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SLC22A4

Synonyms: MGC34546, MGC40524, OCTN1

Entrez Gene Link

Expression Data
Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

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    0.00217
Kidney* Nishimura    0.0274
Liver Nishimura    0.000202
Placenta Nishimura    0.00582
Small Intestine* Nishimura    0.00694
Kidney* Mean across all PMT Samples 1.621
Liver Mean across all PMT Samples    0.159
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
Acetylcholine 1000 hOCTN1 reconstituted proteoliposome Pochini, 2012
Amisulpride 180 HEK293-hOCTN1 Dos, 2014
Cytarabine 1.95 HEK293-hOCTN1 Drenberg, 2017
Ergothioneine 21 HEK-OCTN1 Grundemann, 2005
Ergothioneine 38.4 HEK293-hOCTN1 Futatsugi, 2016
Ethambutol 336.8 HEK293-hOCTN1 Parvez, 2018
Gabapentin 417 HEK293-hOCTN1 Futatsugi, 2016
Ipratropium 444 HEK293-OCTN1 Nakamura, 2010
L-carnitine 571 HEK293-hOCTN1 Peltekova, 2004
Quinidine ND OCTN1-expressing oocytes Yabuuchi, 1999
Sulpiride 250 MDCK-hOCTN1 Li, 2017
Tetraethylammonium 195 OCTN1-expressing oocytes Yabuuchi, 1999
Tetraethylammonium 1800 HEK293-OCTN1 Urban, 2007
Tetraethylammonium 770 hOCTN1 reconstituted proteoliposome Pochini, 2011
Verapamil ND OCTN1-expressing oocytes Yabuuchi, 1999

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
Acetylcholine 440 Tetraethylammonium hOCTN1-reconstituted proteoliposomes Pochini, 2011
Carnitine 24.08 Tetraethylammonium HEK293-hOCTN1 Peltekova, 2004
Carvedilol 73.1 Tetraethylammonium MDCKII-hOCTN1 Grube, 2011
Choline 230.5 Tetraethylammonium HEK293-hOCTN1 Peltekova, 2004
Cimetidine 1500 Tetraethylammonium HRPE-rOCTN1 Wu, 2000
Cimetidine 434.8 Tetraethylammonium HEK293-hOCTN1 Peltekova, 2004
Cobicistat 2.49 Tetraethylammonium S2-hOCTN1 DARUNAVIR/COBICISTAT PHARMACOKINETICS WRITTEN SUMMARY
Desipramine 80 Tetraethylammonium HRPE-rOCTN1 Wu, 2000
Diltiazem 126.4 Tetraethylammonium MDCKII-hOCTN1 Grube, 2011
Dipyridamole 0.0077 Cytarabine HEK293-hOCTN1 Drenberg, 2017
Disprocynium24 14.6 Ergothioneine HEK293-OCTN1 Grigat, 2007
Doxorubicin 0.00931 Tetraethylammonium KB-3-3-hOCTN1 Okabe, 2008
Flecainide 176 Tetraethylammonium MDCKII-hOCTN1 Grube, 2011
Gamma-butyrobetaine 630 Tetraethylammonium hOCTN1-reconstituted proteoliposomes Pochini, 2011
Hercynine 1450 Ergothioneine HEK293-OCTN1 Grigat, 2007
Imatinib 31 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-hOCTN1 Schmidt-Lauber, 2012
L-ergothioneine 9 Tetraethylammonium HEK293-OCTN1 Urban, 2007
Lidocaine 0.83 Tetraethylammonium HEK293-hOCTN1 Peltekova, 2004
Linagliptin >100 Not stated HEK293-hOCTN1 Linagliptin NDA application
Methimazole 7520 Ergothioneine HEK293-OCTN1 Grigat, 2007
Mitoxantrone 0.00275 Tetraethylammonium KB-3-3-hOCTN1 Okabe, 2008
Nifedipine 74.6 Tetraethylammonium MDCKII-hOCTN1 Grube, 2011
Procainamide <1000 Tetraethylammonium HEK293-OCTN1 Yabuuchi, 1999
Procainamide 1000 Tetraethylammonium HRPE-rOCTN1 Wu, 2000
Propafenone 67.5 Tetraethylammonium MDCKII-hOCTN1 Grube, 2011
Pyrilamide 182 Ergothioneine HEK293-OCTN1 Grigat, 2007
Quinidine <1000 Tetraethylammonium HEK293-OCTN1 Yabuuchi, 1999
Quinidine 68.38 Tetraethylammonium HEK293-hOCTN1 Peltekova, 2004
Quinine <1000 Tetraethylammonium HEK293-OCTN1 Yabuuchi, 1999
Spironolactone 125 Tetraethylammonium MDCKII-hOCTN1 Grube, 2011
Tetraethylammonium 439 Tetraethylammonium HEK293-hOCTN1 Peltekova, 2004
Thioperamide 254 Ergothioneine HEK293-OCTN1 Grigat, 2007
Verapamil 10.8 Ergothioneine HEK293-OCTN1 Grigat, 2007
Verapamil 12 Ethambutol HEK293-hOCTN1 Parvez, 2018
Verapamil 8.38 Tetraethylammonium HEK293-hOCTN1 Peltekova, 2004
Verapamil 11 Tetraethylammonium MDCKII-hOCTN1 Grube, 2011

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

No drug-drug interaction information.


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