Table 1.

Substrates and inhibitors of OATP1A2.

Category	Substrate	Inhibitor	Model	Ref.
Bile salts	Taurocholate	Ursodeoxycholate, tauroursodeoxycholate, aurochenodeoxycholate, ursodeoxycholate, indocyanine green, glycocholate, cholate, chenodeoxycholate	Oocyte	[9]
	Cholate, glycocholate, TCDCA, TUDCA		Oocyte	[5,9]
Hormones	DHEAS	Tauroursodeoxycholate, taurochenodeoxycholate, E-3-S, dexamethasone	Oocyte	[10]
	E217βG	Bilirubin	Oocyte	[5,23]
	Unconjugated bilirubin	E217βG	Oocyte	[23]
	E-3-S, T4, T3, rT3		Oocyte	[7,16,33]
Peptides	Deltorphin II	Naltrindole, naloxone, Leu-enkephalin, E-3-S, DPDPE	Oocyte	[11,16]
	BQ-123, CRC-220, DPDPE		Oocyte	[5,11,16]
Organic anions	BSP	Rifampin, rifamycin SV, oubain, tauroursodeoxycholate, ursodeoxycholate, taurocholate, taurochenodeoxycholate, indocyanine green, glycocholate, cholate, chenodeoxycholate	Oocyte	[9,22]
Organic cations	APD-ajmalinium, N-methylquinine, N-methylquinidine, rocuronium		Oocyte	[15]
Drugs	Fexofenadine	Grapefruit juice (naringin), orange juice (hesperidin), apple juice, verapamil, saquinavir, ritonavir, quinidine, PSC-833, nelfinavir, lovastatin, ketoconazole, indinavir, erythromycin	HeLa	[13,20,21]
	Ouabain	Taurochenodeoxycholate	Oocyte	[5,12]
	Imatinib	Uremic toxins (CMPF)	Oocyte	[19]
	Rocuronium	Taurocholate, quinidine, N-methylquinidine, K-strophantoside, Azidoprocainamide methiodide	Oocyte	[14,15]
	Chlorambuciltaurocholate, Gd-B 20790, erythromycin, levofloxacin, pitavastatin, pravastatin, rosuvastatin, saquinavir, D-penicillamine, bamet-UD2, bamet-R2, bromosulfophthalein, unprostone, methotrexate		Oocyte	[17,33]
Toxins	Microcystin		Oocyte	[6]
Eicosanoids	Prostaglandin E2		Oocyte	[5]

BSP: Sulfobromophthalein; CMPF: 3-carboxy-4-methyl-5-propyl-2-furan-propanoic acid; CRC-220: 4-methoxy-2,3,6-trimethylphenylsulfonyl-L-aspartyl-D-4-amidino-phenylalanyl-piperidide; DPDPE: (D-Pen2,D-Pen5)-enkephalin; TCDCA: Taurochenodeoxycholate; TUDCA: Tauroursodeoxycholic acid.