TABLE 1

Apparent kinetic parameters for glucuronidation of amitriptyline, imipramine, clomipramine, and trimipramine by pooled human liver microsomes and human recombinant UGT2B10 and UGT1A4

Data are presented as mean ± S.E. of parameter fit. See Materials and Methods for individual kinetic equation.

	K_m^{^a} or S₅₀^{^b}	V_max	K_m2	V_max2	K_si	n	CL_int2	CL_int^{^c} or CL_max^{^d}	Equation
	μM	pmol/min/mg	μM	pmol/min/mg	μM		μl/min/mg	μl/min/mg
UGT2B10
Amitriptyline	2.60 ± 0.48^{^a}	120 ± 7	N.A.	N.A.	353 ± 137	N.A.	N.A.	46.2^{^c}	Eq. 4
Imipramine	16.8 ± 1.3^{^a}	59.6 ± 1.3	N.A.	N.A.	N.A.	N.A.	N.A.	3.5^{^c}	Eq. 1
Clomipramine	14.4 ± 0.8^{^a}	150 ± 2	N.A.	N.A.	N.A.	N.A.	N.A.	10.4^{^c}	Eq. 1
Trimipramine	11.2 ± 0.9^{^a}	9.90 ± 0.19	N.A.	N.A.	N.A.	N.A.	N.A.	0.9^{^c}	Eq. 1
UGT1A4
Amitriptyline	448 ± 27^{^a}	1890 ± 70	N.A.	N.A.	N.A.	N.A.	N.A.	4.2^{^c}	Eq. 1
Imipramine	262 ± 46^{^b}	700 ± 78	N.A.	N.A.	N.A.	1.5 ± 0.1	N.A.	1.4^{^d}	Eq. 3
Clomipramine	112 ± 8^{^b}	1430 ± 60	N.A.	N.A.	N.A.	1.8 ± 0.2	N.A.	6.4^{^d}	Eq. 3
Trimipramine	258 ± 26^{^a}	313 ± 15	N.A.	N.A.	N.A.	N.A.	N.A.	1.2^{^c}	Eq. 1
Pooled HLM
Amitriptyline	1.75 ± 1.45^{^a}	85.6 ± 21.7	343 ± 65	1210 ± 80	N.A.	N.A.	N.A.	52.4^{^c}	Eq. 2
Imipramine	9.92 ± 7.49^{^a}	55.7 ± 15.8	N.A.	N.A.	N.A.	N.A.	0.98 ± 0.03	6.6^{^c}	Eq. 5
Clomipramine	108 ± 6^{^b}	1750 ± 50	N.A.	N.A.	N.A.	1.9 ± 0.1	N.A.	8.1^{^d}	Eq. 3
Trimipramine	277 ± 46^{^b}	319 ± 28	N.A.	N.A.	N.A.	1.2 ± 0.1	N.A.	0.7^{^d}	Eq. 3

N.A., not applicable.
↵a K_m fitting from Michaelis-Menten equation, substrate inhibition equation or biphasic equation.
↵b S₅₀ fitting from the Hill equation.
↵c CL_int calculated as V_max/K_m.
↵d CL_max calculated according to eq. 6.