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Identification
NamePhenformin
Accession NumberDB00914  (APRD00511)
TypeSmall Molecule
GroupsApproved, Withdrawn
DescriptionA biguanide hypoglycemic agent with actions and uses similar to those of metformin. Although it is generally considered to be associated with an unacceptably high incidence of lactic acidosis, often fatal, it is still available in some countries. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290)
Structure
Thumb
Synonyms
DBI
Fenformin
Fenformina
Phenformine
Phenforminum
β-Phenethybiguanide
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
DBICiba-Geigy
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Phenformin Hydrochloride
834-28-6
Thumb
  • InChI Key: YSUCWSWKRIOILX-UHFFFAOYSA-N
  • Monoisotopic Mass: 241.109423244
  • Average Mass: 241.721
DBSALT000273
Categories
UNIIDD5K7529CE
CAS number114-86-3
WeightAverage: 205.2596
Monoisotopic: 205.132745505
Chemical FormulaC10H15N5
InChI KeyInChIKey=ICFJFFQQTFMIBG-UHFFFAOYSA-N
InChI
InChI=1S/C10H15N5/c11-9(12)15-10(13)14-7-6-8-4-2-1-3-5-8/h1-5H,6-7H2,(H6,11,12,13,14,15)
IUPAC Name
1-carbamimidamido-N-(2-phenylethyl)methanimidamide
SMILES
NC(=N)NC(=N)NCCC1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenethylamines. These are compounds containing a phenethylamine moiety, which consists of a phenyl group substituted at the second position by an ethan-1-amine.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenethylamines
Direct ParentPhenethylamines
Alternative Parents
Substituents
  • Phenethylamine
  • Biguanide
  • Guanidine
  • Carboximidamide
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Imine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the reatment of type II diabetes mellitus.
PharmacodynamicsUsed to treat diabetes, phenformin is a biguanide (contains 2 guanidino groups) hypoglycemic agent with actions and uses similar to those of metformin (Glucophage). Both drugs work by (1) decreasing the absorption of glucose by the intestines, (2) decreasing the production of glucose in the liver, and by (3) increasing the body's ability to use insulin more effectively. More specifically, phenformin improves glycemic control by improving insulin sensitivity. Phenformin is generally considered to be associated with an unacceptably high incidence of actic acidosis. In general biguanides should be used only in stable type II diabetics who are free of liver, kidney and cardiovascular problems and who cannot be controlled with diet.
Mechanism of actionPhenformin binds to the AMP-activated protein kinase (AMPK). AMPK is an ultra-sensitive cellular energy sensor that monitors energy consumption and down-regulates ATP-consuming processes when activated. The biguanide phenformin has been shown to independently decrease ion transport processes, influence cellular metabolism and activate AMPK. Phenformin's hypoglycemic activity is related the effect it has in activating AMPK and fooling insulin sensitive cells into thinking that insulin levels are low and causing the body to use glucose as if in a state of low caloric consumption. This drug also seems to inhibit several varients of ATP-sensitive potassium channels (namely the receptor subtype Kir6.1).
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9604
Blood Brain Barrier+0.6967
Caco-2 permeable-0.5144
P-glycoprotein substrateNon-substrate0.5078
P-glycoprotein inhibitor INon-inhibitor0.9322
P-glycoprotein inhibitor IINon-inhibitor0.6863
Renal organic cation transporterInhibitor0.6874
CYP450 2C9 substrateNon-substrate0.7776
CYP450 2D6 substrateSubstrate0.8415
CYP450 3A4 substrateNon-substrate0.7896
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9163
CYP450 2D6 inhibitorInhibitor0.8875
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.881
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9116
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.928
BiodegradationNot ready biodegradable0.692
Rat acute toxicity2.5305 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9162
hERG inhibition (predictor II)Non-inhibitor0.901
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point176.5 °CPhysProp
water solubility210 mg/mLNot Available
logP-0.83HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.232 mg/mLALOGPS
logP-0.72ALOGPS
logP0.83ChemAxon
logS-3ALOGPS
pKa (Strongest Basic)11.97ChemAxon
Physiological Charge2ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count5ChemAxon
Polar Surface Area97.78 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity80.72 m3·mol-1ChemAxon
Polarizability22.14 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis ReferenceNot Available
General References
  1. Enia G, Garozzo M, Zoccali C: Lactic acidosis induced by phenformin is still a public health problem in Italy. BMJ. 1997 Nov 29;315(7120):1466-7. [PubMed:9418116 ]
  2. Rosand J, Friedberg JW, Yang JM: Fatal phenformin-associated lactic acidosis. Ann Intern Med. 1997 Jul 15;127(2):170. [PubMed:9230023 ]
External Links
ATC CodesA10BA01A10BD01
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneThe metabolism of Phenformin can be decreased when combined with Abiraterone.
AmiodaroneThe metabolism of Phenformin can be decreased when combined with Amiodarone.
AripiprazoleThe therapeutic efficacy of Phenformin can be decreased when used in combination with Aripiprazole.
Arsenic trioxideThe therapeutic efficacy of Phenformin can be decreased when used in combination with Arsenic trioxide.
ArtemetherThe metabolism of Phenformin can be decreased when combined with Artemether.
ArticaineThe therapeutic efficacy of Phenformin can be decreased when used in combination with Articaine.
AsenapineThe therapeutic efficacy of Phenformin can be decreased when used in combination with Asenapine.
AtazanavirThe therapeutic efficacy of Phenformin can be decreased when used in combination with Atazanavir.
AtomoxetineThe metabolism of Phenformin can be decreased when combined with Atomoxetine.
BendroflumethiazideThe therapeutic efficacy of Phenformin can be decreased when used in combination with Bendroflumethiazide.
BetamethasoneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Betamethasone.
BetaxololThe metabolism of Phenformin can be decreased when combined with Betaxolol.
BrexpiprazoleThe therapeutic efficacy of Phenformin can be decreased when used in combination with Brexpiprazole.
BumetanideThe therapeutic efficacy of Phenformin can be decreased when used in combination with Bumetanide.
BupropionThe metabolism of Phenformin can be decreased when combined with Bupropion.
BuserelinThe therapeutic efficacy of Phenformin can be decreased when used in combination with Buserelin.
CelecoxibThe metabolism of Phenformin can be decreased when combined with Celecoxib.
CeritinibThe therapeutic efficacy of Phenformin can be decreased when used in combination with Ceritinib.
ChloroquineThe metabolism of Phenformin can be decreased when combined with Chloroquine.
ChlorothiazideThe therapeutic efficacy of Phenformin can be decreased when used in combination with Chlorothiazide.
ChlorpromazineThe metabolism of Phenformin can be decreased when combined with Chlorpromazine.
ChlorpropamidePhenformin may increase the hypoglycemic activities of Chlorpropamide.
ChlorthalidoneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Chlorthalidone.
CholecalciferolThe metabolism of Phenformin can be decreased when combined with Cholecalciferol.
CimetidineThe metabolism of Phenformin can be decreased when combined with Cimetidine.
CinacalcetThe metabolism of Phenformin can be decreased when combined with Cinacalcet.
CitalopramThe metabolism of Phenformin can be decreased when combined with Citalopram.
ClemastineThe metabolism of Phenformin can be decreased when combined with Clemastine.
ClobazamThe metabolism of Phenformin can be decreased when combined with Clobazam.
ClomipramineThe metabolism of Phenformin can be decreased when combined with Clomipramine.
ClotrimazoleThe metabolism of Phenformin can be decreased when combined with Clotrimazole.
ClozapineThe therapeutic efficacy of Phenformin can be decreased when used in combination with Clozapine.
CobicistatThe serum concentration of Phenformin can be increased when it is combined with Cobicistat.
CocaineThe metabolism of Phenformin can be decreased when combined with Cocaine.
CorticotropinThe therapeutic efficacy of Phenformin can be decreased when used in combination with Corticotropin.
Cortisone acetateThe therapeutic efficacy of Phenformin can be decreased when used in combination with Cortisone acetate.
Cyproterone acetateThe therapeutic efficacy of Phenformin can be decreased when used in combination with Cyproterone acetate.
DabrafenibThe therapeutic efficacy of Phenformin can be decreased when used in combination with Dabrafenib.
DanazolThe therapeutic efficacy of Phenformin can be decreased when used in combination with Danazol.
DarifenacinThe metabolism of Phenformin can be decreased when combined with Darifenacin.
DarunavirThe serum concentration of Phenformin can be increased when it is combined with Darunavir.
DelavirdineThe metabolism of Phenformin can be decreased when combined with Delavirdine.
DesipramineThe metabolism of Phenformin can be decreased when combined with Desipramine.
DesogestrelThe therapeutic efficacy of Phenformin can be decreased when used in combination with Desogestrel.
DexamethasoneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Dexamethasone.
DiazoxideThe therapeutic efficacy of Phenformin can be decreased when used in combination with Diazoxide.
DienogestThe therapeutic efficacy of Phenformin can be decreased when used in combination with Dienogest.
DiphenhydramineThe metabolism of Phenformin can be decreased when combined with Diphenhydramine.
DisopyramidePhenformin may increase the hypoglycemic activities of Disopyramide.
DronedaroneThe metabolism of Phenformin can be decreased when combined with Dronedarone.
DrospirenoneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Drospirenone.
DuloxetineThe metabolism of Phenformin can be decreased when combined with Duloxetine.
EliglustatThe metabolism of Phenformin can be decreased when combined with Eliglustat.
EpinephrineThe therapeutic efficacy of Phenformin can be decreased when used in combination with Epinephrine.
EstradiolThe therapeutic efficacy of Phenformin can be decreased when used in combination with Estradiol.
Estrone sulfateThe therapeutic efficacy of Phenformin can be decreased when used in combination with Estrone sulfate.
Etacrynic acidThe therapeutic efficacy of Phenformin can be decreased when used in combination with Etacrynic acid.
Ethinyl EstradiolThe therapeutic efficacy of Phenformin can be decreased when used in combination with Ethinyl Estradiol.
Ethynodiol diacetateThe therapeutic efficacy of Phenformin can be decreased when used in combination with Ethynodiol diacetate.
EtonogestrelThe therapeutic efficacy of Phenformin can be decreased when used in combination with Etonogestrel.
EverolimusThe therapeutic efficacy of Phenformin can be decreased when used in combination with Everolimus.
FludrocortisoneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Fludrocortisone.
FluoxetineThe metabolism of Phenformin can be decreased when combined with Fluoxetine.
FluvoxamineThe metabolism of Phenformin can be decreased when combined with Fluvoxamine.
FosamprenavirThe therapeutic efficacy of Phenformin can be decreased when used in combination with Fosamprenavir.
FurosemideThe therapeutic efficacy of Phenformin can be decreased when used in combination with Furosemide.
GliclazidePhenformin may increase the hypoglycemic activities of Gliclazide.
GlimepiridePhenformin may increase the hypoglycemic activities of Glimepiride.
GlipizidePhenformin may increase the hypoglycemic activities of Glipizide.
GlyburidePhenformin may increase the hypoglycemic activities of Glyburide.
GoserelinThe therapeutic efficacy of Phenformin can be decreased when used in combination with Goserelin.
HaloperidolThe metabolism of Phenformin can be decreased when combined with Haloperidol.
HistrelinThe therapeutic efficacy of Phenformin can be decreased when used in combination with Histrelin.
HydrochlorothiazideThe therapeutic efficacy of Phenformin can be decreased when used in combination with Hydrochlorothiazide.
HydrocortisoneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Hydrocortisone.
HydroflumethiazideThe therapeutic efficacy of Phenformin can be decreased when used in combination with Hydroflumethiazide.
Hydroxyprogesterone caproateThe therapeutic efficacy of Phenformin can be decreased when used in combination with Hydroxyprogesterone caproate.
IloperidoneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Iloperidone.
ImipramineThe metabolism of Phenformin can be decreased when combined with Imipramine.
IndapamideThe therapeutic efficacy of Phenformin can be decreased when used in combination with Indapamide.
IndinavirThe therapeutic efficacy of Phenformin can be decreased when used in combination with Indinavir.
Insulin AspartPhenformin may increase the hypoglycemic activities of Insulin Aspart.
Insulin DetemirPhenformin may increase the hypoglycemic activities of Insulin Detemir.
Insulin GlarginePhenformin may increase the hypoglycemic activities of Insulin Glargine.
Insulin GlulisinePhenformin may increase the hypoglycemic activities of Insulin Glulisine.
Insulin HumanPhenformin may increase the hypoglycemic activities of Insulin Human.
Insulin LisproPhenformin may increase the hypoglycemic activities of Insulin Lispro.
IsoniazidThe metabolism of Phenformin can be decreased when combined with Isoniazid.
KetoconazoleThe metabolism of Phenformin can be decreased when combined with Ketoconazole.
LanreotideThe therapeutic efficacy of Phenformin can be decreased when used in combination with Lanreotide.
LanreotidePhenformin may increase the hypoglycemic activities of Lanreotide.
LeuprolideThe therapeutic efficacy of Phenformin can be decreased when used in combination with Leuprolide.
LevonorgestrelThe therapeutic efficacy of Phenformin can be decreased when used in combination with Levonorgestrel.
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Phenformin.
LopinavirThe therapeutic efficacy of Phenformin can be decreased when used in combination with Lopinavir.
LorcaserinThe metabolism of Phenformin can be decreased when combined with Lorcaserin.
LumefantrineThe metabolism of Phenformin can be decreased when combined with Lumefantrine.
LurasidoneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Lurasidone.
MecaserminPhenformin may increase the hypoglycemic activities of Mecasermin.
Medroxyprogesterone acetateThe therapeutic efficacy of Phenformin can be decreased when used in combination with Medroxyprogesterone acetate.
Megestrol acetateThe therapeutic efficacy of Phenformin can be decreased when used in combination with Megestrol acetate.
MestranolThe therapeutic efficacy of Phenformin can be decreased when used in combination with Mestranol.
MethadoneThe metabolism of Phenformin can be decreased when combined with Methadone.
MethotrimeprazineThe therapeutic efficacy of Phenformin can be decreased when used in combination with Methotrimeprazine.
MethyclothiazideThe therapeutic efficacy of Phenformin can be decreased when used in combination with Methyclothiazide.
MethylprednisoloneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Methylprednisolone.
MetolazoneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Metolazone.
MetoprololThe metabolism of Phenformin can be decreased when combined with Metoprolol.
MifepristonePhenformin may increase the hypoglycemic activities of Mifepristone.
MirabegronThe metabolism of Phenformin can be decreased when combined with Mirabegron.
NateglinidePhenformin may increase the hypoglycemic activities of Nateglinide.
NelfinavirThe therapeutic efficacy of Phenformin can be decreased when used in combination with Nelfinavir.
NevirapineThe metabolism of Phenformin can be decreased when combined with Nevirapine.
NiacinThe therapeutic efficacy of Phenformin can be decreased when used in combination with Niacin.
NicardipineThe metabolism of Phenformin can be decreased when combined with Nicardipine.
NilotinibThe therapeutic efficacy of Phenformin can be decreased when used in combination with Nilotinib.
NorethisteroneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Norethisterone.
NorgestimateThe therapeutic efficacy of Phenformin can be decreased when used in combination with Norgestimate.
OctreotideThe therapeutic efficacy of Phenformin can be decreased when used in combination with Octreotide.
OctreotidePhenformin may increase the hypoglycemic activities of Octreotide.
OlanzapineThe therapeutic efficacy of Phenformin can be decreased when used in combination with Olanzapine.
PaliperidoneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Paliperidone.
PanobinostatThe metabolism of Phenformin can be decreased when combined with Panobinostat.
ParoxetineThe metabolism of Phenformin can be decreased when combined with Paroxetine.
PasireotideThe therapeutic efficacy of Phenformin can be decreased when used in combination with Pasireotide.
PasireotidePhenformin may increase the hypoglycemic activities of Pasireotide.
Peginterferon alfa-2bThe serum concentration of Phenformin can be decreased when it is combined with Peginterferon alfa-2b.
PentamidineThe therapeutic efficacy of Phenformin can be decreased when used in combination with Pentamidine.
PentamidinePhenformin may increase the hypoglycemic activities of Pentamidine.
PiperazineThe therapeutic efficacy of Phenformin can be decreased when used in combination with Piperazine.
PipotiazineThe therapeutic efficacy of Phenformin can be decreased when used in combination with Pipotiazine.
PolythiazideThe therapeutic efficacy of Phenformin can be decreased when used in combination with Polythiazide.
PrednisoloneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Prednisolone.
PrednisoneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Prednisone.
ProgesteroneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Progesterone.
PromazineThe metabolism of Phenformin can be decreased when combined with Promazine.
QuetiapineThe therapeutic efficacy of Phenformin can be decreased when used in combination with Quetiapine.
QuinethazoneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Quinethazone.
QuinidineThe metabolism of Phenformin can be decreased when combined with Quinidine.
QuininePhenformin may increase the hypoglycemic activities of Quinine.
QuinineThe metabolism of Phenformin can be decreased when combined with Quinine.
RanolazineThe metabolism of Phenformin can be decreased when combined with Ranolazine.
RepaglinidePhenformin may increase the hypoglycemic activities of Repaglinide.
RisperidoneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Risperidone.
RitonavirThe therapeutic efficacy of Phenformin can be decreased when used in combination with Ritonavir.
RolapitantThe metabolism of Phenformin can be decreased when combined with Rolapitant.
RopiniroleThe metabolism of Phenformin can be decreased when combined with Ropinirole.
SaquinavirThe therapeutic efficacy of Phenformin can be decreased when used in combination with Saquinavir.
SertralineThe metabolism of Phenformin can be decreased when combined with Sertraline.
SirolimusThe therapeutic efficacy of Phenformin can be decreased when used in combination with Sirolimus.
StiripentolThe metabolism of Phenformin can be decreased when combined with Stiripentol.
SulfadiazinePhenformin may increase the hypoglycemic activities of Sulfadiazine.
SulfamethoxazolePhenformin may increase the hypoglycemic activities of Sulfamethoxazole.
SulfisoxazolePhenformin may increase the hypoglycemic activities of Sulfisoxazole.
SunitinibPhenformin may increase the hypoglycemic activities of Sunitinib.
TacrolimusThe therapeutic efficacy of Phenformin can be decreased when used in combination with Tacrolimus.
TemsirolimusThe therapeutic efficacy of Phenformin can be decreased when used in combination with Temsirolimus.
TerbinafineThe metabolism of Phenformin can be decreased when combined with Terbinafine.
ThioridazineThe metabolism of Phenformin can be decreased when combined with Thioridazine.
TiclopidineThe metabolism of Phenformin can be decreased when combined with Ticlopidine.
TipranavirThe therapeutic efficacy of Phenformin can be decreased when used in combination with Tipranavir.
TolazamidePhenformin may increase the hypoglycemic activities of Tolazamide.
TolbutamidePhenformin may increase the hypoglycemic activities of Tolbutamide.
TorasemideThe therapeutic efficacy of Phenformin can be decreased when used in combination with Torasemide.
TranylcypromineThe metabolism of Phenformin can be decreased when combined with Tranylcypromine.
TriamcinoloneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Triamcinolone.
TrichlormethiazideThe therapeutic efficacy of Phenformin can be decreased when used in combination with Trichlormethiazide.
TriptorelinThe therapeutic efficacy of Phenformin can be decreased when used in combination with Triptorelin.
VenlafaxineThe metabolism of Phenformin can be decreased when combined with Venlafaxine.
VorinostatThe therapeutic efficacy of Phenformin can be decreased when used in combination with Vorinostat.
ZiprasidoneThe therapeutic efficacy of Phenformin can be decreased when used in combination with Ziprasidone.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
activator
General Function:
Tau-protein kinase activity
Specific Function:
Catalytic subunit of AMP-activated protein kinase (AMPK), an energy sensor protein kinase that plays a key role in regulating cellular energy metabolism. In response to reduction of intracellular ATP levels, AMPK activates energy-producing pathways and inhibits energy-consuming processes: inhibits protein, carbohydrate and lipid biosynthesis, as well as cell growth and proliferation. AMPK acts ...
Gene Name:
PRKAA1
Uniprot ID:
Q13131
Molecular Weight:
64008.64 Da
References
  1. Woollhead AM, Sivagnanasundaram J, Kalsi KK, Pucovsky V, Pellatt LJ, Scott JW, Mustard KJ, Hardie DG, Baines DL: Pharmacological activators of AMP-activated protein kinase have different effects on Na+ transport processes across human lung epithelial cells. Br J Pharmacol. 2007 Aug;151(8):1204-15. Epub 2007 Jul 2. [PubMed:17603555 ]
  2. Chen S, Murphy J, Toth R, Campbell DG, Morrice NA, Mackintosh C: Complementary regulation of TBC1D1 and AS160 by growth factors, insulin and AMPK activators. Biochem J. 2008 Jan 15;409(2):449-59. [PubMed:17995453 ]
  3. Zhang L, He H, Balschi JA: Metformin and phenformin activate AMP-activated protein kinase in the heart by increasing cytosolic AMP concentration. Am J Physiol Heart Circ Physiol. 2007 Jul;293(1):H457-66. Epub 2007 Mar 16. [PubMed:17369473 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Inward rectifier potassium channel activity
Specific Function:
This potassium channel is controlled by G proteins. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward...
Gene Name:
KCNJ8
Uniprot ID:
Q15842
Molecular Weight:
47967.455 Da
References
  1. Aziz Q, Thomas A, Khambra T, Tinker A: Phenformin has a direct inhibitory effect on the ATP-sensitive potassium channel. Eur J Pharmacol. 2010 May 25;634(1-3):26-32. doi: 10.1016/j.ejphar.2010.02.023. Epub 2010 Feb 25. [PubMed:20188727 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Quaternary ammonium group transmembrane transporter activity
Specific Function:
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creatinine, amantadine, memantine, acriflavine, 4-[4-(dimethylamino)-styryl]-N-methylpyridinium ASP, amiloride, metformin, N-1-methylnicotinamide (NMN), tetraethylammonium (TEA), 1-methyl-4-phenylpyridiniu...
Gene Name:
SLC22A2
Uniprot ID:
O15244
Molecular Weight:
62579.99 Da
References
  1. Dresser MJ, Xiao G, Leabman MK, Gray AT, Giacomini KM: Interactions of n-tetraalkylammonium compounds and biguanides with a human renal organic cation transporter (hOCT2). Pharm Res. 2002 Aug;19(8):1244-7. [PubMed:12240953 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Secondary active organic cation transmembrane transporter activity
Specific 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...
Gene Name:
SLC22A1
Uniprot ID:
O15245
Molecular Weight:
61153.345 Da
References
  1. Dresser MJ, Xiao G, Leabman MK, Gray AT, Giacomini KM: Interactions of n-tetraalkylammonium compounds and biguanides with a human renal organic cation transporter (hOCT2). Pharm Res. 2002 Aug;19(8):1244-7. [PubMed:12240953 ]
  2. Wang DS, Jonker JW, Kato Y, Kusuhara H, Schinkel AH, Sugiyama Y: Involvement of organic cation transporter 1 in hepatic and intestinal distribution of metformin. J Pharmacol Exp Ther. 2002 Aug;302(2):510-5. [PubMed:12130709 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23