Table 8.

Pharmacokinetic Profiles of Top Analogues in CD1 Mice^a

compd	route	dose	Cl (mL/min/kg)	T1/2 (h)	bCmax (μg/mL)	AUClast (μg/mL·h)	Vss (L/kg)	F (%)
43	IV	10	16.1	5.2	41.79	10.57	1.79
	PO	40		2.78	5.26	31.39		73.8
44	IV	10	75	5.1	4.77	2.32	10.3
	PO	50		10.7	1.26	13.52		106
46	IV	10	97	5.75	5.5	1.82	13.9
	PO	50		3.2	1.82	3.44		38
47	IV	10	128	4.9	3.32	1.36	17.9
	PO	50		3.54	2.03	2.65		39
52	IV	10	10.4	5.3	33.82	16.53	1.7
	PO	50		2.6	8.83	53.54		64
61	IV	10	72.3	5	4.57	2.28	12.5
	PO	50		3.7	2.28	10.17		89
69	IV	10	74.7	5.5	6.44	2.81	13.3
	PO	50		3.1	1.2	9.22		83
74	IV	10	74.7	6.5	35.33	6.65	2.5
	PO	50		3.2	4.73	12.24		37
75	IV	10	18.6	5.8	58.23	9.6	1.47
	PO	50		3.7	6.85	20.03		42

^aValues calculated from drug concentration in plasma following IV or PO dosing. n = 3, 8 time points taken over 24 h. Compounds were formulated as a solution in PBS with 1.1 equiv of NaOH (final pH 7–8).

^bC_max = C₀ (t = 0) for IV administration. All pharmacokinetic studies were conducted at Pharmaron, Inc.