Table 2

Pharmacokinetic parameters of ET_A antagonists 7 to 16 in rat

Compound	t_1/2	CL	fu	CL_u	Vd	F	Estimated A
	h	ml/min/kg		ml/min/kg	l/kg	%
7	1.4	72	0.01	7200	1.2	16	55
8	0.9	38	0.002	19000	2.8	60	100
9	0.9	36	0.002	18000	2.9	100	100
10	5.4	8.7	0.005	1740	4.0	100	100
11	1.7	34	0.002	17000	5.0	100	100
12	1.1	33	0.017	1940	3.0	56	70
13	0.4	37	0.011	3364	1.1	49	75
14	0.5	22	0.005	4400	0.5	95	100
15	0.6	42	0.006	7000	2.2	30	60
16	0.9	49	0.018	2722	3.8	8.0	20

Pharmacokinetic studies were performed in male rats after single intravenous (2 mg/kg, n = 1) and oral (10 mg/kg, n = 1) doses.

fu, function unbound in plasma; CL_u, unbound systemic clearance; Vd, volume of distribution; F, bioavailability; A, absorption.