General Information of Drug Transporter (DTP) (ID: DTT79CX)

DTP Name Organic cation transporter 1 (SLC22A1)
Gene Name SLC22A1
UniProt ID
O15245 (S22A1_HUMAN)
VARIDT ID
DTD0010
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Synonyms OCT1; SLC22A1; Solute carrier family 22 member 1; hOCT1; oct1_cds
DTP Family Major Facilitator Superfamily (MFS)
Organic Cation Transporter (OCT) Family
Tissue Specificity primarily expressed on the sinusoidal (blood side) membrane of hepatocytes. OCT1 is also located on the basolateral membrane of small intestinal enterocytes, renal proximal tubular cells, and with much lower abundance in some neurons, the heart, skeletal muscle, lung, tumor cells, and basophilic granulocytes
Sequence
MPTVDDILEQVGESGWFQKQAFLILCLLSAAFAPICVGIVFLGFTPDHHCQSPGVAELSQ
RCGWSPAEELNYTVPGLGPAGEAFLGQCRRYEVDWNQSALSCVDPLASLATNRSHLPLGP
CQDGWVYDTPGSSIVTEFNLVCADSWKLDLFQSCLNAGFLFGSLGVGYFADRFGRKLCLL
GTVLVNAVSGVLMAFSPNYMSMLLFRLLQGLVSKGNWMAGYTLITEFVGSGSRRTVAIMY
QMAFTVGLVALTGLAYALPHWRWLQLAVSLPTFLFLLYYWCVPESPRWLLSQKRNTEAIK
IMDHIAQKNGKLPPADLKMLSLEEDVTEKLSPSFADLFRTPRLRKRTFILMYLWFTDSVL
YQGLILHMGATSGNLYLDFLYSALVEIPGAFIALITIDRVGRIYPMAMSNLLAGAACLVM
IFISPDLHWLNIIIMCVGRMGITIAIQMICLVNAELYPTFVRNLGVMVCSSLCDIGGIIT
PFIVFRLREVWQALPLILFAVLGLLAAGVTLLLPETKGVALPETMKDAENLGRKAKPKEN
TIYLKVQTSEPSGT
Function
This transporter translocates organic cations in an electrogenic and pH-independent manner. Translocates organic cations across the plasma membrane in both directions. Transports the polyamines spermine and spermidine. Transports pramipexole across the basolateral membrane of the proximal tubular epithelial cells. The choline transport is activated by MMTS. Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine, and metformin. The transport of organic cations is inhibited by a broad array of compounds like tetramethylammonium (TMA), cocaine, lidocaine, NMDA receptor antagonists, atropine, prazosin, cimetidine, TEA and NMN, guanidine, cimetidine, choline, procainamide, quinine, tetrabutylammonium, and tetrapentylammonium.
Endogenous Substrate(s) Primary polyamines
TCDB ID
2.A.1.19.29
Gene ID
6580
KEGG Pathway
Bile secretion (hsa04976 )
Choline metabolism in cancer (hsa05231 )
Reactome Pathway
Norepinephrine Neurotransmitter Release Cycle (R-HSA-181430 )
Abacavir transmembrane transport (R-HSA-2161517 )
Na+/Cl- dependent neurotransmitter transporters (R-HSA-442660 )
Organic cation transport (R-HSA-549127 )
Neurotransmitter clearance (R-HSA-112311 )

Molecular Interaction Atlas (MIA) of This DTP

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTP
65 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acebutolol DM0TI4U Hypertension BA00-BA04 Approved [1]
Acetylcholine DMDF79Z Cataract 9B10 Approved [2]
Aciclovir DMYLOVR Genital herpes 1A94 Approved [3]
Amiloride DMRTSGP Congestive heart failure BD10 Approved [4]
Atenolol DMNKG1Z Angina pectoris BA40 Approved [4]
Atropine DMEN6X7 Organophosphate poisoning NE6Z Approved [4]
Auranofin DMWE2N4 Inflammatory arthritis FA2Z Approved [5]
Buformin DMX82DO N. A. N. A. Approved [6]
Cimetidine DMH61ZB Acid-reflux disorder DA22 Approved [4]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [7]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [8]
Cladribine DM3JDRP Hairy cell leukaemia 2A82.2 Approved [6]
Clidinium DMUMQZ0 Abdominal stomach pain DD91.4 Approved [4]
Clonidine DM6RZ9Q Attention deficit hyperactivity disorder 6A05.Z Approved [9]
Codeine DMJX6ZG Allergic rhinitis CA08.0 Approved [10]
Cytarabine DMZD5QR Acute lymphoblastic leukaemia 2A85 Approved [6]
Debrisoquin DMC50ME Hypertension BA00-BA04 Approved [11]
Desipramine DMT2FDC Attention deficit hyperactivity disorder 6A05.Z Approved [1]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [12]
Disopyramide DM5SYZP Long QT syndrome BC65.0 Approved [4]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [8]
Epinephrine DM3KJBC Acute asthma CA23 Approved [6]
Fenoterol DMIP3ZV Asthma CA23 Approved [4]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [13]
Formoterol DMSOURV Allergic asthma CA23.0 Approved [4]
Ganciclovir DM1MBYQ Cytomegalovirus infection 1D82 Approved [3]
Glycopyrrolate DM2M3ZA Anaesthesia 9A78.6 Approved [4]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [14]
Indacaterol DMQJHR7 Chronic obstructive pulmonary disease CA22 Approved [4]
Ipratropium DMFQ320 Obstructive lung disease CA22.Z Approved [4]
Lamivudine DMI347A Chronic HBV infection 1E51.0Z Approved [15]
Lamotrigine DM8SXYG Bipolar disorder 6A60 Approved [16]
Metformin DM89QE1 Colorectal carcinoma Approved [17]
Metoclopramide DMFA5MY Nausea MD90 Approved [4]
Naratriptan DMO50U2 Headache 8A80-8A84 Approved [18]
Nizatidine DMGFV3Z Acid-reflux disorder DA22 Approved [4]
Norepinephrine DMOUC09 Alopecia ED70 Approved [8]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [19]
Oxyphenonium DMMQHOZ Visceral spasms MD81.4 Approved [4]
Pentamidine DMHZJCG African trypanosomiasis 1F51 Approved [20]
Perphenazine DMA4MRX Schizophrenia 6A20 Approved [4]
Phenoxybenzamine DM8KSQH Malignant essential hypertension BA00 Approved [1]
Pramipexole DMNMW9R Parkinson disease 8A00.0 Approved [21]
Prazosin DMCD9YG Benign prostatic hyperplasia GA90 Approved [1]
Procainamide DMNMXR8 Ventricular arrhythmias BC71 Approved [4]
Procaterol DM1M0Q4 Asthma CA23 Approved [4]
Propranolol DM79NTF Angina pectoris BA40 Approved [9]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [22]
Ranitidine DM0GUSX Gastric ulcer DA60 Approved [23]
Rizatriptan DMDJMA3 Migraine 8A80 Approved [18]
Salbutamol DMN9CWF Acute asthma CA23 Approved [4]
Sitagliptin DMGDKXN Cystic fibrosis CA25 Approved [24]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [25]
Sumatriptan DMVYXR8 Cluster headache 8A81.0 Approved [4]
Terbutaline DMD4381 Asthma CA23 Approved [4]
Tiotropium DMFDC0Q Chronic obstructive pulmonary disease CA22 Approved [4]
Triamterene DM2HU9I Congestive heart failure BD10 Approved [4]
Trimethoprim DMM7CHK Acute otitis media AB00 Approved [4]
Trospium chloride DM32XZT Discovery agent N.A. Approved [26]
Tubocurarine DMBZIVP Anaesthesia 9A78.6 Approved [6]
Varenicline DMMUOLJ Drug dependence Approved [4]
Verapamil DMA7PEW Angina pectoris BA40 Approved [1]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [6]
Zolmitriptan DM1IB4Q Migraine 8A80 Approved [18]
Berberine DMC5Q8X N. A. N. A. Phase 4 [27]
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⏷ Show the Full List of 65 Approved Drug(s)
5 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Spermidine DMVJNFI Plaque psoriasis EA90.0 Phase 3 [6]
N1-methylnicotinamide DM16PWF Hyperlipidemia 5C80.Z Phase 2/3 [28]
Camostat DMQ7UL8 Cystic fibrosis CA25 Phase 2 [4]
YM155 DM5Q1W4 Breast cancer 2C60-2C65 Phase 2 [29]
PGF2alpha DM4XAU7 Solid tumour/cancer 2A00-2F9Z Clinical trial [30]
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1 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Phenformin DMQ52JG Diabetic complication 5A2Y Withdrawn from market [4]
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3 Preclinical Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(R)-Xamoterol DMXWD08 N. A. N. A. Preclinical [4]
(S)-Xamoterol DM1ZQ5G N. A. N. A. Preclinical [4]
N-methylpyridinium DMVUKEW N. A. N. A. Preclinical [31]
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6 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
benzamil DM57SVW Discovery agent N.A. Investigative [4]
CHOLINE DM5D9YK Insomnia 7A00-7A0Z Investigative [6]
PHENCYCLIDINE DMQBEYX Discovery agent N.A. Investigative [32]
Tetramethylammonium Ion DMLEPYN Discovery agent N.A. Investigative [33]
tyramine DM4UXT1 Discovery agent N.A. Investigative [6]
[14C]TEA DM6SFYH Discovery agent N.A. Investigative [34]
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⏷ Show the Full List of 6 Investigative Drug(s)

Molecular Expression Atlas (MEA) of This DTP

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTP
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Acute myelocytic leukaemia 2B33.1 Bone marrow 6.07E-01 -1.05E-02 -3.21E-02
Adrenocortical carcinoma 2D11.Z Kidney 4.74E-01 -3.60E-02 -8.84E-02
Alopecia ED70 Skin from scalp 1.81E-03 2.26E-01 6.62E-01
Alzheimer's disease 8A20 Entorhinal cortex 8.54E-01 1.24E-02 7.20E-02
Ankylosing spondylitis FA92.0 Pheripheral blood 7.31E-01 9.11E-02 6.05E-01
Aortic stenosis BB70 Calcified aortic valve 8.60E-01 -9.43E-03 -1.21E-01
Apnea 7A40 Hyperplastic tonsil 4.92E-01 -7.19E-02 -3.60E-01
Arthropathy FA00-FA5Z Peripheral blood 1.97E-01 1.18E-01 4.54E-01
Asthma CA23 Nasal and bronchial airway 8.27E-06 1.93E-01 5.03E-01
Atopic dermatitis EA80 Skin 2.73E-02 -7.37E-02 -5.37E-01
Autism 6A02 Whole blood 1.16E-01 -2.19E-01 -7.09E-01
Autoimmune uveitis 9A96 Peripheral monocyte 4.09E-01 -6.22E-02 -2.84E-01
Autosomal dominant monocytopenia 4B04 Whole blood 4.78E-02 -5.96E-01 -7.95E-01
Bacterial infection of gingival 1C1H Gingival tissue 3.31E-03 1.18E-01 3.97E-01
Batten disease 5C56.1 Whole blood 7.94E-01 8.96E-02 7.70E-01
Behcet's disease 4A62 Peripheral blood 2.41E-01 5.20E-02 2.61E-01
Bipolar disorder 6A60-6A6Z Prefrontal cortex 8.60E-01 1.43E-02 7.01E-02
Bladder cancer 2C94 Bladder tissue 7.62E-03 3.49E-01 1.27E+00
Breast cancer 2C60-2C6Z Breast tissue 4.65E-16 -2.30E-01 -5.01E-01
Cardioembolic stroke 8B11.20 Whole blood 1.15E-06 9.53E-01 1.47E+00
Cervical cancer 2C77 Cervical tissue 2.83E-01 1.86E-01 4.27E-01
Childhood onset rheumatic disease FA20.Z Peripheral blood 6.09E-01 1.07E-02 9.02E-03
Chronic hepatitis C 1E51.1 Whole blood 1.97E-01 1.91E-01 1.25E+00
Chronic obstructive pulmonary disease CA22 Lung tissue 1.48E-01 6.33E-02 3.20E-01
Chronic obstructive pulmonary disease CA22 Small airway epithelium 1.74E-02 1.21E-01 4.40E-01
Chronic rhinosinusitis CA0A Sinus mucosa tissue 8.21E-01 -3.04E-02 -1.62E-01
Colon cancer 2B90 Colon tissue 2.93E-01 -1.27E-02 -3.91E-02
Coronary artery disease BA80-BA8Z Peripheral blood 5.81E-01 -8.57E-02 -2.65E-01
Diffuse large B-cell lymphoma 2A81 Tonsil tissue 9.11E-02 4.66E-01 1.39E+00
Endometriosis GA10 Endometrium tissue 4.21E-02 1.27E-01 3.83E-01
Familial hypercholesterolemia 5C80.00 Peripheral blood 5.54E-01 9.80E-02 5.18E-01
Familial hypercholesterolemia 5C80.00 Whole blood 3.14E-01 -3.85E-01 -9.43E-01
Gastric cancer 2B72 Gastric tissue 1.05E-01 -2.44E-01 -2.34E+00
Glioblastopma 2A00.00 Nervous tissue 6.12E-03 -2.40E-02 -7.73E-02
Glioma 2A00.0Y-2A00.0Z White matter tissue 8.25E-03 5.15E-01 9.18E-01
Head and neck cancer 2D42 Head and neck tissue 1.94E-08 1.59E-01 6.93E-01
HIV-associated neurocognitive impairment 8A2Y-8A2Z White matter tissue 2.29E-01 -1.32E-01 -5.78E-01
Huntington's disease 8A01.10 Whole blood 4.75E-01 -1.27E-01 -6.47E-01
Idiopathic pulmonary fibrosis CB03.4 Lung tissue 8.20E-02 -1.02E-01 -6.53E-01
Immunodeficiency 4A00-4A20 Peripheral blood 9.17E-01 -5.75E-02 -3.49E-01
Influenza 1.00E+30 Whole blood 3.64E-01 -9.96E-01 -9.50E-01
Interstitial cystitis GC00.3 Bladder tissue 2.38E-01 8.90E-02 4.16E-01
Intracranial aneurysm 8B01.0 Intracranial artery 4.22E-01 6.35E-02 4.42E-01
Irritable bowel syndrome DD91.0 Rectal colon tissue 8.55E-01 2.42E-02 6.43E-02
Ischemic stroke 8B11 Peripheral blood 3.96E-02 1.10E-01 5.72E-01
Juvenile idiopathic arthritis FA24 Peripheral blood 9.26E-01 1.15E-01 1.54E-01
Lateral sclerosis 8B60.4 Cervical spinal cord 6.39E-01 0.00E+00 0.00E+00
Lateral sclerosis 8B60.4 Skin 5.78E-01 -6.72E-02 -2.12E-01
Liver cancer 2C12.0 Liver tissue 5.69E-68 -5.04E+00 -7.45E+00
Liver failure DB99.7-DB99.8 Liver tissue 6.88E-04 -5.00E+00 -1.03E+01
Lung cancer 2C25 Lung tissue 1.45E-02 -7.93E-02 -2.43E-01
Lupus erythematosus 4A40 Whole blood 1.00E-11 4.89E-01 7.74E-01
Major depressive disorder 6A70-6A7Z Whole blood 4.42E-01 3.66E-02 6.62E-02
Major depressive disorder 6A70-6A7Z Hippocampus 5.15E-01 1.61E-02 7.93E-02
Melanoma 2C30 Skin 2.73E-01 1.64E-01 2.55E-01
Multiple myeloma 2A83.1 Bone marrow 1.15E-01 -2.20E-01 -6.45E-01
Multiple myeloma 2A83.1 Peripheral blood 6.58E-01 -8.69E-02 -4.45E-01
Multiple sclerosis 8A40 Plasmacytoid dendritic cells 5.44E-01 1.29E-01 3.80E-01
Myelodysplastic syndrome 2A36-2A3Z Bone marrow 3.14E-02 -1.03E-01 -5.15E-01
Myelofibrosis 2A20.2 Whole blood 2.36E-01 3.30E-02 1.58E-01
Myocardial infarction BA41-BA50 Peripheral blood 7.45E-03 3.37E-01 5.37E-01
Myopathy 8C70.6 Muscle tissue 7.22E-02 -1.72E-01 -8.58E-01
Neonatal sepsis KA60 Whole blood 2.55E-02 1.39E-01 3.12E-01
Neuroectodermal tumour 2A00.11 Brain stem tissue 3.52E-02 -4.16E-01 -9.36E-01
Non-alcoholic fatty liver disease DB92 Liver tissue 5.28E-02 2.28E-01 5.08E-01
Obesity related type 2 diabetes 5A11 Omental adipose tissue 2.94E-02 1.28E-01 1.14E+00
Olive pollen allergy CA08.00 Peripheral blood 1.66E-01 -2.88E-01 -6.53E-01
Oral cancer 2B6E Oral tissue 7.90E-01 -2.08E-01 -6.14E-01
Osteoarthritis FA00-FA0Z Synovial tissue 6.53E-01 6.72E-03 1.95E-02
Osteoporosis FB83.1 Bone marrow 3.50E-01 -1.28E-01 -5.08E-01
Ovarian cancer 2C73 Ovarian tissue 4.36E-01 -2.57E-02 -6.60E-02
Pancreatic cancer 2C10 Pancreas 6.39E-01 -2.19E-01 -6.43E-01
Parkinson's disease 8A00.0 Substantia nigra tissue 6.27E-01 5.04E-02 1.96E-01
Pediatric respiratory syncytial virus infection CA40.11 Peripheral blood 6.29E-01 1.67E-02 7.87E-02
Pituitary cancer 2D12 Pituitary tissue 5.03E-02 2.57E-01 7.75E-01
Pituitary gonadotrope tumour 2D12 Pituitary tissue 5.81E-01 3.01E-04 8.11E-04
Polycystic ovary syndrome 5A80.1 Vastus lateralis muscle 6.51E-01 1.61E-01 7.32E-01
Polycythemia vera 2A20.4 Whole blood 3.16E-11 3.71E-01 1.34E+00
Pompe disease 5C51.3 Biceps muscle 2.19E-01 2.21E-01 1.18E+00
Preterm birth KA21.4Z Myometrium 2.02E-01 -1.24E-01 -6.39E-01
Prostate cancer 2C82 Prostate 9.56E-01 -1.44E-01 -3.03E-01
Psoriasis EA90 Skin 2.90E-01 -1.11E-01 -2.75E-01
Rectal cancer 2B92 Rectal colon tissue 6.71E-01 -1.26E-01 -3.59E-01
Renal cancer 2C90-2C91 Kidney 2.40E-01 -2.62E-01 -6.25E-01
Retinoblastoma 2D02.2 Uvea 7.90E-01 -3.37E-03 -2.26E-02
Rheumatoid arthritis FA20 Synovial tissue 2.37E-01 1.03E-01 2.87E-01
Rhinovirus infection CA42.1 Nasal epithelium tissue 7.61E-01 5.26E-04 3.70E-03
Schizophrenia 6A20 Prefrontal cortex 2.25E-02 7.43E-02 2.28E-01
Schizophrenia 6A20 Superior temporal cortex 2.05E-01 -3.00E-02 -2.99E-01
Scleroderma 4A42.Z Whole blood 2.54E-01 7.38E-02 3.02E-01
Seizure 8A60-8A6Z Whole blood 2.52E-01 -2.52E-01 -6.14E-01
Sensitive skin EK0Z Skin 9.02E-01 -4.77E-02 -3.68E-01
Sepsis with septic shock 1G41 Whole blood 1.21E-01 4.52E-02 9.15E-02
Shwachman-Diamond syndrome 3A70.0 Bone marrow 6.91E-02 1.62E-01 5.93E-01
Sickle cell disease 3A51.0-3A51.3 Peripheral blood 4.61E-01 2.07E-01 7.86E-01
Simpson golabi behmel syndrome LD2C Adipose tissue 7.72E-01 -1.23E-01 -7.41E-01
Sjogren's syndrome 4A43.2 Salivary gland tissue 1.46E-01 1.04E-01 7.22E-01
Skin cancer 2C30-2C3Z Skin 1.34E-01 -9.10E-02 -1.97E-01
Thrombocythemia 3B63 Whole blood 1.24E-04 2.41E-01 1.07E+00
Thrombocytopenia 3B64 Whole blood 5.90E-01 1.63E-01 5.36E-01
Thyroid cancer 2D10 Thyroid 9.50E-04 7.31E-02 2.95E-01
Tibial muscular dystrophy 8C75 Muscle tissue 1.42E-03 -2.68E-01 -1.56E+00
Tuberous sclerosis complex LD2D.2 Perituberal tissue 3.85E-01 -3.52E-02 -9.97E-02
Type 2 diabetes 5A11 Liver tissue 1.46E-01 2.34E-01 7.18E-01
Ureter cancer 2C92 Urothelium 7.23E-01 -1.33E-02 -8.12E-02
Uterine cancer 2C78 Endometrium tissue 1.05E-08 2.71E-01 7.86E-01
Vitiligo ED63.0 Skin 4.40E-01 -7.97E-02 -2.68E-01
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⏷ Show the Full List of Expression Under 107 Diseases

Drug Affinity of This DTP Assessed by Cell Line

Approved Drug(s)
Drug Name Highest Status Cell Line Affinity REF
Aciclovir Approved Proximal tubule (S2) cells-OCT1 Km = 151.2 microM [3]
Dinoprostone Approved Proximal tubule (S2) cells-OCT1 Km = 0.657 microM [30]
Ganciclovir Approved Proximal tubule (S2) cells-OCT1 Km = 516.2 microM [3]
Ipratropium Approved Human embryonic kidney cells (HEK293)-OCT1 Km = 9.0 microM [4]
Metformin Approved Chinese hamster ovary (CHO) cells-OCT1 Km = 2160.0 microM [35]
Metformin Approved Human embryonic kidney cells (HEK293)-OCT1 Km = 1060.0 microM [36]
Metformin Approved Human embryonic kidney cells (HEK293)-OCT1 Km = 1470.0 microM [17]
Metformin Approved Human embryonic kidney cells (HEK293)-OCT1 Km = 5450.0 microM [37]
Pentamidine Approved Chinese hamster ovary (CHO) cells-OCT1 Km = 36.4 microM [20]
Ranitidine Approved Oocytes-OCT1 Km = 70.0 microM [23]
Trospium chloride Approved Primary human bladder urothelium cells (HBU) Km = 106.0 microM [26]
⏷ Show the Full List of 11 Approved Drug(s)
Clinical Trial Drug(s)
Drug Name Highest Status Cell Line Affinity REF
YM155 Phase 2 Human embryonic kidney cells (HEK293)-OCT1 Km = 22.1 microM [29]
PGF2alpha Clinical trial Proximal tubule (S2) cells-OCT1 Km = 0.477 microM [30]
Investigative Drug(s)
Drug Name Highest Status Cell Line Affinity REF
[14C]TEA Investigative Human cervical cancer cell line (Hela)-OCT1 Km = 229.0 microM [38]
[14C]TEA Investigative Proximal tubule (S2) cells-OCT1 Km = 566.0 microM [34]

The Drug Therapeutic Target (DTT) Role of This DTP

DTP DTT Name Organic cation transporter 1 DTT Info

References

1 Implications of genetic polymorphisms in drug transporters for pharmacotherapy. Cancer Lett. 2006 Mar 8;234(1):4-33.
2 Role of acetylcholine and polyspecific cation transporters in serotonin-induced bronchoconstriction in the mouse. Respir Res. 2006 Apr 12;7:65.
3 Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. J Pharmacol Exp Ther. 2002 Mar;300(3):918-24.
4 Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2. J Med Chem. 2013 Sep 26;56(18):7232-42.
5 Selection and characterization of a human ovarian cancer cell line resistant to auranofin. Oncotarget. 2017 Oct 9;8(56):96062-96078.
6 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
7 Cisplatin and oxaliplatin, but not carboplatin and nedaplatin, are substrates for human organic cation transporters (SLC22A1-3 and multidrug and toxin extrusion family). J Pharmacol Exp Ther. 2006 Nov;319(2):879-86.
8 Organic cation transporters and their pharmacokinetic and pharmacodynamic consequences. Drug Metab Pharmacokinet. 2008;23(4):243-53.
9 Influx Transport of Cationic Drug at the Blood-Retinal Barrier: Impact on the Retinal Delivery of Neuroprotectants. Biol Pharm Bull. 2017;40(8):1139-1145.
10 Association of Organic Cation Transporter 1 With Intolerance to Metformin in Type 2 Diabetes: A GoDARTS Study. Diabetes. 2015 May;64(5):1786-93.
11 The prototypic pharmacogenetic drug debrisoquine is a substrate of the genetically polymorphic organic cation transporter OCT1. Biochem Pharmacol. 2012 May 15;83(10):1427-34.
12 Are organic cation transporters capable of transporting prostaglandins? Naunyn Schmiedebergs Arch Pharmacol. 2005 Aug;372(2):125-30.
13 Intestinal drug transporter expression and the impact of grapefruit juice in humans. Clin Pharmacol Ther. 2007 Mar;81(3):362-70.
14 Pharmacologic markers and predictors of responses to imatinib therapy in patients with chronic myeloid leukemia. Leuk Lymphoma. 2008 Apr;49(4):639-42.
15 Relevance of the organic cation transporters 1 and 2 for antiretroviral drug therapy in human immunodeficiency virus infection. Drug Metab Dispos. 2008 Aug;36(8):1616-23.
16 Lamotrigine is a substrate for OCT1 in brain endothelial cells. Biochem Pharmacol. 2012 Mar 15;83(6):805-14.
17 Metformin is a superior substrate for renal organic cation transporter OCT2 rather than hepatic OCT1. Drug Metab Pharmacokinet. 2005 Oct;20(5):379-86.
18 OCT1 mediates hepatic uptake of sumatriptan and loss-of-function OCT1 polymorphisms affect sumatriptan pharmacokinetics. Clin Pharmacol Ther. 2016 Jun;99(6):633-41.
19 Organic cation transporters are determinants of oxaliplatin cytotoxicity. Cancer Res. 2006 Sep 1;66(17):8847-57.
20 Transport of dicationic drugs pentamidine and furamidine by human organic cation transporters. Drug Metab Dispos. 2009 Feb;37(2):424-30.
21 OCT1 polymorphism is associated with response and survival time in anti-Parkinsonian drug users. Neurogenetics. 2011 Feb;12(1):79-82.
22 Comparison of type I and type II organic cation transport by organic cation transporters and organic anion-transporting polypeptides. J Pharmacol Exp Ther. 2001 Jul;298(1):110-5.
23 Differential substrate and inhibitory activities of ranitidine and famotidine toward human organic cation transporter 1 (hOCT1; SLC22A1), hOCT2 (SLC22A2), and hOCT3 (SLC22A3). J Pharmacol Exp Ther. 2005 Dec;315(3):1288-97.
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