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Showing drug card for Cimetidine (DB00501)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-06-23 18:08:06
Primary Accession Number DB00501
Secondary Accession Number
  • APRD00568
Name Cimetidine
Drug Type
  • Approved
  • Small Molecule
Description A histamine congener, it competitively inhibits histamine binding to histamine H2 receptors. Cimetidine has a range of pharmacological actions. It inhibits gastric acid secretion, as well as pepsin and gastrins output. It also blocks the activity of cytochrome P-450 which might explain proposals for use in neoadjuvant therapy. [PubChem]
Synonyms
  1. Cimetidine A/AB
  2. Cimetidine Hcl
Brand Names
  1. Acibilin
  2. Acinil
  3. Cimal
  4. Cimetag
  5. Cimetum
  6. Dyspamet
  7. Edalene
  8. Eureceptor
  9. Gastromet
  10. Peptol
  11. Tagamet
  12. Tagamet HB
  13. Tagamet HB 200
  14. Tametin
  15. Tratul
  16. Ulcedin
  17. Ulcedine
  18. Ulcerfen
  19. Ulcimet
  20. Ulcofalk
  21. Ulcomedina
  22. Ulcomet
  23. Ulhys
Brand Mixtures Not Available
Chemical IUPAC Name 3-cyano-2-methyl-1-[2-[(5-methyl-1H-imidazol-4-yl)methylsulfanyl]ethyl]guanidine
Chemical Formula C10H16N6S
Chemical Structure Structure
CAS Registry Number 51481-61-9
InChI Identifier InChI=1/C10H16N6S/c1-8-9(16-7-15-8)5-17-4-3-13-10(12-2)14-6-11/h7H,3-5H2,1-2H3,(H,15,16)(H2,12,13,14)/f/h13-15H/b12-10-
InChI Key AQIXAKUUQRKLND-BKVUICMLDM
KEGG Drug D00295 Link Image
KEGG Compound Not Available
PubChem Compound 2756 Link Image
PubChem Substance 180968 Link Image
ChEBI ID 30731 Link Image
PharmGKB ID PA449001 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 00749494 Link Image
RxList Link http://www.rxlist.com/cgi/generic/cimet.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Cimetidine Link Image
FDA Label
Material Safety Data Sheet (MSDS)
Synthesis Reference G. J. Durant et al.; U.S. Pat. 3,950,333 (1976)
Average Molecular Weight 252.3390
Monoisotopic Molecular Weight 252.1157
State Solid
Melting Point 142 oC
Experimental Water Solubility 0.5 g/100 mL Source: PhysProp
Predicted Water Solubility 8.16e-01 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 1 Source: PhysProp
Predicted LogP 0.44 Calculated using ALOGPS
Experimental LogS -1.35 [ADME Research, USCD]
Predicted LogS -2.49 Calculated using ALOGPS
Experimental Caco2 Permeability -5.89 [ADME Research, USCD]
pKa/Isoelectric Point 6.8
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID Not Available
Isomeric SMILES C\N=C(\NCCSCC1=C(C)NC=N1)NC#N
Canonical SMILES CN=C(NCCSCC1=C(C)NC=N1)NC#N
Drug Category
  • Adjuvants
  • Analgesics
  • Anti-Ulcer Agents
  • Enzyme Inhibitors
  • Histamine Antagonists
  • Histamine H2 Antagonists
ATC Codes
AHFS Codes
  • 56:28.12
Indication For the treatment and the management of acid-reflux disorders (GERD), peptic ulcer disease, heartburn, and acid indigestion.
Pharmacology Cimetidine is a histamine H2-receptor antagonist. It reduces basal and nocturnal gastric acid secretion and a reduction in gastric volume, acidity, and amount of gastric acid released in response to stimuli including food, caffeine, insulin, betazole, or pentagastrin. It is used to treat gastrointestinal disorders such as gastric or duodenal ulcer, gastroesophageal reflux disease, and pathological hypersecretory conditions. Cimetidine inhibits many of the isoenzymes of the hepatic CYP450 enzyme system. Other actions of Cimetidine include an increase in gastric bacterial flora such as nitrate-reducing organisms.
Mechanism of Action Cimetidine binds to an H2-receptor located on the basolateral membrane of the gastric parietal cell, blocking histamine effects. This competitive inhibition results in reduced gastric acid secretion and a reduction in gastric volume and acidity.
Absorption Rapid 60-70%
Toxicity Symptoms of overdose include nausea, vomiting, diarrhea, increased saliva production, difficulty breathing, and a fast heartbeat.
Protein Binding 15-20%
Biotransformation Hepatic
Half Life 2 hours
Dosage Forms
Form Route
Liquid Oral
Tablet Oral
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions
Drug Interaction
Acenocoumarol The anti-H2 increases the anticoagulant effect
Alfentanil Increases the effect of the narcotic
Alprazolam Increases the effect of the benzodiazepine
Aminophylline Increases the effect of theophylline
Amitriptyline Increases the effect of tricyclic agent
Amoxapine Increases the effect of tricyclic agent
Anisindione The ANTI-H2 increases the anticoagulant effect
Astemizole Increased risk of cardiotoxicity and arrhythmias
Atazanavir This gastric pH modifier decreases the levels/effects of atazanavir
Carbamazepine Increases the effect of carbamazepine
Carmustine Increases myelosuppression caused by carmustine
Chlordiazepoxide Increases the effect of the benzodiazepine
Clomipramine Increases the effect of tricyclic agent
Clonazepam Increases the effect of the benzodiazepine
Clorazepate Increases the effect of the benzodiazepine
Clozapine Increases the effect of clozapine
Codeine Increases the effect of the narcotic
Desipramine Increases the effect of tricyclic agent
Diazepam Increases the effect of the benzodiazepine
Dicumarol The anti-H2 increases the anticoagulant effect
Dihydroquinidine barbiturate Increases the effect of quinidine
Dofetilide Increases effect/toxicity of dofetilide
Donepezil Possible antagonism of action
Doxepin Increases the effect of tricyclic agent
Dyphylline Increases the effect of theophylline
Dyphylline Increases the effect of theophylline
Enoxacin The agent decreases the absorption of enoxacin
Epirubicin Cimetidine can increase epirubicin levels
Estazolam Increases the effect of the benzodiazepine
Ethotoin Increases the effect of hydantoin
Fentanyl Increases the effect of the narcotic
Flecainide Increases serum levels of flecainide
Fluorouracil Increases the effect of and toxicity of fluorouacil
Flurazepam Increases the effect of the benzodiazepine
Fosphenytoin Increases the effect of hydantoin
Galantamine Possible antagonism of action
Halazepam Increases the effect of the benzodiazepine
Heroin Cimetidine increases the effect of the narcotic
Hydrocodone Increases the effect of the narcotic
Hydromorphone Increases the effect of the narcotic
Imipramine Increases the effect of tricyclic agent
Itraconazole The anti-H2 decreases the absorption of the imidazole
Ketazolam Cimetidine increases the effect of the benzodiazepine
Ketoconazole The anti-H2 decreases the absorption of the imidazole
Labetalol Cimetidine increases the effect of the beta-blocker
Levorphanol Increases the effect of the narcotic
Lidocaine Increases the effect and toxicity of lidocaine
Meperidine Increases the effect of the narcotic
Mephenytoin Increases the effect of hydantoin
Metformin Increases the effect of metformin
Methadone Increases the effect of the narcotic
Metoprolol Increases the effect of the beta-blocker
Midazolam Increases the effect of the benzodiazepine
Moclobemide Increases the effect of moclobemide
Morphine Increases the effect of the narcotic
Nalbuphine Increases the effect of the narcotic
Nifedipine Increases the effect of the calcium channel blocker
Nimodipine Increases the effect of the calcium channel blocker
Nitrendipine Increases the effect of the calcium channel blocker
Nortriptyline Increases the effect of tricyclic agent
Oxtriphylline Increases the effect of theophylline
Oxycodone Increases the effect of the narcotic
Oxymorphone Increases the effect of the narcotic
Pentazocine Increases the effect of the narcotic
Phenytoin Increases the effect of hydantoin
Posaconazole Significant decrease of posaconazole levels
Pramipexole Increases the effect and toxicity of pramipexole
Prazepam Cimetidine increases the effect of the benzodiazepine
Procainamide The histamine H2-receptor antagonist increases the effect of procainamide
Propoxyphene Increases the effect of the narcotic
Propranolol Increases the effect of the beta-blocker
Protriptyline Increases the effect of tricyclic agent
Quazepam Cimetidine increases the effect of the benzodiazepine
Quinidine Increases the effect of quinidine
Quinidine barbiturate Increases the effect of quinidine
Rivastigmine Possible antagonism of action
Sildenafil Increases the effect and toxicity of sildenafil
Sufentanil Increases the effect of the narcotic
Tacrine Increases the effect and toxicity of tacrine
Terfenadine Increased risk of cardiotoxicity and arrhythmias
Theophylline Increases the effect of theophylline
Timolol Increases the effect of the beta-blocker
Tolazoline Anticipated loss of efficacy of tolazoline
Triazolam Increases the effect of the benzodiazepine
Trimipramine Increases the effect of tricyclic agent
Warfarin The anti-H2 increases the anticoagulant effect
Zaleplon Increases the effect and toxicity of zaleplon
Food Interactions
  • Avoid alcohol.
  • Best effect when taken with food.
  • Limit caffeine intake.
Pathways
Name SMPDB Link KEGG Link
Cimetidine Pathway SMP00232 Link Image
General References
  1. Michnovicz JJ, Galbraith RA: Cimetidine inhibits catechol estrogen metabolism in women. Metabolism. 1991 Feb;40(2):170-4. [PubMed Link Image]
  2. Drugs.com Link Image
  3. Wikipedia Link Image
  4. RxList Link Image
Organisms Affected
  • Humans and other mammals
Phase 1 Metabolizing Enzymes
  1. Cytochrome P450 11A1 (CYP11A1)
  2. Cytochrome P450 1A2 (CYP1A2)
  3. Cytochrome P450 2D6 (CYP2D6)
Targets
  1. Histamine H2 receptor
  2. Putative renal organic anion transporter 1
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cytochrome P450 11A1 (CYP11A1)
Enzyme 1 Gene Name CYP11A1
Enzyme 1 SwissProt ID P05108 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|P05108|C11A_HUMAN Cytochrome P450 11A1 
MLAKGLPPRSVLVKGYQTFLSAPREGLGRLRVPTGEGAGISTRSPRPFNEIPSPGDNGWL
NLYHFWRETGTHKVHLHHVQNFQKYGPIYREKLGNVESVYVIDPEDVALLFKSEGPNPER
FLIPPWVAYHQYYQRPIGVLLKKSAAWKKDRVALNQEVMAPEATKNFLPLLDAVSRDFVS
VLHRRIKKAGSGNYSGDISDDLFRFAFESITNVIFGERQGMLEEVVNPEAQRFIDAIYQM
FHTSVPMLNLPPDLFRLFRTKTWKDHVAAWDVIFSKADIYTQNFYWELRQKGSVHHDYRG
MLYRLLGDSKMSFEDIKANVTEMLAGGVDTTSMTLQWHLYEMARNLKVQDMLRAEVLAAR
HQAQGDMATMLQLVPLLKASIKETLRLHPISVTLQRYLVNDLVLRDYMIPAKTLVQVAIY
ALGREPTFFFDPENFDPTRWLSKDKNITYFRNLGFGWGVRQCLGRRIAELEMTIFLINML
ENFRVEIQHLSDVGTTFNLILMPEKPISFTFWPFNQEATQQ
Phase 1 Metabolizing Enzyme 2 [top]
Enzyme 2 Name Cytochrome P450 1A2 (CYP1A2)
Enzyme 2 Gene Name CYP1A2
Enzyme 2 SwissProt ID P05177 Link Image
Enzyme 2 SNPs SNPJam Report Link Image
Enzyme 2 Protein Sequence >P05177|CP1A2_HUMAN Cytochrome P450 1A2 - Homo sapiens (Human). 
MALSQSVPFSATELLLASAIFCLVFWVLKGLRPRVPKGLKSPPEPWGWPLLGHVLTLGKN
PHLALSRMSQRYGDVLQIRIGSTPVLVLSRLDTIRQALVRQGDDFKGRPDLYTSTLITDG
QSLTFSTDSGPVWAARRRLAQNALNTFSIASDPASSSSCYLEEHVSKEAKALISRLQELM
AGPGHFDPYNQVVVSVANVIGAMCFGQHFPESSDEMLSLVKNTHEFVETASSGNPLDFFP
ILRYLPNPALQRFKAFNQRFLWFLQKTVQEHYQDFDKNSVRDITGALFKHSKKGPRASGN
LIPQEKIVNLVNDIFGAGFDTVTTAISWSLMYLVTKPEIQRKIQKELDTVIGRERRPRLS
DRPQLPYLEAFILETFRHSSFLPFTIPHSTTRDTTLNGFYIPKKCCVFVNQWQVNHDPEL
WEDPSEFRPERFLTADGTAINKPLSEKMMLFGMGKRRCIGEVLAKWEIFLFLAILLQQLE
FSVPPGVKVDLTPIYGLTMKHARCEHVQARRFSIN
Phase 1 Metabolizing Enzyme 3 [top]
Enzyme 3 Name Cytochrome P450 2D6 (CYP2D6)
Enzyme 3 Gene Name CYP2D6
Enzyme 3 SwissProt ID P10635 Link Image
Enzyme 3 SNPs SNPJam Report Link Image
Enzyme 3 Protein Sequence >sp|P10635|CP2D6_HUMAN Cytochrome P450 2D6 (EC 1.14.14.1) 
MGLEALVPLAVIVAIFLLLVDLMHRRQRWAARYPPGPLPLPGLGNLLHVDFQNTPYCFDQ
LRRRFGDVFSLQLAWTPVVVLNGLAAVREALVTHGEDTADRPPVPITQILGFGPRSQGVF
LARYGPAWREQRRFSVSTLRNLGLGKKSLEQWVTEEAACLCAAFANHSGRPFRPNGLLDK
AVSNVIASLTCGRRFEYDDPRFLRLLDLAQEGLKEESGFLREVLNAVPVLLHIPALAGKV
LRFQKAFLTQLDELLTEHRMTWDPAQPPRDLTEAFLAEMEKAKGNPESSFNDENLRIVVA
DLFSAGMVTTSTTLAWGLLLMILHPDVQRRVQQEIDDVIGQVRRPEMGDQAHMPYTTAVI
HEVQRFGDIVPLGMTHMTSRDIEVQGFRIPKGTTLITNLSSVLKDEAVWEKPFRFHPEHF
LDAQGHFVKPEAFLPFSAGRRACLGEPLARMELFLFFTSLLQHFSFSVPTGQPRPSHHGV
FAFLVSPSPYELCAVPR
Drug Target 1 [top]
Target 1 ID 124
Target 1 Name Histamine H2 receptor
Target 1 Synonyms
  1. Gastric receptor I
  2. H2R
Target 1 Gene Name HRH2
Target 1 Protein Sequence >Histamine H2 receptor 
MAPNGTASSFCLDSTACKITITVVLAVLILITVAGNVVVCLAVGLNRRLRNLTNCFIVSL
AITDLLLGLLVLPFSAIYQLSCKWSFGKVFCNIYTSLDVMLCTASILNLFMISLDRYCAV
MDPLRYPVLVTPVRVAISLVLIWVISITLSFLSIHLGWNSRNETSKGNHTTSKCKVQVNE
VYGLVDGLVTFYLPLLIMCITYYRIFKVARDQAKRINHISSWKAATIREHKATVTLAAVM
GAFIICWFPYFTAFVYRGLRGDDAINEVLEAIVLWLGYANSALNPILYAALNRDFRTGYQ
QLFCCRLANRNSHKTSLRSNASQLSRTQSREPRQQEEKPLKLQVWSGTEVTAPQGATDR
Target 1 Number of Residues 364
Target 1 Molecular Weight 40099
Target 1 Theoretical pI 9.39
Target 1 GO Classification
Function
amine receptor activity
histamine receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 1 General Function Involved in rhodopsin-like receptor activity
Target 1 Specific Function The H2 subclass of histamine receptors mediates gastric acid secretion. Also appears to regulate gastrointestinal motility and intestinal secretion. Possible role in regulating cell growth and differentiation. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase and, through a separate G protein-dependent mechanism, the phosphoinositide/protein kinase (PKC) signaling pathway
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 23-44
  • 58-81
  • 93-114
  • 135-159
  • 181-204
  • 235-258
  • 268-289
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 184088 Link Image
Target 1 UniProtKB/Swiss-Prot ID P25021 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name HRH2_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >1080 bp 
ATGGCACCCAATGGCACAGCCTCTTCCTTTTGCCTGGACTCTACCGCATGCAAGATCACC
ATCACCGTGGTCCTTGCGGTCCTCATCCTCATCACCGTTGCTGGCAATGTGGTCGTCTGT
CTGGCCGTGGGCTTGAACCGCCGGCTCCGCAACCTGACCAATTGTTTCATCGTGTCCTTG
GCTATCACTGACCTGCTCCTCGGCCTCCTGGTGCTGCCCTTCTCTGCCATCTACCAGCTG
TCCTGCAAGTGGAGCTTTGGCAAGGTCTTCTGCAATATCTACACCAGCCTGGATGTGATG
CTCTGCACAGCCTCCATTCTTAACCTCTTCATGATCAGCCTCGACCGGTACTGCGCTGTC
ATGGACCCACTGCGGTACCCTGTGCTGGTCACCCCAGTTCGGGTCGCCATCTCTCTGGTC
TTAATTTGGGTCATCTCCATTACCCTGTCCTTTCTGTCTATCCACCTGGGGTGGAACAGC
AGGAACGAGACCAGCAAGGGCAATCATACCACCTCTAAGTGCAAAGTCCAGGTCAATGAA
GTGTACGGGCTGGTGGATGGGCTGGTCACCTTCTACCTCCCGCTACTGATCATGTGCATC
ACCTACTACCGCATCTTCAAGGTCGCCCGGGATCAGGCCAAGAGGATCAATCACATTAGC
TCCTGGAAGGCAGCCACCATCAGGGAGCACAAAGCCACAGTGACACTGGCCGCCGTCATG
GGGGCCTTCATCATCTGCTGGTTTCCCTACTTCACCGCGTTTGTGTACCGTGGGCTGAGA
GGGGATGATGCCATCAATGAGGTGTTAGAAGCCATCGTTCTGTGGCTGGGCTATGCCAAC
TCAGCCCTGAACCCCATCCTGTATGCTGCGCTGAACAGAGACTTCCGCACCGGGTACCAA
CAGCTCTTCTGCTGCAGGCTGGCCAACCGCAACTCCCACAAAACTTCTCTGAGGTCCAAC
GCCTCTCAGCTGTCCAGGACCCAAAGCCGAGAACCCAGGCAACAGGAAGAGAAACCCCTG
AAGCTCCAGGTGTGGAGTGGGACAGAAGTCACGGCCCCCCAGGGAGCCACAGACAGGTAA
Target 1 GenBank Gene ID
Target 1 GeneCard ID HRH2 Link Image
Target 1 GenAtlas ID HRH2 Link Image
Target 1 HGNC ID HGNC:5183 Link Image
Target 1 Chromosome Location 5
Target 1 Locus 5q35.2
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Murakami H, Sun-Wada GH, Matsumoto M, Nishi T, Wada Y, Futai M: Human histamine H2 receptor gene: multiple transcription initiation and tissue-specific expression. FEBS Lett. 1999 May 28;451(3):327-31. [PubMed Link Image]
  2. Gantz I, Munzert G, Tashiro T, Schaffer M, Wang L, DelValle J, Yamada T: Molecular cloning of the human histamine H2 receptor. Biochem Biophys Res Commun. 1991 Aug 15;178(3):1386-92. [PubMed Link Image]
  3. Nishi T, Koike T, Oka T, Maeda M, Futai M: Identification of the promoter region of the human histamine H2-receptor gene. Biochem Biophys Res Commun. 1995 May 16;210(2):616-23. [PubMed Link Image]
  4. Orange PR, Heath PR, Wright SR, Pearson RC: Allelic variations of the human histamine H2 receptor gene. Neuroreport. 1996 May 17;7(7):1293-6. [PubMed Link Image]
  5. Del Valle J, Gantz I: Novel insights into histamine H2 receptor biology. Am J Physiol. 1997 Nov;273(5 Pt 1):G987-96. [PubMed Link Image]
Target 1 Drug References
  1. Hernandez-Munoz R, Montiel-Ruiz C, Vazquez-Martinez O: Gastric mucosal cell proliferation in ethanol-induced chronic mucosal injury is related to oxidative stress and lipid peroxidation in rats. Lab Invest. 2000 Aug;80(8):1161-9. [PubMed Link Image]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
  3. Takahashi HK, Watanabe T, Yokoyama A, Iwagaki H, Yoshino T, Tanaka N, Nishibori M: Cimetidine induces interleukin-18 production through H2-agonist activity in monocytes. Mol Pharmacol. 2006 Aug;70(2):450-3. Epub 2006 May 24. [PubMed Link Image]
  4. Kuint J, Linder N, Reichman B: Hypoxemia associated with cimetidine therapy in a newborn infant. Am J Perinatol. 1996 Jul;13(5):301-3. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 1729
Target 2 Name Putative renal organic anion transporter 1
Target 2 Synonyms Not Available
Target 2 Gene Name hROAT1
Target 2 Protein Sequence >Putative renal organic anion transporter 1 
MAFNDLLQQVGGVGRFQQIQVTLVVLPLLLMASHNTLQNFTAAIPTHHCRPPADANLSKN
GGLEVWLPRDRQGQPESCLRFTSPQWGLPFLNGTEANGTGATEPCTDGWIYDNSTFPSTI
VTEWDLVCSHRALRQLAQSLYMVGVLLGAMVFGYLADRLGRRKVLILNYLQTAVSGTCAA
FAPNFPIYCAFRLLSGMALAGISLNCMTLNVEWMPIHTRACVGTLIGYVYSLGQFLLAGV
AYAVPHWRHLQLLVSAPFFAFFIYSWFFIESARWHSSSGRLDLTLRALQRVARINGKREE
GAKLSMEVLRASLQKELTMGKGQASAMELLRCPTLRHLFLCLSMLWFATSFAYYGLVMDL
QGFGVSIYLIQVIFGAVDLPAKLVGFLVINSLGRRPAQMAALLLAGICILLNGVIPQDQS
IVRTSLAVLGKGCLAASFNCIFLYTGELYPTMIRQTGMGMGSTMARVGSIVSPLVSMTAE
LYPSMPLFIYGAVPVAASAVTVLLPETLGQPLPDTVQDLESRKGKQTRQQQEHQKYMVPL
QASAQEKNGF
Target 2 Number of Residues 559
Target 2 Molecular Weight 60353
Target 2 Theoretical pI 8.78
Target 2 GO Classification
Function
ion transporter activity
transporter activity
Process
ion transport
physiological process
cellular physiological process
transport
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 2 General Function Carbohydrate transport and metabolism
Target 2 Specific Function Not Available
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • None
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 3831566 Link Image
Target 2 UniProtKB/Swiss-Prot ID O95742 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name O95742_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location Not Available
Target 2 Gene Sequence >1653 bp 
ATGGCCTTTAATGACCTCCTGCAGCAGGTGGGGGGTGTCGGCCGCTTCCAGCAGATCCAG
GTCACCCTGGTGGTCCTCCCCCTGCTCCTGATGGCTTCTCACAACACCCTGCAGAACTTC
ACTGCTGCCATCCCTACCCACCACTGCCGCCCGCCTGCCGATGCCAACCTCAGCAAGAAC
GGGGGGCTGGAGGTCTGGCTGCCCCGGGACAGGCAGGGGCAGCCTGAGTCCTGCCTCCGC
TTCACCTCCCCGCAGTGGGGACTGCCCTTTCTCAATGGCACAGAAGCCAATGGCACAGGG
GCCACAGAGCCCTGCACCGATGGCTGGATCTATGACAACAGCACCTTCCCGTCTACCATC
GTGACTGAGTGGGACCTTGTGTGCTCTCACAGGGCCCTACGCCAGCTGGCCCAGTCCTTG
TACATGGTGGGGGTGCTGCTCGGAGCCATGGTGTTCGGCTACCTTGCAGACAGGCTAGGC
CGCCGGAAGGTACTCATCTTGAACTACCTGCAGACAGCTGTGTCAGGGACCTGCGCAGCC
TTCGCACCCAACTTCCCCATCTACTGCGCCTTCCGGCTCCTCTCGGGCATGGCTCTGGCT
GGCATCTCCCTCAACTGCATGACACTGAATGTGGAGTGGATGCCCATTCACACACGGGCC
TGCGTGGGCACCTTGATTGGCTATGTCTACAGCCTGGGCCAGTTCCTCCTGGCTGGTGTG
GCCTACGCTGTGCCCCACTGGCGCCACCTGCAGCTACTGGTCTCTGCGCCTTTTTTTGCC
TTCTTCATCTACTCCTGGTTCTTCATTGAGTCGGCCCGCTGGCACTCCTCCTCCGGGAGG
CTGGACCTCACCCTGAGGGCCCTGCAGAGAGTCGCCCGGATCAATGGGAAGCGGGAAGAA
GGAGCCAAATTGAGTATGGAGGTACTCCGGGCCAGTCTGCAGAAGGAGCTGACCATGGGC
AAAGGCCAGGCATCGGCCATGGAGCTGCTGCGCTGCCCCACCCTCCGCCACCTCTTCCTC
TGCCTCTCCATGCTGTGGTTTGCCACTAGCTTTGCATACTATGGGCTGGTCATGGACCTG
CAGGGCTTTGGAGTCAGCATCTACCTAATCCAGGTGATCTTTGGTGCTGTGGACCTGCCT
GCCAAGCTTGTGGGCTTCCTTGTCATCAACTCCCTGGGTCGCCGGCCTGCCCAGATGGCT
GCACTGCTGCTGGCAGGCATCTGCATCCTGCTCAATGGGGTGATACCCCAGGACCAGTCC
ATTGTCCGAACCTCTCTTGCTGTGCTGGGGAAGGGTTGTCTGGCTGCCTCCTTCAACTGC
ATCTTCCTGTATACTGGGGAACTGTATCCCACAATGATCCGGCAGACAGGCATGGGAATG
GGCAGCACCATGGCCCGAGTGGGCAGCATCGTGAGCCCACTGGTGAGCATGACTGCCGAG
CTCTACCCCTCCATGCCTCTCTTCATCTACGGTGCTGTTCCTGTGGCCGCCAGCGCTGTC
ACTGTCCTCCTGCCAGAGACCCTGGGCCAGCCACTGCCAGACACGGTGCAGGACCTGGAG
AGCAGGAAAGGGAAACAGACGCGACAGCAACAAGAGCACCAGAAGTATATGGTCCCACTG
CAGGCCTCAGCACAAGAGAAGAATGGATTTTGA
Target 2 GenBank Gene ID
Target 2 GeneCard ID hROAT1 Link Image
Target 2 GenAtlas ID hROAT1 Link Image
Target 2 HGNC ID HGNC:10970 Link Image
Target 2 Chromosome Location Not Available
Target 2 Locus Not Available
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Reid G, Wolff NA, Dautzenberg FM, Burckhardt G: Cloning of a human renal p-aminohippurate transporter, hROAT1. Kidney Blood Press Res. 1998;21(2-4):233-7. [PubMed Link Image]
Target 2 Drug References
  1. Burckhardt BC, Brai S, Wallis S, Krick W, Wolff NA, Burckhardt G: Transport of cimetidine by flounder and human renal organic anion transporter 1. Am J Physiol Renal Physiol. 2003 Mar;284(3):F503-9. Epub 2002 Nov 12. [PubMed Link Image]
  2. Khamdang S, Takeda M, Shimoda M, Noshiro R, Narikawa S, Huang XL, Enomoto A, Piyachaturawat P, Endou H: Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine. J Pharmacol Sci. 2004 Feb;94(2):197-202. [PubMed Link Image]
  3. Hashimoto T, Narikawa S, Huang XL, Minematsu T, Usui T, Kamimura H, Endou H: Characterization of the renal tubular transport of zonampanel, a novel alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptor antagonist, by human organic anion transporters. Drug Metab Dispos. 2004 Oct;32(10):1096-102. [PubMed Link Image]
  4. Motohashi H, Uwai Y, Hiramoto K, Okuda M, Inui K: Different transport properties between famotidine and cimetidine by human renal organic ion transporters (SLC22A). Eur J Pharmacol. 2004 Oct 25;503(1-3):25-30. [PubMed Link Image]
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This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.