.2 | 0.45 | 1.4 | 3.1 | 0.87 | 40 | n.d. |
Oral bioavailability.
n.d.: not determined.