Table 7. In Vivo Evaluation for Selected Compounds^a,47.

		pharmacokinetic Profileb			receptor occupancy ED50c
compd	species	%F	T1/2 (hr)	Cl (mL/min/kg)	IV dosing (mg/kg)	PO dosing (mg/kg)
6	rat	45	2.7	26	2.0	4.9
9	rat	14	1.2	8.7	7.2	21
14	rat	67	11.2	0.8	<10
16	rat	23	1.4	10	0.6	8.1
22	rat	34	0.7	24	0.9	4.8
22	dog	83	7.5	3.6
22	rhesus	17	1.5	12
23	rat	13	2.1	13	1.8	3.5
30	rat	3	0.3	18	>3
37	rat	3.1	10.8

^aAbbreviations: %F, oral bioavailability; T_1/2, half-life; Cl, clearance.

^bSprague–Dawley rats (n = 3); oral dose =10 mg/kg, intravenous dose = 2 mg/kg; Beagle dogs (n = 2), intravenous dose = 0.3 mg/kg; Rhesus monkeys (n = 2), oral dose = 1 mg/kg, intravenous dose = 1 mg/kg.

^cSprague–Dawley rats, n = 4 at each dose of 1, 3, and 10 mg/kg; <10 = 70% inhibition at 10 mpk; >3 = 34% inhibition at 3 mpk.