Identification

Name
Tolazoline
Accession Number
DB00797  (APRD00170)
Type
Small Molecule
Groups
Approved, Vet Approved
Description

A 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
Product Ingredients
IngredientUNIICASInChI Key
Benzazoline hydrochlorideNot AvailableNot AvailableNot applicable
Tolazoline HydrochlorideE669Z6S1JG 59-97-2RHTNTTODYGNRSP-UHFFFAOYSA-N
International/Other Brands
Divascol (VUAB Pharma) / Imidalin (Astellas Pharma)
Categories
UNII
CHH9H12AQ3
CAS number
59-98-3
Weight
Average: 160.2157
Monoisotopic: 160.100048394
Chemical Formula
C10H12N2
InChI Key
JIVZKJJQOZQXQB-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

Indication

For the treatment of pulmonary artery anomalies

Structured Indications
Not Available
Pharmacodynamics

Tolazoline is a pulmonary vasodilator indicated used to decrease pulmonary vascular resistance (PVR) in persistent pulmonary hypertension of the newborn (PPHN).

Mechanism of action

Vasodilation 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.

TargetActionsOrganism
AAlpha-1A adrenergic receptor
antagonist
Human
UAlpha-2A adrenergic receptor
antagonist
Human
UHistamine H1 receptor
agonist
Human
UHistamine H2 receptor
agonist
Human
UAlpha-2C adrenergic receptor
binder
Human
UAlpha-2B adrenergic receptor
binder
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not 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
AldesleukinThe risk or severity of adverse effects can be increased when Tolazoline is combined with Aldesleukin.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 Tolazoline is combined with Amiloride.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 Tolazoline is combined with Amyl Nitrite.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 Tolazoline is combined with Apraclonidine.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 Tolazoline is combined with Azilsartan medoxomil.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
BietaserpineBietaserpine may increase the hypotensive activities of Tolazoline.Experimental
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
BQ-123Tolazoline may increase the hypotensive activities of BQ-123.Investigational
BretyliumTolazoline may increase the hypotensive activities of Bretylium.Approved
BrimonidineBrimonidine may increase the antihypertensive activities of Tolazoline.Approved
BrofaromineBrofaromine may increase the hypotensive activities of Tolazoline.Experimental
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 Tolazoline is combined with Bumetanide.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
CadralazineCadralazine may increase the hypotensive activities of Tolazoline.Experimental
CafedrineTolazoline may increase the hypotensive activities of Cafedrine.Investigational
CanagliflozinThe risk or severity of adverse effects can be increased when Tolazoline is combined with Canagliflozin.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
CicletanineTolazoline may increase the hypotensive activities of Cicletanine.Investigational
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 Tolazoline is combined with Clevidipine.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
CloranololTolazoline may increase the hypotensive activities of Cloranolol.Experimental
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
CyclopenthiazideTolazoline may increase the hypotensive activities of Cyclopenthiazide.Experimental
CyclothiazideCyclothiazide may increase the hypotensive activities of Tolazoline.Approved
DapagliflozinThe risk or severity of adverse effects can be increased when Tolazoline is combined with Dapagliflozin.Approved
DebrisoquinDebrisoquin may increase the hypotensive activities of Tolazoline.Approved
DelaprilTolazoline may increase the hypotensive activities of Delapril.Experimental
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 Tolazoline is combined with Dexmedetomidine.Approved, Vet Approved
DiazoxideDiazoxide may increase the hypotensive activities of Tolazoline.Approved
DiclofenamideThe risk or severity of adverse effects can be increased when Tolazoline is combined with Diclofenamide.Approved
diethylnorspermineTolazoline may increase the hypotensive activities of diethylnorspermine.Investigational
DihydralazineDihydralazine may increase the hypotensive activities of Tolazoline.Investigational
DiltiazemDiltiazem may increase the hypotensive activities of Tolazoline.Approved
DinutuximabThe risk or severity of adverse effects can be increased when Tolazoline is combined with Dinutuximab.Approved
DipyridamoleThe risk or severity of adverse effects can be increased when Tolazoline is combined with Dipyridamole.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 Tolazoline is combined with Empagliflozin.Approved
EnalaprilEnalapril may increase the hypotensive activities of Tolazoline.Approved, Vet Approved
EnalaprilatTolazoline may increase the hypotensive activities of Enalaprilat.Approved
EndralazineEndralazine may increase the hypotensive activities of Tolazoline.Experimental
EpanololTolazoline may increase the hypotensive activities of Epanolol.Experimental
EplerenoneThe risk or severity of adverse effects can be increased when Tolazoline is combined with Eplerenone.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 Tolazoline is combined with Esmolol.Approved
Etacrynic acidThe risk or severity of adverse effects can be increased when Tolazoline is combined with Etacrynic acid.Approved
FelodipineTolazoline may increase the hypotensive activities of Felodipine.Approved, Investigational
FenoldopamTolazoline may increase the hypotensive activities of Fenoldopam.Approved
Ferulic acidTolazoline may increase the hypotensive activities of Ferulic acid.Experimental
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 Tolazoline is combined with Furosemide.Approved, Vet Approved
GuanabenzGuanabenz may increase the hypotensive activities of Tolazoline.Approved
GuanadrelGuanadrel may increase the hypotensive activities of Tolazoline.Approved
GuanazodineTolazoline may increase the hypotensive activities of Guanazodine.Experimental
GuanethidineGuanethidine may increase the hypotensive activities of Tolazoline.Approved
GuanfacineGuanfacine may increase the hypotensive activities of Tolazoline.Approved, Investigational
GuanoclorTolazoline may increase the hypotensive activities of Guanoclor.Experimental
GuanoxabenzTolazoline may increase the hypotensive activities of Guanoxabenz.Experimental
GuanoxanTolazoline may increase the hypotensive activities of Guanoxan.Experimental
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Tolazoline.Approved, Vet Approved
HarmalineHarmaline may increase the hypotensive activities of Tolazoline.Experimental
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.Experimental
HydralazineHydralazine may increase the hypotensive activities of Tolazoline.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
IndoraminIndoramin may increase the hypotensive activities of Tolazoline.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 Tolazoline is combined with Isosorbide Dinitrate.Approved
Isosorbide MononitrateThe risk or severity of adverse effects can be increased when Tolazoline is combined with Isosorbide Mononitrate.Approved
IsoxsuprineThe risk or severity of adverse effects can be increased when Tolazoline is combined with Isoxsuprine.Approved, Withdrawn
IsradipineIsradipine may increase the hypotensive activities of Tolazoline.Approved
KetanserinKetanserin may increase the hypotensive activities of Tolazoline.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 Tolazoline is combined with Levobunolol.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
LinsidomineTolazoline may increase the hypotensive activities of Linsidomine.Experimental
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 Tolazoline is combined with Mannitol.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 Tolazoline is combined with Methazolamide.Approved
MethohexitalMethohexital may increase the hypotensive activities of Tolazoline.Approved
MethoserpidineTolazoline may increase the hypotensive activities of Methoserpidine.Experimental
MethyclothiazideThe risk or severity of adverse effects can be increased when Tolazoline is combined with Methyclothiazide.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
MirodenafilMirodenafil may increase the antihypertensive activities of Tolazoline.Investigational
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
MoxonidineMoxonidine may increase the hypotensive activities of Tolazoline.Approved
MuzolimineTolazoline may increase the hypotensive activities of Muzolimine.Experimental
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 Tolazoline is combined with Nesiritide.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 Tolazoline is combined with Nifedipine.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 Tolazoline is combined with Nitroglycerin.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 Tolazoline is combined with Papaverine.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
PinacidilPinacidil may increase the hypotensive activities of Tolazoline.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 Tolazoline is combined with Quetiapine.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
RilmenidineRilmenidine may increase the hypotensive activities of Tolazoline.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 Tolazoline is combined with Sotalol.Approved
SpiraprilTolazoline may increase the hypotensive activities of Spirapril.Approved
SpironolactoneThe risk or severity of adverse effects can be increased when Tolazoline is combined with Spironolactone.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
TalinololTolazoline may increase the hypotensive activities of Talinolol.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 Tolazoline is combined with Terazosin.Approved
TerlipressinTolazoline may increase the hypotensive activities of Terlipressin.Approved, Investigational
TetrahydropalmatineTolazoline may increase the hypotensive activities of Tetrahydropalmatine.Investigational
ThalidomideThe risk or severity of adverse effects can be increased when Thalidomide is combined with Tolazoline.Approved, Investigational, Withdrawn
TheodrenalineTolazoline may increase the hypotensive activities of Theodrenaline.Investigational
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.Withdrawn
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 Tolazoline is combined with Tizanidine.Approved
TolcaponeThe risk or severity of adverse effects can be increased when Tolazoline is combined with Tolcapone.Approved, Withdrawn
TolonidineTolazoline may increase the hypotensive activities of Tolonidine.Experimental
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 Tolazoline is combined with Triamterene.Approved
TrichlormethiazideTolazoline may increase the hypotensive activities of Trichlormethiazide.Approved, Vet Approved
TrimazosinTrimazosin may increase the hypotensive activities of Tolazoline.Experimental
TrimethaphanTrimethaphan may increase the hypotensive activities of Tolazoline.Approved
UdenafilUdenafil may increase the antihypertensive activities of Tolazoline.Approved, Investigational
UnoprostoneTolazoline may increase the hypotensive activities of Unoprostone.Approved
UrapidilUrapidil may increase the hypotensive activities of Tolazoline.Investigational
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 Tolazoline is combined with Verapamil.Approved
VincamineTolazoline may increase the hypotensive activities of Vincamine.Experimental
VinpocetineTolazoline may increase the hypotensive activities of Vinpocetine.Investigational
XipamideTolazoline may increase the hypotensive activities of Xipamide.Experimental
XylometazolineTolazoline may increase the hypotensive activities of Xylometazoline.Approved
YohimbineYohimbine may decrease the antihypertensive activities of Tolazoline.Approved, Vet Approved
ZofenoprilTolazoline may increase the hypotensive activities of Zofenopril.Experimental
Food Interactions
Not Available

References

Synthesis Reference
Not Available
General References
Not Available
External Links
Human Metabolome Database
HMDB14935
KEGG Compound
C07147
PubChem Compound
5504
PubChem Substance
46505641
ChemSpider
5303
BindingDB
55436
ChEBI
28502
ChEMBL
CHEMBL770
Therapeutic Targets Database
DAP000477
PharmGKB
PA451716
Wikipedia
Tolazoline
ATC Codes
M02AX02 — TolazolineC04AB02 — Tolazoline
AHFS Codes
Not Available
PDB Entries
Not Available
FDA label
Not Available
MSDS
Download (73.7 KB)

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
  • Novartis pharmaceuticals corp
Packagers
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)174 °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 RuleNoChemAxon
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 )

Spectra

Mass Spec (NIST)
Download (8.79 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
GC-MS Spectrum - EI-BGC-MSsplash10-0006-9400000000-7b6f1c4b249d1fba8927
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-03di-0900000000-692cb3b89bff443fa65f
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-03di-0900000000-03a59847388e2e741709
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-03di-4900000000-54d799a1c61663a2e513
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0006-9100000000-c36b35a2866405756d0a
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0006-9000000000-c543ee9f104cc9558d70

Taxonomy

Description
This compound belongs to the class of chemical entities known as benzene and substituted derivatives. These are aromatic compounds containing one monocyclic ring system consisting of benzene.
Kingdom
Chemical entities
Super Class
Organic compounds
Class
Benzenoids
Sub Class
Benzene and substituted derivatives
Direct Parent
Benzene and substituted derivatives
Alternative Parents
Imidolactams / Imidazolines / Propargyl-type 1,3-dipolar organic compounds / Carboximidamides / Carboxamidines / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
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
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
imidazoles (CHEBI:28502 )

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) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
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 oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
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 catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
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 diff...
Gene Name
HRH2
Uniprot ID
P25021
Uniprot Name
Histamine H2 receptor
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
Uniprot Name
Alpha-2C adrenergic receptor
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...
Gene Name
ADRA2B
Uniprot ID
P18089
Uniprot Name
Alpha-2B adrenergic receptor
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 ]

Drug created on June 13, 2005 07:24 / Updated on October 02, 2017 04:45