Table 2.

Pharmacokinetic parameters of 1 analogs.

	i.v. PK parametersa			p.o. PK parametersb
Compound	AUC0-inf (min·µg·mL−1)	CL (mL·min–1·kg−1)	t1/2 (min)	Cmax (µg·mL−1)	AUC0-inf (µg·min·mL−1)	F (%)
1	519 ± 115	4.9 ± 0.9	11 ± 2	0.4 ± 0.2	66 ± 41	1.3 ± 0.7
2	nd	nd	nd	<LD	<LD	na
3	nd	nd	nd	0.03 ± 0.01	2.9 ± 0.8	na
4	304 ± 60	8.4 ± 1.9	10.6 ± 0.7	0.70 ± 0.07	99.8 ± 13.6	3.5 ± 0.2
5	63 ± 47	46.3 ± 4.5	10.6 ± 2.1	0.09 ± 0.01	16.8 ± 4.2	3.7 ± 0.3
6	209 ± 76	9.6 ± 0.1	15.1 ± 1.3	0.14 ± 0.01	18.1 ± 2.1	1.0 ± 0.4
7	184 ± 30	13.6 ± 2	15.5 ± 10.6	0.10 ± 0.01	4.0 ± 0.9	0.3 ± 0.1
8	1043 ± 326	2.5 ± 0.9	32.5 ± 7.4	0.46 ± 0.30	188 ± 110	1.8 ± 0.9
9	1981 ± 200	1.3 ± 0.1	121 ± 18	0.50 ± 0.16	140 ± 46	0.80 ± 0.15
10	959 ± 135	2.6 ± 0.5	62 ± 6.4	0.56 ± 0.12	198 ± 49	2.0 ± 0.08

^ai.v. dose (D_i.v.) = 2.5 mg/kg.

^bp.o. dose (D_p.o.) = 25 mg/kg. Values are reported as the mean ± SD. AUC_0-inf: area under the plasma concentration-time curve from time 0 to infinity, CL: clearance, t_1/2: terminal elimination half-life, C_max: maximum plasma concentration, F: relative oral bioavailability calculated as follows F = 100 × [(AUC_p.o × D_i.v.)/(AUC_i.v. × D_p.o.)], nd: not determined, na: not applicable, LD: below the limit of detection.