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Identification
NameGuanabenz
Accession NumberDB00629  (APRD00487)
TypeSmall Molecule
GroupsApproved
DescriptionAn alpha-2 selective adrenergic agonist used as an antihypertensive agent. [PubChem]
Structure
Thumb
Synonyms
Guanabenz
Guanabenzo
Guanabenzum
WY-8678
Wytensin
External Identifiers
  • BR 750
  • FLA 137
  • GBZ
  • SD 15468
  • Wy 8678
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
LisapresLibbs
RexiteneL.P.B.
WytensAlfresa Pharma
WytensinWyeth
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Guanabenz Acetate
Thumb
  • InChI Key: MCSPBPXATWBACD-GAYQJXMFSA-N
  • Monoisotopic Mass: 290.033731062
  • Average Mass: 291.134
DBSALT000649
Categories
UNIIGGD30112WC
CAS number5051-62-7
WeightAverage: 231.082
Monoisotopic: 230.01260169
Chemical FormulaC8H8Cl2N4
InChI KeyInChIKey=WDZVGELJXXEGPV-YIXHJXPBSA-N
InChI
InChI=1S/C8H8Cl2N4/c9-6-2-1-3-7(10)5(6)4-13-14-8(11)12/h1-4H,(H4,11,12,14)/b13-4+
IUPAC Name
2-{[(2,6-dichlorophenyl)methylidene]amino}guanidine
SMILES
NC(N)=NN=CC1=C(Cl)C=CC=C1Cl
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as dichlorobenzenes. These are compounds containing a benzene with exactly two chlorine atoms attached to it.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassHalobenzenes
Direct ParentDichlorobenzenes
Alternative Parents
Substituents
  • 1,3-dichlorobenzene
  • Aryl halide
  • Aryl chloride
  • Guanidine
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor management of High blood pressure
PharmacodynamicsGuanabenz, a centrally acting α-2 adrenergic agonist, is indicated for treatment of hypertension.
Mechanism of actionGuanabenz's antihypertensive effect is thought to be due to central alpha-adrenergic stimulation, which results in a decreased sympathetic outflow to the heart, kidneys, and peripheral vasculature in addition to a decreased systolic and diastolic blood pressure and a slight slowing of pulse rate. Chronic administration of guanabenz also causes a decrease in peripheral vascular resistance.
Related Articles
AbsorptionApproximately 75% absorbed from gastrointestinal tract
Volume of distributionNot Available
Protein binding90%
Metabolism

Hepatic

Route of eliminationNot Available
Half life6 hours.
ClearanceNot Available
ToxicityExcessive contraction of the pupils, irritability, low blood pressure, sleepiness, slow heartbeat, sluggishness
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+0.9921
Blood Brain Barrier+0.8593
Caco-2 permeable+0.8867
P-glycoprotein substrateNon-substrate0.6838
P-glycoprotein inhibitor INon-inhibitor0.9248
P-glycoprotein inhibitor IINon-inhibitor0.9857
Renal organic cation transporterNon-inhibitor0.6424
CYP450 2C9 substrateNon-substrate0.8798
CYP450 2D6 substrateNon-substrate0.9003
CYP450 3A4 substrateNon-substrate0.7563
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.925
CYP450 2D6 inhibitorInhibitor0.884
CYP450 2C19 inhibitorNon-inhibitor0.9158
CYP450 3A4 inhibitorNon-inhibitor0.9135
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8825
Ames testNon AMES toxic0.618
CarcinogenicityNon-carcinogens0.6862
BiodegradationNot ready biodegradable0.9972
Rat acute toxicity2.8555 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8927
hERG inhibition (predictor II)Non-inhibitor0.9652
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Sandoz inc
  • Teva pharmaceuticals usa
  • Watson laboratories inc
  • Wyeth ayerst laboratories
Packagers
Dosage formsNot Available
Prices
Unit descriptionCostUnit
Guanabenz acetate 8 mg tablet2.13USD tablet
Guanabenz acetate 4 mg tablet1.07USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point225-227British Patent 1,019,120.
logP3.2Not Available
Caco2 permeability-4.5ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.0889 mg/mLALOGPS
logP2.25ALOGPS
logP1.71ChemAxon
logS-3.4ALOGPS
pKa (Strongest Basic)6.82ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area76.76 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity58.15 m3·mol-1ChemAxon
Polarizability21.58 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

British Patent 1,019,120.

General ReferencesNot Available
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (219 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypotensive activities of Guanabenz.
AbirateroneThe serum concentration of Guanabenz can be increased when it is combined with Abiraterone.
AcebutololGuanabenz may increase the hypotensive activities of Acebutolol.
AlfuzosinAlfuzosin may increase the hypotensive activities of Guanabenz.
AliskirenGuanabenz may increase the hypotensive activities of Aliskiren.
AlprenololGuanabenz may increase the hypotensive activities of Alprenolol.
AmbrisentanGuanabenz may increase the hypotensive activities of Ambrisentan.
AmifostineGuanabenz may increase the hypotensive activities of Amifostine.
AmineptineThe therapeutic efficacy of Guanabenz can be decreased when used in combination with Amineptine.
AmitriptylineThe therapeutic efficacy of Guanabenz can be decreased when used in combination with Amitriptyline.
AmlodipineAmlodipine may increase the hypotensive activities of Guanabenz.
ArotinololGuanabenz may increase the atrioventricular blocking (AV block) activities of Arotinolol.
AtenololAtenolol may increase the hypotensive activities of Guanabenz.
AzithromycinThe metabolism of Guanabenz can be decreased when combined with Azithromycin.
BefunololGuanabenz may increase the atrioventricular blocking (AV block) activities of Befunolol.
BenazeprilBenazepril may increase the hypotensive activities of Guanabenz.
BendroflumethiazideBendroflumethiazide may increase the hypotensive activities of Guanabenz.
BenmoxinBenmoxin may increase the hypotensive activities of Guanabenz.
BepridilGuanabenz may increase the hypotensive activities of Bepridil.
BetaxololBetaxolol may increase the hypotensive activities of Guanabenz.
BethanidineBethanidine may increase the hypotensive activities of Guanabenz.
BevantololGuanabenz may increase the atrioventricular blocking (AV block) activities of Bevantolol.
BimatoprostGuanabenz may increase the hypotensive activities of Bimatoprost.
BisoprololBisoprolol may increase the hypotensive activities of Guanabenz.
BopindololGuanabenz may increase the atrioventricular blocking (AV block) activities of Bopindolol.
BortezomibThe metabolism of Guanabenz can be decreased when combined with Bortezomib.
BosentanBosentan may increase the hypotensive activities of Guanabenz.
BretyliumGuanabenz may increase the hypotensive activities of Bretylium.
BrimonidineGuanabenz may increase the hypotensive activities of Brimonidine.
BrimonidineBrimonidine may increase the antihypertensive activities of Guanabenz.
BufuralolGuanabenz may increase the atrioventricular blocking (AV block) activities of Bufuralol.
BupranololGuanabenz may increase the hypotensive activities of Bupranolol.
CaffeineThe metabolism of Guanabenz can be decreased when combined with Caffeine.
CandesartanGuanabenz may increase the hypotensive activities of Candesartan.
CandoxatrilCandoxatril may increase the hypotensive activities of Guanabenz.
CaptoprilGuanabenz may increase the hypotensive activities of Captopril.
CarbamazepineThe metabolism of Guanabenz can be increased when combined with Carbamazepine.
CaroxazoneCaroxazone may increase the hypotensive activities of Guanabenz.
CarteololCarteolol may increase the hypotensive activities of Guanabenz.
CarvedilolGuanabenz may increase the hypotensive activities of Carvedilol.
CeliprololGuanabenz may increase the hypotensive activities of Celiprolol.
ChlorothiazideGuanabenz may increase the hypotensive activities of Chlorothiazide.
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Guanabenz.
CilazaprilGuanabenz may increase the hypotensive activities of Cilazapril.
CitalopramThe metabolism of Guanabenz can be decreased when combined with Citalopram.
ClomipramineThe therapeutic efficacy of Guanabenz can be decreased when used in combination with Clomipramine.
ClonidineClonidine may increase the hypotensive activities of Guanabenz.
ClotrimazoleThe metabolism of Guanabenz can be decreased when combined with Clotrimazole.
CryptenamineGuanabenz may increase the hypotensive activities of Cryptenamine.
CyclobenzaprineThe therapeutic efficacy of Guanabenz can be decreased when used in combination with Cyclobenzaprine.
CyclothiazideCyclothiazide may increase the hypotensive activities of Guanabenz.
Cyproterone acetateThe serum concentration of Guanabenz can be decreased when it is combined with Cyproterone acetate.
DebrisoquinGuanabenz may increase the hypotensive activities of Debrisoquin.
DeferasiroxThe serum concentration of Guanabenz can be increased when it is combined with Deferasirox.
DeserpidineGuanabenz may increase the hypotensive activities of Deserpidine.
DesipramineThe therapeutic efficacy of Guanabenz can be decreased when used in combination with Desipramine.
DesvenlafaxineDesvenlafaxine may decrease the antihypertensive activities of Guanabenz.
DiazoxideDiazoxide may increase the hypotensive activities of Guanabenz.
DiltiazemDiltiazem may increase the hypotensive activities of Guanabenz.
DorzolamideGuanabenz may increase the hypotensive activities of Dorzolamide.
DosulepinThe therapeutic efficacy of Guanabenz can be decreased when used in combination with Dosulepin.
DoxazosinDoxazosin may increase the hypotensive activities of Guanabenz.
DoxepinThe therapeutic efficacy of Guanabenz can be decreased when used in combination with Doxepin.
DuloxetineDuloxetine may decrease the antihypertensive activities of Guanabenz.
EfonidipineGuanabenz may increase the hypotensive activities of Efonidipine.
EnalaprilEnalapril may increase the hypotensive activities of Guanabenz.
EnalaprilatGuanabenz may increase the hypotensive activities of Enalaprilat.
EpoprostenolGuanabenz may increase the hypotensive activities of Epoprostenol.
EprosartanGuanabenz may increase the hypotensive activities of Eprosartan.
EsmirtazapineThe therapeutic efficacy of Guanabenz can be decreased when used in combination with Esmirtazapine.
EsmololGuanabenz may increase the atrioventricular blocking (AV block) activities of Esmolol.
FelodipineGuanabenz may increase the hypotensive activities of Felodipine.
FenoldopamGuanabenz may increase the hypotensive activities of Fenoldopam.
FluvoxamineThe metabolism of Guanabenz can be decreased when combined with Fluvoxamine.
FosinoprilFosinopril may increase the hypotensive activities of Guanabenz.
FurazolidoneFurazolidone may increase the hypotensive activities of Guanabenz.
GuanadrelGuanadrel may increase the hypotensive activities of Guanabenz.
GuanethidineGuanabenz may increase the hypotensive activities of Guanethidine.
GuanfacineGuanabenz may increase the hypotensive activities of Guanfacine.
HexamethoniumGuanabenz may increase the hypotensive activities of Hexamethonium.
HydracarbazineHydracarbazine may increase the hypotensive activities of Guanabenz.
HydralazineGuanabenz may increase the hypotensive activities of Hydralazine.
HydrochlorothiazideGuanabenz may increase the hypotensive activities of Hydrochlorothiazide.
HydroflumethiazideGuanabenz may increase the hypotensive activities of Hydroflumethiazide.
IloprostIloprost may increase the hypotensive activities of Guanabenz.
ImipramineThe therapeutic efficacy of Guanabenz can be decreased when used in combination with Imipramine.
IndapamideGuanabenz may increase the hypotensive activities of Indapamide.
IndenololGuanabenz may increase the hypotensive activities of Indenolol.
IndoraminGuanabenz may increase the hypotensive activities of Indoramin.
IproclozideIproclozide may increase the hypotensive activities of Guanabenz.
IproniazidIproniazid may increase the hypotensive activities of Guanabenz.
IrbesartanGuanabenz may increase the hypotensive activities of Irbesartan.
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Guanabenz.
IsradipineIsradipine may increase the hypotensive activities of Guanabenz.
LabetalolLabetalol may increase the hypotensive activities of Guanabenz.
LacidipineGuanabenz may increase the hypotensive activities of Lacidipine.
LatanoprostGuanabenz may increase the hypotensive activities of Latanoprost.
LercanidipineLercanidipine may increase the hypotensive activities of Guanabenz.
LevomilnacipranLevomilnacipran may decrease the antihypertensive activities of Guanabenz.
LidocaineThe metabolism of Guanabenz can be decreased when combined with Lidocaine.
LisinoprilGuanabenz may increase the hypotensive activities of Lisinopril.
LofexidineGuanabenz may increase the hypotensive activities of Lofexidine.
LosartanGuanabenz may increase the hypotensive activities of Losartan.
MacitentanGuanabenz may increase the hypotensive activities of Macitentan.
ManidipineGuanabenz may increase the hypotensive activities of Manidipine.
MebanazineMebanazine may increase the hypotensive activities of Guanabenz.
MecamylamineGuanabenz may increase the hypotensive activities of Mecamylamine.
MethyldopaGuanabenz may increase the hypotensive activities of Methyldopa.
Methylene blueMethylene blue may increase the hypotensive activities of Guanabenz.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Guanabenz.
MetipranololGuanabenz may increase the hypotensive activities of Metipranolol.
MetolazoneMetolazone may increase the hypotensive activities of Guanabenz.
MetoprololMetoprolol may increase the hypotensive activities of Guanabenz.
MexiletineThe metabolism of Guanabenz can be decreased when combined with Mexiletine.
MianserinThe therapeutic efficacy of Guanabenz can be decreased when used in combination with Mianserin.
MibefradilGuanabenz may increase the hypotensive activities of Mibefradil.
MilnacipranMilnacipran may decrease the antihypertensive activities of Guanabenz.
MinaprineMinaprine may increase the hypotensive activities of Guanabenz.
MinoxidilMinoxidil may increase the hypotensive activities of Guanabenz.
MirtazapineThe therapeutic efficacy of Guanabenz can be decreased when used in combination with Mirtazapine.
MoclobemideMoclobemide may increase the hypotensive activities of Guanabenz.
MoexiprilGuanabenz may increase the hypotensive activities of Moexipril.
MolsidomineMolsidomine may increase the hypotensive activities of Guanabenz.
MoxonidineGuanabenz may increase the hypotensive activities of Moxonidine.
NadololGuanabenz may increase the hypotensive activities of Nadolol.
NebivololGuanabenz may increase the hypotensive activities of Nebivolol.
NevirapineThe metabolism of Guanabenz can be decreased when combined with Nevirapine.
NialamideNialamide may increase the hypotensive activities of Guanabenz.
NicardipineNicardipine may increase the hypotensive activities of Guanabenz.
NicorandilGuanabenz may increase the hypotensive activities of Nicorandil.
NiguldipineGuanabenz may increase the hypotensive activities of Niguldipine.
NilvadipineGuanabenz may increase the hypotensive activities of Nilvadipine.
NimodipineNimodipine may increase the hypotensive activities of Guanabenz.
NisoldipineNisoldipine may increase the hypotensive activities of Guanabenz.
NitrendipineGuanabenz may increase the hypotensive activities of Nitrendipine.
NitroprussideNitroprusside may increase the hypotensive activities of Guanabenz.
NortriptylineThe therapeutic efficacy of Guanabenz can be decreased when used in combination with Nortriptyline.
ObinutuzumabGuanabenz may increase the hypotensive activities of Obinutuzumab.
OctamoxinOctamoxin may increase the hypotensive activities of Guanabenz.
OlmesartanOlmesartan may increase the hypotensive activities of Guanabenz.
OmapatrilatGuanabenz may increase the hypotensive activities of Omapatrilat.
OsimertinibThe serum concentration of Guanabenz can be decreased when it is combined with Osimertinib.
OxprenololGuanabenz may increase the hypotensive activities of Oxprenolol.
PargylineGuanabenz may increase the hypotensive activities of Pargyline.
Peginterferon alfa-2bThe serum concentration of Guanabenz can be increased when it is combined with Peginterferon alfa-2b.
PenbutololGuanabenz may increase the hypotensive activities of Penbutolol.
PentoliniumGuanabenz may increase the hypotensive activities of Pentolinium.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Guanabenz.
PerindoprilGuanabenz may increase the hypotensive activities of Perindopril.
PhenelzinePhenelzine may increase the hypotensive activities of Guanabenz.
PheniprazinePheniprazine may increase the hypotensive activities of Guanabenz.
PhenobarbitalThe metabolism of Guanabenz can be increased when combined with Phenobarbital.
PhenoxybenzamineGuanabenz may increase the hypotensive activities of Phenoxybenzamine.
PhenoxypropazinePhenoxypropazine may increase the hypotensive activities of Guanabenz.
PhentolamineGuanabenz may increase the hypotensive activities of Phentolamine.
PinacidilGuanabenz may increase the hypotensive activities of Pinacidil.
PindololGuanabenz may increase the hypotensive activities of Pindolol.
PirlindolePirlindole may increase the hypotensive activities of Guanabenz.
PivhydrazinePivhydrazine may increase the hypotensive activities of Guanabenz.
PolythiazideGuanabenz may increase the hypotensive activities of Polythiazide.
PractololGuanabenz may increase the atrioventricular blocking (AV block) activities of Practolol.
PrazosinPrazosin may increase the hypotensive activities of Guanabenz.
PrimidoneThe metabolism of Guanabenz can be increased when combined with Primidone.
PropranololPropranolol may increase the hypotensive activities of Guanabenz.
ProtriptylineThe therapeutic efficacy of Guanabenz can be decreased when used in combination with Protriptyline.
QuinaprilGuanabenz may increase the hypotensive activities of Quinapril.
QuinineQuinine may increase the hypotensive activities of Guanabenz.
RamiprilRamipril may increase the hypotensive activities of Guanabenz.
RasagilineRasagiline may increase the hypotensive activities of Guanabenz.
RemikirenRemikiren may increase the hypotensive activities of Guanabenz.
RescinnamineGuanabenz may increase the hypotensive activities of Rescinnamine.
ReserpineReserpine may increase the hypotensive activities of Guanabenz.
RifampicinThe metabolism of Guanabenz can be increased when combined with Rifampicin.
RiociguatGuanabenz may increase the hypotensive activities of Riociguat.
RituximabGuanabenz may increase the hypotensive activities of Rituximab.
RopiniroleThe metabolism of Guanabenz can be decreased when combined with Ropinirole.
SafrazineSafrazine may increase the hypotensive activities of Guanabenz.
SaprisartanGuanabenz may increase the hypotensive activities of Saprisartan.
SelegilineSelegiline may increase the hypotensive activities of Guanabenz.
SelexipagGuanabenz may increase the hypotensive activities of Selexipag.
SildenafilSildenafil may increase the antihypertensive activities of Guanabenz.
SimeprevirThe metabolism of Guanabenz can be decreased when combined with Simeprevir.
SitaxentanGuanabenz may increase the hypotensive activities of Sitaxentan.
SotalolGuanabenz may increase the atrioventricular blocking (AV block) activities of Sotalol.
SpiraprilGuanabenz may increase the hypotensive activities of Spirapril.
TadalafilTadalafil may increase the antihypertensive activities of Guanabenz.
TelmisartanGuanabenz may increase the hypotensive activities of Telmisartan.
TemocaprilGuanabenz may increase the hypotensive activities of Temocapril.
TenofovirThe metabolism of Guanabenz can be decreased when combined with Tenofovir.
TeriflunomideThe serum concentration of Guanabenz can be decreased when it is combined with Teriflunomide.
TerlipressinGuanabenz may increase the hypotensive activities of Terlipressin.
TheophyllineThe metabolism of Guanabenz can be decreased when combined with Theophylline.
TianeptineThe therapeutic efficacy of Guanabenz can be decreased when used in combination with Tianeptine.
TiboloneGuanabenz may increase the hypotensive activities of Tibolone.
TiclopidineThe metabolism of Guanabenz can be decreased when combined with Ticlopidine.
TicrynafenGuanabenz may increase the hypotensive activities of Ticrynafen.
TimololTimolol may increase the hypotensive activities of Guanabenz.
TolazolineGuanabenz may increase the hypotensive activities of Tolazoline.
ToloxatoneToloxatone may increase the hypotensive activities of Guanabenz.
TorasemideTorasemide may increase the hypotensive activities of Guanabenz.
TrandolaprilTrandolapril may increase the hypotensive activities of Guanabenz.
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Guanabenz.
TranylcypromineTranylcypromine may increase the hypotensive activities of Guanabenz.
TravoprostTravoprost may increase the hypotensive activities of Guanabenz.
TreprostinilTreprostinil may increase the hypotensive activities of Guanabenz.
TrichlormethiazideGuanabenz may increase the hypotensive activities of Trichlormethiazide.
TrimazosinGuanabenz may increase the hypotensive activities of Trimazosin.
TrimethaphanGuanabenz may increase the hypotensive activities of Trimethaphan.
TrimipramineThe therapeutic efficacy of Guanabenz can be decreased when used in combination with Trimipramine.
UdenafilUdenafil may increase the antihypertensive activities of Guanabenz.
UnoprostoneGuanabenz may increase the hypotensive activities of Unoprostone.
ValsartanValsartan may increase the hypotensive activities of Guanabenz.
VardenafilVardenafil may increase the antihypertensive activities of Guanabenz.
VemurafenibThe serum concentration of Guanabenz can be increased when it is combined with Vemurafenib.
VenlafaxineVenlafaxine may decrease the antihypertensive activities of Guanabenz.
XylometazolineGuanabenz may increase the hypotensive activities of Xylometazoline.
YohimbineYohimbine may decrease the antihypertensive activities of Guanabenz.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 Da
References
  1. Piletz JE, Sletten K: Nonadrenergic imidazoline binding sites on human platelets. J Pharmacol Exp Ther. 1993 Dec;267(3):1493-502. [PubMed:8263811 ]
  2. Bockman CS, Jeffries WB, Abel PW: Binding and functional characterization of alpha-2 adrenergic receptor subtypes on pig vascular endothelium. J Pharmacol Exp Ther. 1993 Dec;267(3):1126-33. [PubMed:7903385 ]
  3. Bockman CS, Gonzalez-Cabrera I, Abel PW: Alpha-2 adrenoceptor subtype causing nitric oxide-mediated vascular relaxation in rats. J Pharmacol Exp Ther. 1996 Sep;278(3):1235-43. [PubMed:8819507 ]
  4. Galeotti N, Bartolini A, Ghelardini C: Alpha-2 agonist-induced memory impairment is mediated by the alpha-2A-adrenoceptor subtype. Behav Brain Res. 2004 Aug 31;153(2):409-17. [PubMed:15265636 ]
  5. van Zwieten PA: Centrally acting antihypertensives: a renaissance of interest. Mechanisms and haemodynamics. J Hypertens Suppl. 1997 Jan;15(1):S3-8. [PubMed:9050980 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Epinephrine binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phent...
Gene Name:
ADRA2B
Uniprot ID:
P18089
Molecular Weight:
49565.8 Da
References
  1. Uhlen S, Wikberg JE: Delineation of rat kidney alpha 2A- and alpha 2B-adrenoceptors with [3H]RX821002 radioligand binding: computer modelling reveals that guanfacine is an alpha 2A-selective compound. Eur J Pharmacol. 1991 Sep 17;202(2):235-43. [PubMed:1666366 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Wang B, Zhou SF: Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218. [PubMed:19754423 ]
  2. Clement B, Demesmaeker M: Formation of guanoxabenz from guanabenz in human liver. A new metabolic marker for CYP1A2. Drug Metab Dispos. 1997 Nov;25(11):1266-71. [PubMed:9351903 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23