Table 8.

Inhibitory effects on the specific binding of [¹²⁵I]AT1 and AT1-induced pressor responses in rats.^[43]

Compd	X	Properties of X		BA[a] [%]	IC50[b] [μm]	Inhibition[c] [%] 3h/7 h
		pKa	logP
39		5.3	0.32	5	0.11	100/92
40		6.1	0.9	20	0.42	100/100
41		6.6	1.58	51	0.25	100/100

^[a]Oral bioavailability (BA).

^[b]Receptor affinity as determined by the inhibition of specific binding of [¹²⁵I]AT1 (0.2 nm) to bovine adrenal cortex. The IC₅₀ value is the concentration of compound which inhibits [¹²⁵I]AT1 binding by 50%.

^[c]Percent inhibition of AT1 (0.1 μgkg⁻¹ iv)-induced pressor response at 3 and 7 h after administration of the test compounds (1 mgkg⁻¹ po) in conscious male Sprague–Dawley rats.