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Identification
NameGuanethidine
Accession NumberDB01170  (APRD01007)
TypeSmall Molecule
GroupsApproved
DescriptionAn antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues. [PubChem]
Structure
Thumb
Synonyms
(2-(hexahydro-1(2h)-azocinyl)ethyl)guanidine
(2-(Octahydro-1-azocinyl)ethyl)guanidine
2-(1-N,N-Heptamethyleneimino)ethylguanidine
2-(1'-Azacyclooctyl)ethylguanidine
Azocine, 1-(2-guanidinoethyl)octahydro-
guanéthidine
guanethidinum
guanetidina
Guanidine, (2-(hexahydro-1(2H)-azocinyl)ethyl)-
Heptamethylenimine, 1-(2-guanidinoethyl)-
N-(2-Perhydroazocin-1-ylethyl)guanidine
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Guanethidine 10 Tab 10mgtablet10 mgoralPro Doc Limitee1984-12-311999-08-12Canada
Ismelin 25mgtablet25 mgoralCiba Pharmaceuticals, Ciba Geigy Canada Ltd.1960-12-311996-09-09Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo Guanethidine Sulfate Tab 10mgtablet10 mgoralApotex Inc1977-12-312013-03-28Canada
Apo Guanethidine Sulfate Tab 25mgtablet25 mgoralApotex Inc1977-12-312013-03-28Canada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
IsmedineChen Ho
IsmelinAmdipharm
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Guanethidine monosulfate
645-43-2
Thumb
  • InChI Key: YUFWAVFNITUSHI-UHFFFAOYSA-N
  • Monoisotopic Mass: 296.151826443
  • Average Mass: 296.39
DBSALT001071
Guanethidine sulfate
60-02-6
Thumb
  • InChI Key: NBJGGHFXCGHTNJ-UHFFFAOYSA-N
  • Monoisotopic Mass: 494.336273167
  • Average Mass: 494.7
DBSALT001861
Categories
UNIIZTI6C33Q2Q
CAS number55-65-2
WeightAverage: 198.3085
Monoisotopic: 198.184446724
Chemical FormulaC10H22N4
InChI KeyInChIKey=ACGDKVXYNVEAGU-UHFFFAOYSA-N
InChI
InChI=1S/C10H22N4/c11-10(12)13-6-9-14-7-4-2-1-3-5-8-14/h1-9H2,(H4,11,12,13)
IUPAC Name
2-[2-(azocan-1-yl)ethyl]guanidine
SMILES
NC(N)=NCCN1CCCCCCC1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as guanidines. These are compounds containing a guanidine moiety, with the general structure (R1R2N)(R3R4N)C=N-R5.
KingdomOrganic compounds
Super ClassOrganonitrogen compounds
ClassGuanidines
Sub ClassNot Available
Direct ParentGuanidines
Alternative Parents
Substituents
  • Tertiary aliphatic amine
  • Tertiary amine
  • Guanidine
  • Azacycle
  • Organoheterocyclic compound
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Carboximidamide
  • Hydrocarbon derivative
  • Amine
  • Aliphatic heteromonocyclic compound
Molecular FrameworkAliphatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of moderate and severe hypertension, either alone or as an adjunct, and for the treatment of renal hypertension.
PharmacodynamicsHigh blood pressure can cause the heart and arteries to not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure. High blood pressure may also increase the risk of heart attacks. These problems may be less likely to occur if blood pressure is controlled. Guanethidine works by decreasing the heart rate and relaxing the blood vessels so that blood can flow more easily through the body, thereby reducing these risks. It is a postganglionic sympathetic nerve terminal blocker that prevents the release of norepinephrine from nerve terminals.
Mechanism of actionGuanethidine acts at the sympathetic neuroeffector junction by inhibiting or interfering with the release and/or distribution of norepinephrine, rather than acting at the effector cell by inhibiting the association of norepinephrine with its receptors. It is taken up by norepinephrine transporters. It becomes concentrated in NE transmitter vesicles, replacing NE in these vesicles. This leads to a gradual depletion of NE stores in the nerve endings. Once inside the terminal it blocks the release of noradrenaline in response to arrival of an action potential. In contrast to ganglionic blocking agents, Guanethidine suppresses equally the responses mediated by alpha-and beta-adrenergic receptors but does not produce parasympathetic blockade. Since sympathetic blockade results in modest decreases in peripheral resistance and cardiac output, Guanethidine lowers blood pressure in the supine position. It further reduces blood pressure by decreasing the degree of vasoconstriction that normally results from reflex sympathetic nervous activity upon assumption of the upright posture, thus reducing venous return and cardiac output more.
Related Articles
Absorption3-30% of oral dose (poor and highly variable)
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Guanethidine is converted by the liver to three metabolites, which are excreted in the urine. The metabolites are pharmacologically less active than the parent compound.

Route of eliminationIsmelin is converted by the liver to three metabolites, which are excreted in the urine.
Half life1.5 days
Clearance
  • Renal cl=56 ml/min
ToxicitySide effects include drowsiness, dizziness, tiredness or confusion. LD50=1000 mg/kg (mouse, oral)
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+0.945
Blood Brain Barrier+0.9015
Caco-2 permeable-0.5683
P-glycoprotein substrateSubstrate0.7743
P-glycoprotein inhibitor INon-inhibitor0.9342
P-glycoprotein inhibitor IIInhibitor0.5063
Renal organic cation transporterInhibitor0.7586
CYP450 2C9 substrateNon-substrate0.8981
CYP450 2D6 substrateSubstrate0.6426
CYP450 3A4 substrateNon-substrate0.7884
CYP450 1A2 substrateNon-inhibitor0.908
CYP450 2C9 inhibitorNon-inhibitor0.9363
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.939
CYP450 3A4 inhibitorNon-inhibitor0.9611
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9748
Ames testNon AMES toxic0.6626
CarcinogenicityNon-carcinogens0.9595
BiodegradationNot ready biodegradable0.9883
Rat acute toxicity2.4210 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6083
hERG inhibition (predictor II)Non-inhibitor0.8115
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral10 mg
Tabletoral25 mg
Prices
Unit descriptionCostUnit
Guanethidine monosulf powder102.0USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point276-281U.S. Patent 2,928,829 U.S. Patent 3,006,913 U.S. Patent 3,055,882
water solubilityVery solubleNot Available
logP0.8Not Available
Predicted Properties
PropertyValueSource
Water Solubility2.25 mg/mLALOGPS
logP0.89ALOGPS
logP0.74ChemAxon
logS-1.9ALOGPS
pKa (Strongest Basic)11.77ChemAxon
Physiological Charge2ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area67.64 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity59.7 m3·mol-1ChemAxon
Polarizability23.67 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 Reference

U.S. Patent 2,928,829
U.S. Patent 3,006,913
U.S. Patent 3,055,882

General ReferencesNot Available
External Links
ATC CodesC02CC02C02LF01S01EX01
AHFS Codes
  • 24:08.32
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (74.5 KB)
Interactions
Drug Interactions
Drug
3,4-MethylenedioxyamphetamineThe serum concentration of 3,4-Methylenedioxyamphetamine can be decreased when it is combined with Guanethidine.
3,4-MethylenedioxymethamphetamineThe serum concentration of 3,4-Methylenedioxymethamphetamine can be decreased when it is combined with Guanethidine.
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypotensive activities of Guanethidine.
AcebutololGuanethidine may increase the hypotensive activities of Acebutolol.
AlfuzosinAlfuzosin may increase the hypotensive activities of Guanethidine.
AliskirenGuanethidine may increase the hypotensive activities of Aliskiren.
AlprenololAlprenolol may increase the hypotensive activities of Guanethidine.
AmbrisentanGuanethidine may increase the hypotensive activities of Ambrisentan.
AmifostineGuanethidine may increase the hypotensive activities of Amifostine.
AmlodipineAmlodipine may increase the hypotensive activities of Guanethidine.
AmphetamineThe serum concentration of Amphetamine can be decreased when it is combined with Guanethidine.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Guanethidine.
AtenololAtenolol may increase the hypotensive activities of Guanethidine.
BenazeprilBenazepril may increase the hypotensive activities of Guanethidine.
BendroflumethiazideBendroflumethiazide may increase the hypotensive activities of Guanethidine.
BenmoxinBenmoxin may increase the hypotensive activities of Guanethidine.
BenzphetamineThe serum concentration of Benzphetamine can be decreased when it is combined with Guanethidine.
BepridilGuanethidine may increase the hypotensive activities of Bepridil.
BetaxololBetaxolol may increase the hypotensive activities of Guanethidine.
BethanidineBethanidine may increase the hypotensive activities of Guanethidine.
BimatoprostBimatoprost may increase the hypotensive activities of Guanethidine.
BisoprololBisoprolol may increase the hypotensive activities of Guanethidine.
BosentanBosentan may increase the hypotensive activities of Guanethidine.
BretyliumBretylium may increase the hypotensive activities of Guanethidine.
BrimonidineGuanethidine may increase the hypotensive activities of Brimonidine.
BrimonidineBrimonidine may increase the antihypertensive activities of Guanethidine.
BupranololGuanethidine may increase the hypotensive activities of Bupranolol.
CandesartanCandesartan may increase the hypotensive activities of Guanethidine.
CandoxatrilCandoxatril may increase the hypotensive activities of Guanethidine.
CaptoprilGuanethidine may increase the hypotensive activities of Captopril.
CaroxazoneCaroxazone may increase the hypotensive activities of Guanethidine.
CarteololCarteolol may increase the hypotensive activities of Guanethidine.
CarvedilolCarvedilol may increase the hypotensive activities of Guanethidine.
CeliprololGuanethidine may increase the hypotensive activities of Celiprolol.
ChlorothiazideChlorothiazide may increase the hypotensive activities of Guanethidine.
ChlorphentermineThe serum concentration of Chlorphentermine can be decreased when it is combined with Guanethidine.
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Guanethidine.
CilazaprilGuanethidine may increase the hypotensive activities of Cilazapril.
ClonidineClonidine may increase the hypotensive activities of Guanethidine.
CryptenamineCryptenamine may increase the hypotensive activities of Guanethidine.
CyclothiazideCyclothiazide may increase the hypotensive activities of Guanethidine.
DebrisoquinGuanethidine may increase the hypotensive activities of Debrisoquin.
DeserpidineGuanethidine may increase the hypotensive activities of Deserpidine.
DextroamphetamineThe serum concentration of Dextroamphetamine can be decreased when it is combined with Guanethidine.
DiazoxideDiazoxide may increase the hypotensive activities of Guanethidine.
DiltiazemDiltiazem may increase the hypotensive activities of Guanethidine.
DorzolamideDorzolamide may increase the hypotensive activities of Guanethidine.
DoxazosinDoxazosin may increase the hypotensive activities of Guanethidine.
EfonidipineGuanethidine may increase the hypotensive activities of Efonidipine.
EnalaprilEnalapril may increase the hypotensive activities of Guanethidine.
EnalaprilatGuanethidine may increase the hypotensive activities of Enalaprilat.
EpoprostenolGuanethidine may increase the hypotensive activities of Epoprostenol.
EprosartanEprosartan may increase the hypotensive activities of Guanethidine.
FelodipineFelodipine may increase the hypotensive activities of Guanethidine.
FenoldopamFenoldopam may increase the hypotensive activities of Guanethidine.
FosinoprilFosinopril may increase the hypotensive activities of Guanethidine.
FurazolidoneFurazolidone may increase the hypotensive activities of Guanethidine.
GuanabenzGuanabenz may increase the hypotensive activities of Guanethidine.
GuanadrelGuanadrel may increase the hypotensive activities of Guanethidine.
GuanfacineGuanfacine may increase the hypotensive activities of Guanethidine.
HexamethoniumGuanethidine may increase the hypotensive activities of Hexamethonium.
HydracarbazineHydracarbazine may increase the hypotensive activities of Guanethidine.
HydralazineGuanethidine may increase the hypotensive activities of Hydralazine.
HydrochlorothiazideHydrochlorothiazide may increase the hypotensive activities of Guanethidine.
HydroflumethiazideHydroflumethiazide may increase the hypotensive activities of Guanethidine.
Hydroxyamphetamine hydrobromideThe serum concentration of Hydroxyamphetamine hydrobromide can be decreased when it is combined with Guanethidine.
IloprostIloprost may increase the hypotensive activities of Guanethidine.
IndapamideIndapamide may increase the hypotensive activities of Guanethidine.
IndenololGuanethidine may increase the hypotensive activities of Indenolol.
IndoraminGuanethidine may increase the hypotensive activities of Indoramin.
IproclozideIproclozide may increase the hypotensive activities of Guanethidine.
IproniazidIproniazid may increase the hypotensive activities of Guanethidine.
IrbesartanIrbesartan may increase the hypotensive activities of Guanethidine.
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Guanethidine.
IsradipineIsradipine may increase the hypotensive activities of Guanethidine.
LabetalolLabetalol may increase the hypotensive activities of Guanethidine.
LacidipineGuanethidine may increase the hypotensive activities of Lacidipine.
LatanoprostLatanoprost may increase the hypotensive activities of Guanethidine.
LercanidipineLercanidipine may increase the hypotensive activities of Guanethidine.
LisdexamfetamineThe serum concentration of Lisdexamfetamine can be decreased when it is combined with Guanethidine.
LisinoprilLisinopril may increase the hypotensive activities of Guanethidine.
LofexidineGuanethidine may increase the hypotensive activities of Lofexidine.
LosartanLosartan may increase the hypotensive activities of Guanethidine.
MacitentanGuanethidine may increase the hypotensive activities of Macitentan.
ManidipineGuanethidine may increase the hypotensive activities of Manidipine.
MebanazineMebanazine may increase the hypotensive activities of Guanethidine.
MecamylamineMecamylamine may increase the hypotensive activities of Guanethidine.
MephentermineThe serum concentration of Mephentermine can be decreased when it is combined with Guanethidine.
MethamphetamineThe serum concentration of Methamphetamine can be decreased when it is combined with Guanethidine.
MethyldopaMethyldopa may increase the hypotensive activities of Guanethidine.
Methylene blueMethylene blue may increase the hypotensive activities of Guanethidine.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Guanethidine.
MetipranololGuanethidine may increase the hypotensive activities of Metipranolol.
MetolazoneMetolazone may increase the hypotensive activities of Guanethidine.
MetoprololMetoprolol may increase the hypotensive activities of Guanethidine.
MibefradilGuanethidine may increase the hypotensive activities of Mibefradil.
MinaprineMinaprine may increase the hypotensive activities of Guanethidine.
MinoxidilMinoxidil may increase the hypotensive activities of Guanethidine.
MoclobemideMoclobemide may increase the hypotensive activities of Guanethidine.
MoexiprilMoexipril may increase the hypotensive activities of Guanethidine.
MolsidomineMolsidomine may increase the hypotensive activities of Guanethidine.
MoxonidineGuanethidine may increase the hypotensive activities of Moxonidine.
NadololGuanethidine may increase the hypotensive activities of Nadolol.
NebivololGuanethidine may increase the hypotensive activities of Nebivolol.
NialamideNialamide may increase the hypotensive activities of Guanethidine.
NicardipineNicardipine may increase the hypotensive activities of Guanethidine.
NicorandilGuanethidine may increase the hypotensive activities of Nicorandil.
NiguldipineGuanethidine may increase the hypotensive activities of Niguldipine.
NilvadipineGuanethidine may increase the hypotensive activities of Nilvadipine.
NimodipineNimodipine may increase the hypotensive activities of Guanethidine.
NintedanibThe serum concentration of Nintedanib can be decreased when it is combined with Guanethidine.
NisoldipineNisoldipine may increase the hypotensive activities of Guanethidine.
NitrendipineNitrendipine may increase the hypotensive activities of Guanethidine.
NitroprussideNitroprusside may increase the hypotensive activities of Guanethidine.
ObinutuzumabGuanethidine may increase the hypotensive activities of Obinutuzumab.
OctamoxinOctamoxin may increase the hypotensive activities of Guanethidine.
OlmesartanOlmesartan may increase the hypotensive activities of Guanethidine.
OmapatrilatOmapatrilat may increase the hypotensive activities of Guanethidine.
OxprenololGuanethidine may increase the hypotensive activities of Oxprenolol.
PargylineGuanethidine may increase the hypotensive activities of Pargyline.
PenbutololGuanethidine may increase the hypotensive activities of Penbutolol.
PentoliniumPentolinium may increase the hypotensive activities of Guanethidine.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Guanethidine.
PerindoprilPerindopril may increase the hypotensive activities of Guanethidine.
PhenelzinePhenelzine may increase the hypotensive activities of Guanethidine.
PheniprazinePheniprazine may increase the hypotensive activities of Guanethidine.
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Guanethidine.
PhenoxypropazinePhenoxypropazine may increase the hypotensive activities of Guanethidine.
PhentermineThe serum concentration of Phentermine can be decreased when it is combined with Guanethidine.
PhentolaminePhentolamine may increase the hypotensive activities of Guanethidine.
PinacidilGuanethidine may increase the hypotensive activities of Pinacidil.
PindololPindolol may increase the hypotensive activities of Guanethidine.
PirlindolePirlindole may increase the hypotensive activities of Guanethidine.
PivhydrazinePivhydrazine may increase the hypotensive activities of Guanethidine.
PolythiazideGuanethidine may increase the hypotensive activities of Polythiazide.
PrazosinPrazosin may increase the hypotensive activities of Guanethidine.
PropranololPropranolol may increase the hypotensive activities of Guanethidine.
QuinaprilQuinapril may increase the hypotensive activities of Guanethidine.
QuinineQuinine may increase the hypotensive activities of Guanethidine.
RamiprilRamipril may increase the hypotensive activities of Guanethidine.
RasagilineRasagiline may increase the hypotensive activities of Guanethidine.
RemikirenRemikiren may increase the hypotensive activities of Guanethidine.
RescinnamineGuanethidine may increase the hypotensive activities of Rescinnamine.
ReserpineReserpine may increase the hypotensive activities of Guanethidine.
RiociguatGuanethidine may increase the hypotensive activities of Riociguat.
RituximabGuanethidine may increase the hypotensive activities of Rituximab.
SafrazineSafrazine may increase the hypotensive activities of Guanethidine.
SaprisartanGuanethidine may increase the hypotensive activities of Saprisartan.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Guanethidine.
SelegilineSelegiline may increase the hypotensive activities of Guanethidine.
SelexipagGuanethidine may increase the hypotensive activities of Selexipag.
SildenafilSildenafil may increase the antihypertensive activities of Guanethidine.
SitaxentanGuanethidine may increase the hypotensive activities of Sitaxentan.
SpiraprilGuanethidine may increase the hypotensive activities of Spirapril.
TadalafilTadalafil may increase the antihypertensive activities of Guanethidine.
TelmisartanTelmisartan may increase the hypotensive activities of Guanethidine.
TemocaprilGuanethidine may increase the hypotensive activities of Temocapril.
TerlipressinGuanethidine may increase the hypotensive activities of Terlipressin.
TiboloneGuanethidine may increase the hypotensive activities of Tibolone.
TicrynafenGuanethidine may increase the hypotensive activities of Ticrynafen.
TimololTimolol may increase the hypotensive activities of Guanethidine.
TolazolineTolazoline may increase the hypotensive activities of Guanethidine.
ToloxatoneToloxatone may increase the hypotensive activities of Guanethidine.
TorasemideTorasemide may increase the hypotensive activities of Guanethidine.
TrandolaprilTrandolapril may increase the hypotensive activities of Guanethidine.
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Guanethidine.
TranylcypromineTranylcypromine may increase the hypotensive activities of Guanethidine.
TravoprostTravoprost may increase the hypotensive activities of Guanethidine.
TreprostinilTreprostinil may increase the hypotensive activities of Guanethidine.
TrichlormethiazideTrichlormethiazide may increase the hypotensive activities of Guanethidine.
TrimazosinGuanethidine may increase the hypotensive activities of Trimazosin.
TrimethaphanTrimethaphan may increase the hypotensive activities of Guanethidine.
UdenafilUdenafil may increase the antihypertensive activities of Guanethidine.
UnoprostoneGuanethidine may increase the hypotensive activities of Unoprostone.
ValsartanValsartan may increase the hypotensive activities of Guanethidine.
VardenafilVardenafil may increase the antihypertensive activities of Guanethidine.
XylometazolineGuanethidine may increase the hypotensive activities of Xylometazoline.
YohimbineYohimbine may decrease the antihypertensive activities of Guanethidine.
Food Interactions
  • Take without regard to meals.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inducer
General Function:
Norepinephrine:sodium symporter activity
Specific Function:
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A2
Uniprot ID:
P23975
Molecular Weight:
69331.42 Da
References
  1. Joyce PI, Atcheson R, Marcus RJ, Heffernan AM, Rowbotham DJ, Lambert DG: Interaction of local anaesthetic agents with the endogenous norepinephrine transporter in SH-SY5Y human neuroblastoma cells. Neurosci Lett. 2001 Jun 15;305(3):161-4. [PubMed:11403930 ]
  2. Yi E, Love JA: Alpha-adrenergic modulation of synaptic transmission in rabbit pancreatic ganglia. Auton Neurosci. 2005 Oct 30;122(1-2):45-57. Epub 2005 Aug 25. [PubMed:16126010 ]
  3. Galli A, Blakely RD, DeFelice LJ: Norepinephrine transporters have channel modes of conduction. Proc Natl Acad Sci U S A. 1996 Aug 6;93(16):8671-6. [PubMed:8710929 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23