Drug Metabolism in Drug Design and Development Basic Concepts and Practice

Drugs:

acetaminophen,

beta blocking adrenergicagents (low activity) suchas atenolol, labetolol,metoprolol, pindolol,propranolol, naproxen(R

S

for rat 1A6),

salicylate, valproic acid.

Flavonoids:

chrysin,

7-hydroxy flavone,naringenin

UGT1A7

Estriol, 2-OH-estradiol,

4-OH-estrone

Benzo(

a)pyrene phenols

(7-OH

9-OH

>

-OH),

Benzo(a)pyrene-t-7,8-dihydrodiol(7

R-glucuronide,

low affinity),2-OH-biphenyl,4-methylumbelliferone,1- and 2-naphthol,4-nitrophenol,octylgallate, vanillin

TCDD

UGT1A8/9

2-Hydroxy estrone,

4-Hydroxy estrone,2-Hydroxy estradiol,4-Hydroxy estradiol, estrone,dihydrotestosterone,trans

-retinoic acid,

4-Hydroxy retinoic acid,hyocholic acid,hyodeoxycholic,testosterone,leukotriene B4,

Propofol:

300

mM

Alizarin, anthraflavic acid,

apigenin, Benzo(

a)pyrene-

t-7,

8-dihydrodiol (7

R- and

8 S

-glucuronides), emodin,

fisetin, flavoperidol,genistein, naringenin,quercetin, quinalizarin,4-methylumbelliferone,scopoletin, carvacrol,eugenol, 1-naphthol,p-nitrophenol, 4-aminobiphenyl,

3-Methyl

cloranthrene

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