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Identification
NameTolazoline
Accession NumberDB00797  (APRD00170)
TypeSmall Molecule
GroupsApproved, Vet Approved
DescriptionA vasodilator that apparently has direct actions on blood vessels and also increases cardiac output. Tolazoline can interact to some degree with histamine, adrenergic, and cholinergic receptors, but the mechanisms of its therapeutic effects are not clear. It is used in treatment of persistent pulmonary hypertension of the newborn. [PubChem]
Structure
Thumb
Synonyms
2-Benzyl-2-imidazoline
2-Benzyl-4,5-imidazoline
2-Benzylimidazoline
4,5-Dihydro-2-(phenylmethyl)-1H-imidazole
Benzazolin
Tolazolin
Tolazolina
Tolazoline
Tolazolinum
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
DivascolVUAB Pharma
ImidalinAstellas Pharma
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Benzazoline hydrochloride
ThumbNot applicableDBSALT000947
Tolazoline Hydrochloride
59-97-2
Thumb
  • InChI Key: RHTNTTODYGNRSP-UHFFFAOYSA-N
  • Monoisotopic Mass: 196.0767261
  • Average Mass: 196.68
DBSALT000948
Categories
UNIICHH9H12AQ3
CAS number59-98-3
WeightAverage: 160.2157
Monoisotopic: 160.100048394
Chemical FormulaC10H12N2
InChI KeyJIVZKJJQOZQXQB-UHFFFAOYSA-N
InChI
InChI=1S/C10H12N2/c1-2-4-9(5-3-1)8-10-11-6-7-12-10/h1-5H,6-8H2,(H,11,12)
IUPAC Name
2-benzyl-4,5-dihydro-1H-imidazole
SMILES
C(C1=NCCN1)C1=CC=CC=C1
Pharmacology
IndicationFor the treatment of pulmonary artery anomalies
Structured Indications Not Available
PharmacodynamicsTolazoline is a pulmonary vasodilator indicated used to decrease pulmonary vascular resistance (PVR) in persistent pulmonary hypertension of the newborn (PPHN).
Mechanism of actionVasodilation by means of a direct effect on peripheral vascular smooth muscle and indirect effects produced, in part, by release of endogenous histamine; tolazoline has moderate alpha-adrenergic blocking activity and has histamine agonist activity. Tolazoline usually reduces pulmonary arterial pressure and vascular resistance.
TargetKindPharmacological actionActionsOrganismUniProt ID
Alpha-1A adrenergic receptorProteinyes
antagonist
HumanP35348 details
Alpha-2A adrenergic receptorProteinunknown
antagonist
HumanP08913 details
Histamine H1 receptorProteinunknown
agonist
HumanP35367 details
Histamine H2 receptorProteinunknown
agonist
HumanP25021 details
Alpha-2C adrenergic receptorProteinunknown
binder
HumanP18825 details
Alpha-2B adrenergic receptorProteinunknown
binder
HumanP18089 details
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
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypotensive activities of Tolazoline.Experimental
AcebutololTolazoline may increase the hypotensive activities of Acebutolol.Approved
AcetazolamideThe risk or severity of adverse effects can be increased when Tolazoline is combined with Acetazolamide.Approved, Vet Approved
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Tolazoline.Approved
AlfuzosinAlfuzosin may increase the hypotensive activities of Tolazoline.Approved, Investigational
AliskirenTolazoline may increase the hypotensive activities of Aliskiren.Approved, Investigational
AlprenololTolazoline may increase the hypotensive activities of Alprenolol.Approved, Withdrawn
AmbrisentanTolazoline may increase the hypotensive activities of Ambrisentan.Approved, Investigational
AmifostineTolazoline may increase the hypotensive activities of Amifostine.Approved, Investigational
AmilorideThe risk or severity of adverse effects can be increased when Amiloride is combined with Tolazoline.Approved
AmiodaroneThe risk or severity of adverse effects can be increased when Amiodarone is combined with Tolazoline.Approved, Investigational
AmlodipineAmlodipine may increase the hypotensive activities of Tolazoline.Approved
AmobarbitalAmobarbital may increase the hypotensive activities of Tolazoline.Approved, Illicit
Amphotericin BThe risk or severity of adverse effects can be increased when Amphotericin B is combined with Tolazoline.Approved, Investigational
Amyl NitriteThe risk or severity of adverse effects can be increased when Amyl Nitrite is combined with Tolazoline.Approved
ApomorphineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Tolazoline.Approved, Investigational
ApraclonidineThe risk or severity of adverse effects can be increased when Apraclonidine is combined with Tolazoline.Approved
AripiprazoleAripiprazole may increase the hypotensive activities of Tolazoline.Approved, Investigational
ArotinololThe risk or severity of adverse effects can be increased when Arotinolol is combined with Tolazoline.Approved
Arsenic trioxideThe risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Tolazoline.Approved, Investigational
AtenololAtenolol may increase the hypotensive activities of Tolazoline.Approved
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Azilsartan medoxomil is combined with Tolazoline.Approved
BarbexacloneBarbexaclone may increase the hypotensive activities of Tolazoline.Experimental
BarbitalBarbital may increase the hypotensive activities of Tolazoline.Illicit
BarnidipineThe risk or severity of adverse effects can be increased when Barnidipine is combined with Tolazoline.Approved
BenazeprilBenazepril may increase the hypotensive activities of Tolazoline.Approved, Investigational
BendroflumethiazideBendroflumethiazide may increase the hypotensive activities of Tolazoline.Approved
BenmoxinBenmoxin may increase the hypotensive activities of Tolazoline.Withdrawn
BepridilTolazoline may increase the hypotensive activities of Bepridil.Approved, Withdrawn
BetaxololBetaxolol may increase the hypotensive activities of Tolazoline.Approved
BethanidineBethanidine may increase the hypotensive activities of Tolazoline.Approved
BimatoprostTolazoline may increase the hypotensive activities of Bimatoprost.Approved, Investigational
BisoprololBisoprolol may increase the hypotensive activities of Tolazoline.Approved
BortezomibThe risk or severity of adverse effects can be increased when Bortezomib is combined with Tolazoline.Approved, Investigational
BosentanBosentan may increase the hypotensive activities of Tolazoline.Approved, Investigational
BretyliumTolazoline may increase the hypotensive activities of Bretylium.Approved
BrimonidineBrimonidine may increase the hypotensive activities of Tolazoline.Approved
BrimonidineBrimonidine may increase the antihypertensive activities of Tolazoline.Approved
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Tolazoline.Approved, Investigational
BumetanideThe risk or severity of adverse effects can be increased when Bumetanide is combined with Tolazoline.Approved
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Tolazoline.Approved, Investigational
BupranololTolazoline may increase the hypotensive activities of Bupranolol.Approved
CanagliflozinThe risk or severity of adverse effects can be increased when Canagliflozin is combined with Tolazoline.Approved
CandesartanCandesartan may increase the hypotensive activities of Tolazoline.Approved
CandoxatrilCandoxatril may increase the hypotensive activities of Tolazoline.Experimental
CaptoprilTolazoline may increase the hypotensive activities of Captopril.Approved
CarbetocinThe risk or severity of adverse effects can be increased when Carbetocin is combined with Tolazoline.Approved
CaroxazoneCaroxazone may increase the hypotensive activities of Tolazoline.Withdrawn
CarteololCarteolol may increase the hypotensive activities of Tolazoline.Approved
CarvedilolTolazoline may increase the hypotensive activities of Carvedilol.Approved, Investigational
CeliprololTolazoline may increase the hypotensive activities of Celiprolol.Approved, Investigational
ChlorothiazideTolazoline may increase the hypotensive activities of Chlorothiazide.Approved, Vet Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Tolazoline.Approved, Vet Approved
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Tolazoline.Approved
CilazaprilTolazoline may increase the hypotensive activities of Cilazapril.Approved
CilnidipineThe risk or severity of adverse effects can be increased when Cilnidipine is combined with Tolazoline.Approved
ClevidipineThe risk or severity of adverse effects can be increased when Clevidipine is combined with Tolazoline.Approved
ClofarabineThe risk or severity of adverse effects can be increased when Clofarabine is combined with Tolazoline.Approved, Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Tolazoline.Approved, Vet Approved
ClonidineClonidine may increase the hypotensive activities of Tolazoline.Approved
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Tolazoline.Approved
ConivaptanThe risk or severity of adverse effects can be increased when Conivaptan is combined with Tolazoline.Approved, Investigational
CryptenamineCryptenamine may increase the hypotensive activities of Tolazoline.Approved
CyclothiazideCyclothiazide may increase the hypotensive activities of Tolazoline.Approved
DapagliflozinThe risk or severity of adverse effects can be increased when Dapagliflozin is combined with Tolazoline.Approved
DebrisoquinTolazoline may increase the hypotensive activities of Debrisoquin.Approved
DeserpidineTolazoline may increase the hypotensive activities of Deserpidine.Approved
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Tolazoline.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Tolazoline.Approved, Vet Approved
DiazoxideDiazoxide may increase the hypotensive activities of Tolazoline.Approved
DiclofenamideThe risk or severity of adverse effects can be increased when Diclofenamide is combined with Tolazoline.Approved
DihydralazineTolazoline may increase the hypotensive activities of Dihydralazine.Investigational
DiltiazemDiltiazem may increase the hypotensive activities of Tolazoline.Approved
DinutuximabThe risk or severity of adverse effects can be increased when Dinutuximab is combined with Tolazoline.Approved
DipyridamoleThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Tolazoline.Approved
DorzolamideTolazoline may increase the hypotensive activities of Dorzolamide.Approved
DoxazosinDoxazosin may increase the hypotensive activities of Tolazoline.Approved
DuloxetineTolazoline may increase the orthostatic hypotensive activities of Duloxetine.Approved
EfonidipineTolazoline may increase the hypotensive activities of Efonidipine.Approved
EmpagliflozinThe risk or severity of adverse effects can be increased when Empagliflozin is combined with Tolazoline.Approved
EnalaprilEnalapril may increase the hypotensive activities of Tolazoline.Approved, Vet Approved
EnalaprilatTolazoline may increase the hypotensive activities of Enalaprilat.Approved
EplerenoneThe risk or severity of adverse effects can be increased when Eplerenone is combined with Tolazoline.Approved
EpoprostenolTolazoline may increase the hypotensive activities of Epoprostenol.Approved
EprosartanTolazoline may increase the hypotensive activities of Eprosartan.Approved
EsmololThe risk or severity of adverse effects can be increased when Esmolol is combined with Tolazoline.Approved
Etacrynic acidThe risk or severity of adverse effects can be increased when Etacrynic acid is combined with Tolazoline.Approved
FelodipineTolazoline may increase the hypotensive activities of Felodipine.Approved, Investigational
FenoldopamTolazoline may increase the hypotensive activities of Fenoldopam.Approved
FimasartanThe risk or severity of adverse effects can be increased when Fimasartan is combined with Tolazoline.Approved
FosinoprilFosinopril may increase the hypotensive activities of Tolazoline.Approved
FurazolidoneFurazolidone may increase the hypotensive activities of Tolazoline.Approved, Vet Approved
FurosemideThe risk or severity of adverse effects can be increased when Furosemide is combined with Tolazoline.Approved, Vet Approved
GuanabenzGuanabenz may increase the hypotensive activities of Tolazoline.Approved
GuanadrelGuanadrel may increase the hypotensive activities of Tolazoline.Approved
GuanethidineTolazoline may increase the hypotensive activities of Guanethidine.Approved
GuanfacineTolazoline may increase the hypotensive activities of Guanfacine.Approved, Investigational
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Tolazoline.Approved, Vet Approved
HexamethoniumTolazoline may increase the hypotensive activities of Hexamethonium.Experimental
HexobarbitalHexobarbital may increase the hypotensive activities of Tolazoline.Approved
HydracarbazineHydracarbazine may increase the hypotensive activities of Tolazoline.Approved
HydralazineTolazoline may increase the hypotensive activities of Hydralazine.Approved
HydrochlorothiazideTolazoline may increase the hypotensive activities of Hydrochlorothiazide.Approved, Vet Approved
HydroflumethiazideHydroflumethiazide may increase the hypotensive activities of Tolazoline.Approved
IloprostIloprost may increase the hypotensive activities of Tolazoline.Approved, Investigational
ImidaprilThe risk or severity of adverse effects can be increased when Imidapril is combined with Tolazoline.Investigational
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Tolazoline.Approved
IndapamideTolazoline may increase the hypotensive activities of Indapamide.Approved
IndenololTolazoline may increase the hypotensive activities of Indenolol.Withdrawn
IndoraminTolazoline may increase the hypotensive activities of Indoramin.Withdrawn
IproclozideIproclozide may increase the hypotensive activities of Tolazoline.Withdrawn
IproniazidIproniazid may increase the hypotensive activities of Tolazoline.Withdrawn
IrbesartanTolazoline may increase the hypotensive activities of Irbesartan.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Tolazoline.Approved
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Tolazoline.Approved, Vet Approved
Isosorbide DinitrateThe risk or severity of adverse effects can be increased when Isosorbide Dinitrate is combined with Tolazoline.Approved
Isosorbide MononitrateThe risk or severity of adverse effects can be increased when Isosorbide Mononitrate is combined with Tolazoline.Approved
IsoxsuprineThe risk or severity of adverse effects can be increased when Isoxsuprine is combined with Tolazoline.Approved, Withdrawn
IsradipineIsradipine may increase the hypotensive activities of Tolazoline.Approved
KetanserinTolazoline may increase the hypotensive activities of Ketanserin.Investigational
LabetalolLabetalol may increase the hypotensive activities of Tolazoline.Approved
LacidipineTolazoline may increase the hypotensive activities of Lacidipine.Approved
LatanoprostLatanoprost may increase the hypotensive activities of Tolazoline.Approved, Investigational
LercanidipineLercanidipine may increase the hypotensive activities of Tolazoline.Approved, Investigational
LevobunololThe risk or severity of adverse effects can be increased when Levobunolol is combined with Tolazoline.Approved
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Tolazoline.Approved
LevodopaTolazoline may increase the orthostatic hypotensive activities of Levodopa.Approved
LevosimendanThe risk or severity of adverse effects can be increased when Levosimendan is combined with Tolazoline.Approved, Investigational
LisinoprilLisinopril may increase the hypotensive activities of Tolazoline.Approved, Investigational
LofexidineTolazoline may increase the hypotensive activities of Lofexidine.Approved, Investigational
LosartanLosartan may increase the hypotensive activities of Tolazoline.Approved
MacitentanTolazoline may increase the hypotensive activities of Macitentan.Approved
ManidipineTolazoline may increase the hypotensive activities of Manidipine.Approved
MannitolThe risk or severity of adverse effects can be increased when Mannitol is combined with Tolazoline.Approved, Investigational
MebanazineMebanazine may increase the hypotensive activities of Tolazoline.Withdrawn
MecamylamineMecamylamine may increase the hypotensive activities of Tolazoline.Approved
MethazolamideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Tolazoline.Approved
MethohexitalMethohexital may increase the hypotensive activities of Tolazoline.Approved
MethyclothiazideThe risk or severity of adverse effects can be increased when Methyclothiazide is combined with Tolazoline.Approved
MethyldopaTolazoline may increase the hypotensive activities of Methyldopa.Approved
Methylene blueMethylene blue may increase the hypotensive activities of Tolazoline.Investigational
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Tolazoline.Approved, Investigational
MethylphenobarbitalMethylphenobarbital may increase the hypotensive activities of Tolazoline.Approved
MetipranololTolazoline may increase the hypotensive activities of Metipranolol.Approved
MetolazoneMetolazone may increase the hypotensive activities of Tolazoline.Approved
MetoprololMetoprolol may increase the hypotensive activities of Tolazoline.Approved, Investigational
MetyrosineTolazoline may increase the hypotensive activities of Metyrosine.Approved
MibefradilTolazoline may increase the hypotensive activities of Mibefradil.Withdrawn
MinaprineMinaprine may increase the hypotensive activities of Tolazoline.Approved
MinoxidilMinoxidil may increase the hypotensive activities of Tolazoline.Approved
MoclobemideMoclobemide may increase the hypotensive activities of Tolazoline.Approved
MoexiprilMoexipril may increase the hypotensive activities of Tolazoline.Approved
MolsidomineMolsidomine may increase the hypotensive activities of Tolazoline.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Tolazoline.Approved, Investigational
MoxonidineTolazoline may increase the hypotensive activities of Moxonidine.Approved
NabiloneThe risk or severity of adverse effects can be increased when Nabilone is combined with Tolazoline.Approved, Investigational
NadololTolazoline may increase the hypotensive activities of Nadolol.Approved
NaftopidilTolazoline may increase the hypotensive activities of Naftopidil.Investigational
NebivololTolazoline may increase the hypotensive activities of Nebivolol.Approved, Investigational
NesiritideThe risk or severity of adverse effects can be increased when Nesiritide is combined with Tolazoline.Approved, Investigational
NialamideNialamide may increase the hypotensive activities of Tolazoline.Withdrawn
NicardipineNicardipine may increase the hypotensive activities of Tolazoline.Approved
NicorandilNicorandil may increase the hypotensive activities of Tolazoline.Approved
NifedipineThe risk or severity of adverse effects can be increased when Nifedipine is combined with Tolazoline.Approved
NiguldipineTolazoline may increase the hypotensive activities of Niguldipine.Experimental
NilvadipineTolazoline may increase the hypotensive activities of Nilvadipine.Approved
NimodipineNimodipine may increase the hypotensive activities of Tolazoline.Approved
NisoldipineNisoldipine may increase the hypotensive activities of Tolazoline.Approved
NitrendipineTolazoline may increase the hypotensive activities of Nitrendipine.Approved
Nitric OxideThe risk or severity of adverse effects can be increased when Nitric Oxide is combined with Tolazoline.Approved
NitroglycerinThe risk or severity of adverse effects can be increased when Nitroglycerin is combined with Tolazoline.Approved, Investigational
NitroprussideNitroprusside may increase the hypotensive activities of Tolazoline.Approved
ObinutuzumabTolazoline may increase the hypotensive activities of Obinutuzumab.Approved
OctamoxinOctamoxin may increase the hypotensive activities of Tolazoline.Withdrawn
OlmesartanOlmesartan may increase the hypotensive activities of Tolazoline.Approved, Investigational
OmapatrilatTolazoline may increase the hypotensive activities of Omapatrilat.Investigational
OxprenololTolazoline may increase the hypotensive activities of Oxprenolol.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Tolazoline.Approved, Vet Approved
PapaverineThe risk or severity of adverse effects can be increased when Papaverine is combined with Tolazoline.Approved
PargylinePargyline may increase the hypotensive activities of Tolazoline.Approved
PenbutololTolazoline may increase the hypotensive activities of Penbutolol.Approved, Investigational
PentobarbitalPentobarbital may increase the hypotensive activities of Tolazoline.Approved, Vet Approved
PentoliniumTolazoline may increase the hypotensive activities of Pentolinium.Approved
PentoxifyllinePentoxifylline may increase the hypotensive activities of Tolazoline.Approved, Investigational
PerindoprilPerindopril may increase the hypotensive activities of Tolazoline.Approved
PhenelzinePhenelzine may increase the hypotensive activities of Tolazoline.Approved
PheniprazinePheniprazine may increase the hypotensive activities of Tolazoline.Withdrawn
PhenobarbitalPhenobarbital may increase the hypotensive activities of Tolazoline.Approved
PhenoxybenzamineTolazoline may increase the hypotensive activities of Phenoxybenzamine.Approved
PhenoxypropazinePhenoxypropazine may increase the hypotensive activities of Tolazoline.Withdrawn
PhentolaminePhentolamine may increase the hypotensive activities of Tolazoline.Approved
PinacidilTolazoline may increase the hypotensive activities of Pinacidil.Withdrawn
PindololTolazoline may increase the hypotensive activities of Pindolol.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Pipamperone is combined with Tolazoline.Approved
PirlindolePirlindole may increase the hypotensive activities of Tolazoline.Approved
PivhydrazinePivhydrazine may increase the hypotensive activities of Tolazoline.Withdrawn
PolythiazideTolazoline may increase the hypotensive activities of Polythiazide.Approved
PramipexoleThe risk or severity of adverse effects can be increased when Pramipexole is combined with Tolazoline.Approved, Investigational
PrazosinPrazosin may increase the hypotensive activities of Tolazoline.Approved
PrimidonePrimidone may increase the hypotensive activities of Tolazoline.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Tolazoline.Approved, Investigational, Vet Approved
PropranololPropranolol may increase the hypotensive activities of Tolazoline.Approved, Investigational
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Tolazoline.Approved
QuinaprilTolazoline may increase the hypotensive activities of Quinapril.Approved, Investigational
QuinineQuinine may increase the hypotensive activities of Tolazoline.Approved
RamiprilRamipril may increase the hypotensive activities of Tolazoline.Approved
RasagilineRasagiline may increase the hypotensive activities of Tolazoline.Approved
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Tolazoline.Approved
RemikirenRemikiren may increase the hypotensive activities of Tolazoline.Approved
RescinnamineTolazoline may increase the hypotensive activities of Rescinnamine.Approved
ReserpineReserpine may increase the hypotensive activities of Tolazoline.Approved
RilmenidineTolazoline may increase the hypotensive activities of Rilmenidine.Investigational
RiociguatTolazoline may increase the hypotensive activities of Riociguat.Approved
RisperidoneTolazoline may increase the hypotensive activities of Risperidone.Approved, Investigational
RituximabTolazoline may increase the hypotensive activities of Rituximab.Approved
RopiniroleThe risk or severity of adverse effects can be increased when Ropinirole is combined with Tolazoline.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Tolazoline.Approved
RotigotineThe risk or severity of adverse effects can be increased when Rotigotine is combined with Tolazoline.Approved
SacubitrilThe risk or severity of adverse effects can be increased when Sacubitril is combined with Tolazoline.Approved
SafrazineSafrazine may increase the hypotensive activities of Tolazoline.Withdrawn
SaprisartanTolazoline may increase the hypotensive activities of Saprisartan.Experimental
SecobarbitalSecobarbital may increase the hypotensive activities of Tolazoline.Approved, Vet Approved
SelegilineSelegiline may increase the hypotensive activities of Tolazoline.Approved, Investigational, Vet Approved
SelexipagTolazoline may increase the hypotensive activities of Selexipag.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Tolazoline.Approved, Vet Approved
SildenafilSildenafil may increase the antihypertensive activities of Tolazoline.Approved, Investigational
SitaxentanTolazoline may increase the hypotensive activities of Sitaxentan.Approved, Investigational, Withdrawn
Sodium NitriteThe risk or severity of adverse effects can be increased when Sodium Nitrite is combined with Tolazoline.Approved
SotalolThe risk or severity of adverse effects can be increased when Sotalol is combined with Tolazoline.Approved
SpiraprilTolazoline may increase the hypotensive activities of Spirapril.Approved
SpironolactoneThe risk or severity of adverse effects can be increased when Spironolactone is combined with Tolazoline.Approved
StreptokinaseThe risk or severity of adverse effects can be increased when Streptokinase is combined with Tolazoline.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Tolazoline.Approved, Investigational
TadalafilTadalafil may increase the antihypertensive activities of Tolazoline.Approved, Investigational
TamsulosinThe risk or severity of adverse effects can be increased when Tamsulosin is combined with Tolazoline.Approved, Investigational
TelmisartanTolazoline may increase the hypotensive activities of Telmisartan.Approved, Investigational
TemocaprilTolazoline may increase the hypotensive activities of Temocapril.Experimental, Investigational
TerazosinThe risk or severity of adverse effects can be increased when Terazosin is combined with Tolazoline.Approved
TerlipressinTolazoline may increase the hypotensive activities of Terlipressin.Approved, Investigational
ThalidomideThe risk or severity of adverse effects can be increased when Thalidomide is combined with Tolazoline.Approved, Investigational, Withdrawn
ThiamylalThiamylal may increase the hypotensive activities of Tolazoline.Approved, Vet Approved
ThiopentalThiopental may increase the hypotensive activities of Tolazoline.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Tolazoline.Approved
TiboloneTolazoline may increase the hypotensive activities of Tibolone.Approved
TicrynafenTolazoline may increase the hypotensive activities of Ticrynafen.Withdrawn
TimololTimolol may increase the hypotensive activities of Tolazoline.Approved
TizanidineThe risk or severity of adverse effects can be increased when Tizanidine is combined with Tolazoline.Approved
TolcaponeThe risk or severity of adverse effects can be increased when Tolazoline is combined with Tolcapone.Approved, Withdrawn
ToloxatoneToloxatone may increase the hypotensive activities of Tolazoline.Approved
TorasemideTorasemide may increase the hypotensive activities of Tolazoline.Approved
TrandolaprilTrandolapril may increase the hypotensive activities of Tolazoline.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Tolazoline.Experimental
TranylcypromineTranylcypromine may increase the hypotensive activities of Tolazoline.Approved
TravoprostTravoprost may increase the hypotensive activities of Tolazoline.Approved
TreprostinilTreprostinil may increase the hypotensive activities of Tolazoline.Approved, Investigational
TretinoinThe risk or severity of adverse effects can be increased when Tolazoline is combined with Tretinoin.Approved, Investigational, Nutraceutical
TriamtereneThe risk or severity of adverse effects can be increased when Triamterene is combined with Tolazoline.Approved
TrichlormethiazideTolazoline may increase the hypotensive activities of Trichlormethiazide.Approved, Vet Approved
TrimazosinTolazoline may increase the hypotensive activities of Trimazosin.Experimental
TrimethaphanTolazoline may increase the hypotensive activities of Trimethaphan.Approved
UdenafilUdenafil may increase the antihypertensive activities of Tolazoline.Approved, Investigational
UnoprostoneTolazoline may increase the hypotensive activities of Unoprostone.Approved
ValsartanValsartan may increase the hypotensive activities of Tolazoline.Approved, Investigational
VardenafilVardenafil may increase the antihypertensive activities of Tolazoline.Approved
VerapamilThe risk or severity of adverse effects can be increased when Verapamil is combined with Tolazoline.Approved
VinpocetineTolazoline may increase the hypotensive activities of Vinpocetine.Investigational
XylometazolineTolazoline may increase the hypotensive activities of Xylometazoline.Approved
YohimbineYohimbine may decrease the antihypertensive activities of Tolazoline.Approved, Vet Approved
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesC04AB02M02AX02
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (73.7 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9821
Blood Brain Barrier+0.9334
Caco-2 permeable-0.5062
P-glycoprotein substrateSubstrate0.6249
P-glycoprotein inhibitor INon-inhibitor0.9707
P-glycoprotein inhibitor IINon-inhibitor0.9188
Renal organic cation transporterInhibitor0.7923
CYP450 2C9 substrateNon-substrate0.8404
CYP450 2D6 substrateSubstrate0.6912
CYP450 3A4 substrateNon-substrate0.8088
CYP450 1A2 substrateNon-inhibitor0.6013
CYP450 2C9 inhibitorNon-inhibitor0.9629
CYP450 2D6 inhibitorInhibitor0.7446
CYP450 2C19 inhibitorNon-inhibitor0.9844
CYP450 3A4 inhibitorNon-inhibitor0.9738
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9644
Ames testNon AMES toxic0.8569
CarcinogenicityNon-carcinogens0.9492
BiodegradationNot ready biodegradable0.9824
Rat acute toxicity2.5351 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7268
hERG inhibition (predictor II)Non-inhibitor0.8357
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Novartis pharmaceuticals corp
Packagers
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point174 °CPhysProp
water solubility373 mg/LNot Available
logP2.65SANGSTER (1993)
pKa10.3SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility1.36 mg/mLALOGPS
logP2.05ALOGPS
logP1.2ChemAxon
logS-2.1ALOGPS
pKa (Strongest Basic)10.25ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area24.39 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity49.07 m3·mol-1ChemAxon
Polarizability17.94 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (8.79 KB)
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
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzene and substituted derivatives. These are aromatic compounds containing one monocyclic ring system consisting of benzene.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassNot Available
Direct ParentBenzene and substituted derivatives
Alternative Parents
Substituents
  • Imidolactam
  • Monocyclic benzene moiety
  • 2-imidazoline
  • Azacycle
  • Organoheterocyclic compound
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Carboximidamide
  • Carboxylic acid amidine
  • Amidine
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Teskin O, Uydes-Dogan BS, Enc Y, Alp FI, Kaleli D, Keser S, Iyigun T, Bilgen F, Dagsali S, Ozdemir O: Comparative effects of tolazoline and nitroprusside on human isolated radial artery. Ann Thorac Surg. 2006 Jan;81(1):125-31. [PubMed:16368348 ]
  4. Song W, Zhang Y, Xia L, Liu G: [Effects of some mexiletine derivatives on alpha 1-adrenoceptors]. Yao Xue Xue Bao. 1998;33(2):102-5. [PubMed:11938943 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
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. Song W, Zhang Y, Xia L, Liu G: [Effects of some mexiletine derivatives on alpha 1-adrenoceptors]. Yao Xue Xue Bao. 1998;33(2):102-5. [PubMed:11938943 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Histamine receptor activity
Specific Function:
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
Molecular Weight:
55783.61 Da
References
  1. Roll C, Hanssler L: [Interaction of tolazoline and cimetidine in persistent fetal circulation of the newborn infant]. Monatsschr Kinderheilkd. 1993 Apr;141(4):297-9. [PubMed:8487790 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Histamine receptor activity
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) si...
Gene Name:
HRH2
Uniprot ID:
P25021
Molecular Weight:
40097.65 Da
References
  1. Ward RM: Pharmacology of tolazoline. Clin Perinatol. 1984 Oct;11(3):703-13. [PubMed:6386273 ]
  2. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP: ChEMBL: a large-scale bioactivity database for drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1100-7. doi: 10.1093/nar/gkr777. Epub 2011 Sep 23. [PubMed:21948594 ]
  3. Roll C, Hanssler L: [Interaction of tolazoline and cimetidine in persistent fetal circulation of the newborn infant]. Monatsschr Kinderheilkd. 1993 Apr;141(4):297-9. [PubMed:8487790 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Protein homodimerization activity
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name:
ADRA2C
Uniprot ID:
P18825
Molecular Weight:
49521.585 Da
References
  1. Trendelenburg AU, Sutej I, Starke K: Presynaptic alpha 2A/D-autoreceptors in the brain cortex of Cercopithecus aethiops. Naunyn Schmiedebergs Arch Pharmacol. 1997 Mar;355(3):341-6. [PubMed:9089664 ]
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. Trendelenburg AU, Sutej I, Starke K: Presynaptic alpha 2A/D-autoreceptors in the brain cortex of Cercopithecus aethiops. Naunyn Schmiedebergs Arch Pharmacol. 1997 Mar;355(3):341-6. [PubMed:9089664 ]
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Drug created on June 13, 2005 07:24 / Updated on December 08, 2016 11:11