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SLC22A3

Synonyms: EMT, EMTH, OCT3

Entrez Gene Link

Expression Data
Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

Orthologs in other species

rat Slc22a3

Expression Data

Expression data for other tissues could be found in http://pharmacogenetics.ucsf.edu/gtex/index.html

Asterisk indicates important transporters in the organ as identified in the organ diagram.

Organ Source Relative Expression
Brain Nishimura    0.00578
Kidney* Nishimura    0.0499
Liver* Nishimura    0.124
Placenta* Nishimura    0.146
Small Intestine* Nishimura    0.0256
Kidney* Mean across all PMT Samples 2.184
Liver* Mean across all PMT Samples 6.392
Note that relative expression values should only be compared between entries of the same source.

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In Vitro Substrates

Substrate Km (μM) Cell System Reference
Epinephrine 240 HEK293-OCT3 Amphoux, 2006
Etilefrine 2800 CHO-OCT3 Muller, 2005
Histamine 180 HEK293-OCT3 Grundemann, 1999
Histamine 220 HEK293-OCT3 Amphoux, 2006
Metformin 2260 CHO-OCT3 Nies, 2009
N-methylpyridinium 47 HRPE-OCT3 Wu, 2000
Norepinephrine 2630 HEK293-OCT3 Amphoux, 2006

ND = not determined
1 denotes drugs that can potentially be used as in vitro substrates for studies of the transporter as defined by the FDA as of March 2022
2 denotes drugs that can potentially be used as in vitro inhibitors for studies of the transporter as defined by the FDA as of March 2022
3 denotes drugs that can potentially be used as clinical substrates for studies of the transporter as defined by the FDA as of March 2022
4 denotes drugs that can potentially be used as clinical inhibitors for studies of the transporter as defined by the FDA as of March 2022


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In Vitro Inhibitors

Inhibitor IC50 (μM) Ki (μM) Substrate used Cell System Reference
3,4-methylenedioxymetamphetamine (MDMA) 73.6 N-methylpyridinium HEK293-OCT3 Amphoux, 2006
Amantadine >1000 N-methylpyridinium HEK293-OCT3 Amphoux, 2006
Amiloride 14.5 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Chen, 2022
Amiloride 3 Metformin HEK293-OCT3 Chen, 2022
Atropine 466 N-methylpyridinium CHO-OCT3 Muller, 2005
Chlorhexidine 3.7 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Chen, 2022
Chlorhexidine 0.4 Metformin HEK293-OCT3 Chen, 2022
Clonidine 373 N-methylpyridinium HRPE-OCT3 Wu, 2000
Clonidine 110 N-methylpyridinium CHO-OCT3 Muller, 2005
Cocaine >1000 N-methylpyridinium HEK293-OCT3 Amphoux, 2006
D-amphetamine 460 N-methylpyridinium HEK293-OCT3 Amphoux, 2006
Desipramine 14 N-methylpyridinium HRPE-OCT3 Wu, 2000
Diphenhydramine 695 N-methylpyridinium CHO-OCT3 Muller, 2005
Etilefrine 4448 N-methylpyridinium CHO-OCT3 Muller, 2005
Famotidine 10.7 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Wittwer, 2013
Famotidine 6.7 N-methylpyridinium OCT3-expressing oocytes Bourdet, 2005
Furamidine 20.4 N-methylpyridinium CHO-OCT3 Ming, 2009
Guanabenz 3.2 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Chen, 2022
Guanabenz 1.1 Metformin HEK293-OCT3 Chen, 2022
Guanidine 6201 N-methylpyridinium HRPE-OCT3 Wu, 2000
Histamine 140 N-methylpyridinium HEK293-OCT3 Grundemann, 1999
Imatinib 25.5 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Wittwer, 2013
Imipramine 42 N-methylpyridinium HRPE-OCT3 Wu, 2000
Indinavir >500 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Wittwer, 2013
Irinotecan 74.6 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Wittwer, 2013
Ketamine 225.7 N-methylpyridinium HEK293-OCT3 Amphoux, 2006
Memantine 236 N-methylpyridinium HEK293-OCT3 Amphoux, 2006
Metformin 2332 N-methylpyridinium OCT3-expressing oocytes Bourdet, 2005
Metformin 904 N-methylpyridinium HEK293-OCT3 Umehara, 2007
Mitoxantrone 60.5 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Wittwer, 2013
MK-801 224 N-methylpyridinium HEK293-OCT3 Amphoux, 2006
Nifekalant 146 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Wittwer, 2013
Ondansetron 17.4 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Wittwer, 2013
Pantoprazole 137 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Wittwer, 2013
Papaverine 4.1 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Chen, 2022
Papaverine 1.2 Metformin HEK293-OCT3 Chen, 2022
Pentamidine 9.5 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Wittwer, 2013
Pentamidine 14.8 N-methylpyridinium CHO-OCT3 Ming, 2009
Phencyclidine 333 N-methylpyridinium HEK293-OCT3 Amphoux, 2006
Phenformin 134 N-methylpyridinium HEK293-OCT3 Umehara, 2007
Phenoxybenzamine 6.13 N-methylpyridinium HEK293-OCT2 Hayer-Zillgen, 2002
Prazosin 12.6 N-methylpyridinium HEK293-OCT2 Hayer-Zillgen, 2002
Procainamide 738 N-methylpyridinium HRPE-OCT3 Wu, 2000
Quinidine 18.3 N-methylpyridinium OCT3-expressing oocytes Bourdet, 2005
Quinidine 22.7 N-methylpyridinium CHO-OCT3 Ming, 2009
Quinine 37 N-methylpyridinium CHO-OCT3 Muller, 2005
Ranitidine 290 N-methylpyridinium OCT3-expressing oocytes Bourdet, 2005
Ranitidine 372 N-methylpyridinium CHO-OCT3 Muller, 2005
Ritonavir >300 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Wittwer, 2013
Telmisartan 12 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Chen, 2022
Telmisartan 3.9 Metformin HEK293-OCT3 Chen, 2022
Tetraethylammonium 1372 N-methylpyridinium HRPE-OCT3 Wu, 2000
Tetraethylammonium 1237 N-methylpyridinium OCT3-expressing oocytes Bourdet, 2005
Tetraethylammonium 1476.6 N-methylpyridinium CHO-OCT3 Ming, 2009
Trazodone 5.2 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Chen, 2022
Trazodone 2.5 Metformin HEK293-OCT3 Chen, 2022
YM-252124 (YM758 metabolite) 63.4 N-methylpyridinium HEK293-OCT3 Umehara, 2009
YM155 108 N-methylpyridinium HEK293-OCT3 Minematsu, 2010
YM758 15.9 N-methylpyridinium HEK293-OCT3 Umehara, 2009

ND = not determined
1 denotes drugs that can potentially be used as in vitro substrates for studies of the transporter as defined by the FDA as of March 2022
2 denotes drugs that can potentially be used as in vitro inhibitors for studies of the transporter as defined by the FDA as of March 2022
3 denotes drugs that can potentially be used as clinical substrates for studies of the transporter as defined by the FDA as of March 2022
4 denotes drugs that can potentially be used as clinical inhibitors for studies of the transporter as defined by the FDA as of March 2022


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Clinical Drug-Drug Interactions

DDI Implicated Transporter Interacting Drug Affected Drug AUC Cmax CLR CL/F t1/2 Effect on PD Reference More Details
Clinical PK Impact(fold change)
1 OCTs/MATEs Cetirizine Pilsicainide 1.4 NS ND ND ND ND Tsuruoka, 2006 DDI 1
2 OCTs/MATEs Cimetidine Cephalexin NS NS 0.8 0.8 NS ND van, 1986 DDI 2
3 OCTs/MATEs Cimetidine Dofetilide 1.5 1.3 0.7 0.7 1.3 yes Abel, 2000 DDI 3
4 OCTs/MATEs Cimetidine Metformin 1.5 1.7 0.7 ND ND ND Somogyi, 1987 DDI 4
5 OCTs/MATEs Cimetidine Pilsicainide 1.3 NS 0.7 0.7 1.2 ND Shiga, 2000 DDI 5
6 OCTs/MATEs Cimetidine Pindolol (S-enantiomer) 1.4 1.3 0.7 ND NS ND Somogyi, 1992 DDI 6
7 OCTs/MATEs Cimetidine Procainamide 1.4 NS 0.6 ND 1.3 ND Somogyi, 1983 DDI 7
8 OCTs/MATEs Cimetidine Ranitidine 1.3 NS 0.7 ND 1.3 ND van, 1986 DDI 8
9 OCTs/MATEs Cimetidine Varenicline 1.3 ND 0.8 0.8 ND ND Feng, 2008 DDI 9
10 OATs/OCTs Cotrimoxazole (trimethoprim/sulfamethoxazole) Apricitabine 1.7 1.3 0.6 0.6 1.4 ND Shiveley, 2008 DDI 10
11 OATs/OCTs Cotrimoxazole (trimethoprim/sulfamethoxazole) Zidovudine NS ND 0.4 NS NS ND Chatton, 1992 DDI 11
12 OCTs Trimethoprim Zidovudine NS ND 0.5 NS NS ND Chatton, 1992 DDI 12

The transporters are implicated by in vitro data and/or studies in humans with genetic polymorphisms of the transporter
DDI = Drug Drug Interaction
PK = pharmacokinetic
PD = pharmacodynamic
ND = not determined
NS = not significant
N/A = information not available
Calculation of Fold Change: fold change in the presence of the interacting drug = (value with interacting drug)/(value without interacting drug)
fold change > 1: increase in pharmacokinetic value
fold change < 1: decrease in pharmacokinetic value
1 denotes drugs that can potentially be used as in vitro substrates for studies of the transporter as defined by the FDA as of March 2022
2 denotes drugs that can potentially be used as in vitro inhibitors for studies of the transporter as defined by the FDA as of March 2022
3 denotes drugs that can potentially be used as clinical substrates for studies of the transporter as defined by the FDA as of March 2022
4 denotes drugs that can potentially be used as clinical inhibitors for studies of the transporter as defined by the FDA as of March 2022


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