Table 2.

PET radiotracers to study the activity of hepatic transporters.

PET radiotracer	Hepatic transporters	Species	Application	Ref
[11C]N-acetyl-cysteinyl-leukotriene E4	OATPs, MRP2	Rats, Monkeys	Probe validation	[74]
(15R)-[11C]TIC-Me	OATPs, MRP2	Rats, Humans	Probe validation	[57,63]
[11C]SC-62,807	OATP1B1/3, BCRP	Mice, Rats	Probe validation	[55,73]
[11C]Telmisartan	OATP1B3	Rats, Humans	Mechanistic assessment of hepatic clearance; DDI study with rifampicin; assessment of dose dependency of hepatic disposition	[56,64–66]
[11C]Cholylsarcosine	OATPs, NTCP, BSEP	Pigs, Humans	Probe validation and evaluation of altered hepatic transporter activity in liver disease	[87–90]
[11C]Dehydropravastatin	OATP1B1/3, MRP2	Rats, Humans	Probe validation	[67–69]
[11C]Rhodamine-123	OCT1, P-gp	Mice, Rats	Probe validation	[79]
[11C]Glyburide	OATPs	Mice, Baboons	Mechanistic assessment of hepatic clearance; DDI study with rifampicin and cyclosporine A	[70]
[11C]Metformin	OCT1, MATE1	Mice, Humans	Assessment of the effect of genetic polymorphisms or disease on liver distribution as pharmacological target tissue	[75–78,96]
[11C]Rosuvastatin	OATPs, NTCP, BCRP, P-gp, MRP2	Rats, Humans	Mechanistic assessment of hepatic clearance; DDI study with rifampicin and cyclosporine A; validation of IVIVE	[37,94]
[11C]Erlotinib	OATP2B1, BCRP, P-gp,	Mice, Rats, Humans	Mechanistic assessment of hepatic clearance; DDI study with rifampicin; assessment of dose dependency of hepatic disposition	[60,61,97,98]
[18F]Pitavastatin	OATP1B1/3, BCRP, MRP2	Rats	Mechanistic assessment of hepatic clearance; DDI study with rifampicin	[58,71]
[18F]PTV-F1	OATP1B1/3	Rats	Probe validation	[59,72]
3β-[18F]Fluorocholic acid	OATPs, NTCP, BSEP	Mice	Probe validation and evaluation of altered hepatic transporter activity in mouse models of liver disease	[92,93]
[11C]Sulpiride	OCT1	Mice, Humans	Mechanistic assessment of hepatic clearance; assessment of dose dependency of hepatic disposition	[80]
[11C]Tariquidar	P-gp, BCRP	Mice, Humans	Probe validation; assessment of dose dependency of hepatic disposition	[84]