Drug Metabolism in Drug Design and Development Basic Concepts and Practice

TABLE 3.3 (

Continued

)

Isoenzyme

Endogenous substrates

Reported

Km

Drug or xenobiotic

substrates

Inducers

Inhibitors

UGT1A6

Serotonin

, 3-hydroxy

methyl DOPA

Serotonin: 6

mM

(Krishnaswamy,2003)

Phenols:

acetaminophen,

2-amino-5-nitro-4-trifluoromethylphenol(flutamide metabolite),BHA, BHT, 7-hydroxycoumarin, 4-hydroxy-coumarin (low),dobutamine,4-ethylphenol,3-ethylphenol,4-fluorocatechol,2-hydroxybiphenyl,4-iodophenol,4-isopropylphenol (low),4-methylcatechol,4-methylphenol,methylsalicylate,4-methylumbelliferone,4-nitrophenol, 4-nitrocatechol,octylgallate, phenol,4-propylphenol (low),cis

-resveratrol, salicylate,

4-

tert

-butylphenol (low),

tetrachlorocatechol, vanillin

TCDD,

b-naphtoflavone,3-methylchloranthrene

a-Napthol,

4-t-butylphenol,4-methylum-belliferone,7-hydroxycoumarin

Amines:

4-aminobiphenyl,

1-naphthylamine>

2-naphthylamine,

N-OH-2-naphthylamine.

48