TABLE 1

Incubation conditions for substrates and inhibitors in rat microsomal and hepatocyte studies

Substrate	Inhibitor	Substrate Concentration^a	Inhibitor Concentration^a	Incubation Time			Incubation Concentration
Substrate	Inhibitor	Substrate Concentration^a	Inhibitor Concentration^a					Microsomes	Hepatocytes	Microsomes	Hepatocytes
		μM			min			mg protein/ml	×10⁶ cells/ml
Tolbutamide	Miconazole	250-1000	0.01-100	15	20	0.5	0.5
	Fluconazole		0.01-200
	Ketoconazole		0.01-100
Dextromethorphan	Quinine	0.5-2,^b,^c 0.25-1^c,^d	0.001-100	10	5	0.1	0.25
	Fluoxetine	20-120,^b,^e 6-24^c,^e	0.001-500
	Fluvoxamine		0.001-1000
Midazolam	Fluconazole	5-30	0.1-100,^b 10-250^d	10	10	0.75	0.5
	Ketoconazole		0.01-20^b, 0.1-50^d
Phenytoin	Fluconazole	1-100	0.05-50,^b 1.67-25^d	10	15	0.5	0.5
	Ketoconazole		0.05-50,^b, 0.05-25^d

↵ a Unless indicated, concentration ranges are identical in both microsomal and hepatocyte incubations.
↵ b Concentration range in microsomes.
↵ c Substrate concentrations for the high-affinity, low-capacity site.
↵ d Concentration range in hepatocytes.
↵ e Substrate concentrations for the low-affinity, high-capacity site.