Table 6. In Vitro Stability and in Vivo Pharmacokinetic Properties of Selected Compounds in Mice.
iv dosing (5 mg/kg) |
po
dosing (10 mg/kg) |
|||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|
cAMP pEC50a | aq. sol. (μM)a | log D7.4a | MLM (%)b | t1/2 (min) | Vd (mL/kg) | CLtotal (mL/min/kg) | t1/2 (min) | tmax (min) | cmax (ng/mL) | AUCinf (ng.min/mL) | F (%) | |
1 | 6.28 | 190 | 2.05 | 52 | 62.2 | 759 | 8.45 | 89.7 | 15 | 7470 | 865 000 | 73 |
16 | 6.89 | 5 | 3.19 | 1 | 22.3 | 629 | 19.6 | 60.8 | 30 | 5740 | 423 000 | 88 |
35 | 5.92 | 199 | 2.64 | 23 | ||||||||
47 | 6.60 | 1 | 3.39 | 2 | ||||||||
51 | 6.72 | 1 | 2.59 | 12 | ||||||||
57 | 6.84 | 33 | 4.25 | 1 | 11.4 | 1150 | 70.3 | 63.5 | 30 | 561 | 33 800 | 36 |
62 | 6.60 | 5 | 3.73 | 1 | ||||||||
63 | 6.79 | 9 | >4.3 | 41 | 37.8 | 1110 | 20.3 | 51.8 | 15 | 3800 | 325 000 | 66 |