. 2013 Sep;41(9):1703–1714. doi: 10.1124/dmd.113.052084

TABLE 1.

Pharmacokinetics of VU0403602 and the formation of its principal metabolites (M1, M2) in vivo in male Sprague-Dawley rats after i.p administration (30 mg/kg) in the absence and presence of pretreatment with the cytochrome P450 inactivator 1-aminobenzotriazole (ABT)

Data represent mean values (n = 2).

Analyte	Pretreatment	Plasma C_max	Plasma T_max	Plasma AUC_0-inf	Brain C_max	Brain AUC_0-inf
		μM	h	µMh*	µM	µMh*
VU0403602	—	3.21 (0.005)^a	0.25	3.63 (0.006)^a	11.5 (0.006)^b	7.79 (0.004)^b
	+ABT	11.0 (0.018)^a	0.75	9.64 (0.015)^a	12.9 (0.006)^b	9.64 (0.005)^b
M1	—	0.064 (0.004)^c	1.5	0.046 (0.003)^c	0.406 (0.005)^d	0.258 (0.003)^d
M1	+ABT	0.032 (0.002)^c	1.5	0.003 (0.001)^c	0.031 (0.001)^d	0.031 (0.001)^d
M2^e	—	17.8	1.25	15.8	3.71	3.15
M2^e	+ABT	20.3	1.5	11.7	6.73	4.25

—, Not done; AUC, area under the curve.

^{^a}

Unbound concentrations, f^u 0.0016.

^{^b}

Nonspecific binding, f^u < 0.005.

^{^c}

Unbound concentrations, f^u 0.06.

^{^d}

Nonspecific binding, f^u 0.011.

^{^e}

Unbound concentrations for M2 not determined.