Table 1

Metabolism profiles of EMD68842, EMD96785, and EMD128130 in the dog and monkey in vivo, in CPHs, and in microsomes

	Metabolite	In Vivo	CPHs	Microsomes
EMD68843
Dog	Amine-H₂O	8^1-a	71 ± 9	0^1-b
	OH-1	38^1-a	4 ± 2	50^1-b
	OH-2	8^1-a	11 ± 6	50^1-b
	N-dealk	1^1-a	7 ± 0	0^1-b
	Gluc-OH-1	38^1-a	7 ± 6	0^1-b
	Gluc-OH-2	8^1-a	0 ± 0	0^1-b
Monkey	Amine-H₂O	6^1-a	80 ± 7	0^1-b
	OH-1	33^1-a	9 ± 3	42^1-b
	OH-2	3^1-a	4 ± 6	42^1-b
	N-dealk	22^1-a	0 ± 0	17^1-b
	Gluc-OH-1	33^1-a	7 ± 4	0^1-b
	Gluc-OH-2	3^1-a	0 ± 0	0^1-b
EMD96785
Dog	Aromatic amine	77^1-c	67 ± 17	57^1-b
	Acid	8^1-c	26 ± 16	43^1-b
	Acid oxide	15^1-c	7 ± 7	0^1-b
Monkey	Aromatic amine	88^1-c	97 ± 11	100^1-b
	Acid	12^1-c	3 ± 1	0^1-b
	Acid oxide	0^1-c	0	0^1-b
EMD128130
Dog	OH-1	18^1-d	39 ± 5	45^1-e
	OH-2	12^1-d	12 ± 7	23^1-e
	N-dealk	36^1-d	0.1 ± 0.1	32^1-e
	Gluc-OH-1	18^1-d	12 ± 8	0^1-e
	Gluc-OH-2	12^1-d	28 ± 12	0^1-e
	Gluc-N-dealk	0^1-d	0 ± 0	0^1-e
	Gly-N-dealk	0^1-d	0 ± 0	0^1-e
	Sulf-OH-1	5^1-d	9 ± 2	0^1-e
Monkey	OH-1	12^1-d	20 ± 12	55^1-e
	OH-2	18^1-d	9 ± 3	16^1-e
	N-dealk	36^1-d	0 ± 0	29^1-e
	Gluc-OH-1	12^1-d	17 ± 3	0^1-e
	Gluc-OH-2	18^1-d	36 ± 4	0^1-e
	Gluc-N-dealk	0^1-d	0	0^1-e
	Gly-N-dealk	0^1-d	0	0^1-e
	Sulf-OH-1	<5^1-d	19 ± 6	0^1-e

Values are expressed as the percentage of the total metabolites formed (mean, n = 3 for each system and species; S.D. values shown only for CPHs, all of which were measured after a 4-h incubation).

↵1-a After a 24-h incubation.
↵1-b After a 2-h incubation.
↵1-c After a 4-h incubation.
↵1-d After a 120-h incubation.
↵1-e After a 0.5-h incubation.