Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTM5Q4V)

• DTT Name: Organic cation transporter 1
• Synonyms: Solute carrier family 22 member 1; hOCT1; SLC22A1
• Gene Name: SLC22A1
• BioChemical Class: Single Protein
• UniProt ID: S22A1_HUMAN
• TTD ID: TE0106
• Sequence:
  MPTVDDILEQVGESGWFQKQAFLILCLLSAAFAPICVGIVFLGFTPDHHCQSPGVAELSQ
  RCGWSPAEELNYTVPGLGPAGEAFLGQCRRYEVDWNQSALSCVDPLASLATNRSHLPLGP
  CQDGWVYDTPGSSIVTEFNLVCADSWKLDLFQSCLNAGFLFGSLGVGYFADRFGRKLCLL
  GTVLVNAVSGVLMAFSPNYMSMLLFRLLQGLVSKGNWMAGYTLITEFVGSGSRRTVAIMY
  QMAFTVGLVALTGLAYALPHWRWLQLAVSLPTFLFLLYYWCVPESPRWLLSQKRNTEAIK
  IMDHIAQKNGKLPPADLKMLSLEEDVTEKLSPSFADLFRTPRLRKRTFILMYLWFTDSVL
  YQGLILHMGATSGNLYLDFLYSALVEIPGAFIALITIDRVGRIYPMAMSNLLAGAACLVM
  IFISPDLHWLNIIIMCVGRMGITIAIQMICLVNAELYPTFVRNLGVMVCSSLCDIGGIIT
  PFIVFRLREVWQALPLILFAVLGLLAAGVTLLLPETKGVALPETMKDAENLGRKAKPKEN
  TIYLKVQTSEPSGT
• Function: 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 Drug Transporter (DTP) Role of This DTT

• DTT DTP Name: Organic cation transporter 1 (SLC22A1) DTP Info
• Gene Name: SLC22A1

65 Approved Drug(s) Transported by This DTT

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	Virus infection	1A24-1D9Z	Approved	[3]
Amiloride	DMRTSGP	Congestive heart failure	BD10	Approved	[4]
Atenolol	DMNKG1Z	Hypertension	BA00-BA04	Approved	[4]
Atropine	DMEN6X7	Organophosphate poisoning	NE6Z	Approved	[4]
Auranofin	DMWE2N4	Inflammatory arthritis	FA2Z	Approved	[5]
Buformin	DMX82DO	Type 2 diabetes	5A11	Approved	[6]
Cimetidine	DMH61ZB	Acid-reflux disorder	DA22	Approved	[4]
Cisplatin	DMRHGI9	Solid tumour/cancer	2A00-2F9Z	Approved	[7]
Citalopram	DM2G9AE	Depression	6A70-6A7Z	Approved	[8]
Cladribine	DM3JDRP	Hairy cell leukaemia	2A82.2	Approved	[6]
Clidinium	DMUMQZ0	Abdominal stomach pain	DD91.4	Approved	[4]
Clonidine	DM6RZ9Q	Hypertension	BA00-BA04	Approved	[9]
Codeine	DMJX6ZG	Pain	MG30-MG3Z	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	Ventricular arrhythmias	BC71	Approved	[4]
Dopamine	DMPGUCF	Parkinson disease	8A00.0	Approved	[8]
Epinephrine	DM3KJBC	Allergy	4A80-4A85	Approved	[6]
Fenoterol	DMIP3ZV	Asthma	CA23	Approved	[4]
Fexofenadine	DM17ONX	Allergic rhinitis	CA08.0	Approved	[13]
Formoterol	DMSOURV	Asthma	CA23	Approved	[4]
Ganciclovir	DM1MBYQ	Virus infection	1A24-1D9Z	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	Type-2 diabetes	5A11	Approved	[17]
Metoclopramide	DMFA5MY	Nausea	MD90	Approved	[4]
Naratriptan	DMO50U2	Migraine	8A80	Approved	[18]
Nizatidine	DMGFV3Z	Acid-reflux disorder	DA22	Approved	[4]
Norepinephrine	DMOUC09	Sepsis	1G40-1G41	Approved	[8]
Oxaliplatin	DMQNWRD	Colorectal cancer	2B91.Z	Approved	[19]
Oxyphenonium	DMMQHOZ	Visceral spasms	MD81.4	Approved	[4]
Pentamidine	DMHZJCG	Fungal infection	1F29-1F2F	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	Migraine	8A80	Approved	[9]
Quinine	DMSWYF5	Malaria	1F40-1F45	Approved	[22]
Ranitidine	DM0GUSX	Peptic ulcer	DA61	Approved	[23]
Rizatriptan	DMDJMA3	Migraine	8A80	Approved	[18]
Salbutamol	DMN9CWF	Acute asthma	CA23	Approved	[4]
Sitagliptin	DMGDKXN	Type-2 diabetes	5A11	Approved	[24]
Sorafenib	DMS8IFC	Hepatocellular carcinoma	2C12.02	Approved	[25]
Sumatriptan	DMVYXR8	Migraine	8A80	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	Urinary tract infection	GC08	Approved	[4]
Trospium chloride	DM32XZT	Discovery agent	N.A.	Approved	[26]
Tubocurarine	DMBZIVP	Anaesthesia	9A78.6	Approved	[6]
Varenicline	DMMUOLJ	Smoking dependence	6C4A.2	Approved	[4]
Verapamil	DMA7PEW	Hypertension	BA00-BA04	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]

5 Clinical Trial Drug(s) Transported by This DTT

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]

1 Discontinued Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Phenformin	DMQ52JG	Diabetic complication	5A2Y	Withdrawn from market	[4]

3 Preclinical Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(R)-Xamoterol	DMXWD08	Heart failure	BD10-BD13	Preclinical	[4]
(S)-Xamoterol	DM1ZQ5G	Heart failure	BD10-BD13	Preclinical	[4]
N-methylpyridinium	DMVUKEW	Colon cancer	2B90.Z	Preclinical	[31]

6 Investigative Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Benzamil	DM57SVW	Discovery agent	N.A.	Investigative	[4]
Choline	DM5D9YK	Discovery agent	N.A.	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]

References

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• [30] Human organic anion transporters and human organic cation transporters mediate renal transport of prostaglandins. J Pharmacol Exp Ther. 2002 Apr;301(1):293-8.
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• [34] Involvement of human organic cation transporter 1 in the hepatic uptake of 1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazolium bromide (YM155 monobromide), a novel, small molecule survivin suppressant. Drug Metab Dispos. 2009 Sep;37(9):1856-63.