Drug Metabolism in Drug Design and Development Basic Concepts and Practice

TEA, carnitine, quinidine,

verapamil

SLC22A5

OCTN2, CT1 Kidney, skeletal

muscle, prostate,lung, heart, pancreas,small intestine, liver

Small organic cations

TEA, cimetidine,

acetylcholine, choline,serotonine, quinidine,verapamil

Na

+

dependent: carnitine,

phaloridine

Na

+

independent: verapamil,

quinidine, TEA

SLC22A6

OAT1

Kidney, brain

Organic anions.Although cimetidine is an

organic cation, it is asubstrate that is recognizedby both organic cation andanion transporters. PAH,methotrexate, estrone sulfate,prostaglandin, DHEAS

SLC22A7

OAT2

Liver, kidney

SLC22A8

OAT3

Kidney, brain

SLC29A1

ENT1

Ubiquitous,

cancer cells

Nucleosides and

nucleoside analogues

Nitrobenzylthioinosine

and dipyridamolefor ENT1

Facilitated

transport

Adenosine, uridine,

inosine

SLC29A2

ENT2

Ubiquitous,

cancer cells

SLC28A1 CNT1

Liver, kidney,

intestine, brain

Purine nucleosides,

uridine

Na

+

free buffer

Na

+

dependent

(continued

)

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