Identification

Name
Pentolinium
Accession Number
DB01090  (APRD00038)
Type
Small Molecule
Groups
Approved
Description

A nicotinic antagonist that has been used as a ganglionic blocking agent in hypertension. [PubChem]

Structure
Thumb
Synonyms
  • Pentolineum
  • Pentolonium
  • Pentolonum
Product Ingredients
IngredientUNIICASInChI Key
Pentolinium tartrate953357GACY52-62-0HSMKTIKKPMTUQH-WBPXWQEISA-L
International/Other Brands
Ansolysen
Categories
UNII
ULL76WPU5X
CAS number
144-44-5
Weight
Average: 240.428
Monoisotopic: 240.256549034
Chemical Formula
C15H32N2
InChI Key
XSBSKEQEUFOSDD-UHFFFAOYSA-N
InChI
InChI=1S/C15H32N2/c1-16(12-6-7-13-16)10-4-3-5-11-17(2)14-8-9-15-17/h3-15H2,1-2H3/q+2
IUPAC Name
1-methyl-1-[5-(1-methylpyrrolidin-1-ium-1-yl)pentyl]pyrrolidin-1-ium
SMILES
C[N+]1(CCCCC[N+]2(C)CCCC2)CCCC1

Pharmacology

Indication

Used to produce controlled hypotension during surgical procedures and in hypertensive crises.

Structured Indications
Not Available
Pharmacodynamics

Pentolinium acts as a ganglionic blocking agent. Pentolinium inhibits release of adrenaline and noradrenaline from adrenergic nerves. It is used as an antihypertensive, and can be administered orally, intramuscularly, and subcutaneously.

Mechanism of action

Pentolinium binds to the nicotinic (ganglion) acetylcholine receptor. This receptor/channel is permeable to a range of divalent cations including calcium, the influx of which may activate a potassium current which hyperpolarizes the cell membrane. Blockage of the receptor leads to smooth muscle relaxation and vasodilaton.

TargetActionsOrganism
ANeuronal acetylcholine receptor subunit alpha-10
antagonist
Human
ANeuronal acetylcholine receptor subunit alpha-3
antagonist
Human
ANeuronal acetylcholine receptor subunit beta-4
antagonist
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

Oral, mouse: LD50 = 512 mg/kg; Oral, rat: LD50 = 890 mg/kg.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe therapeutic efficacy of Pentolinium can be decreased when used in combination with 1,10-Phenanthroline.Experimental
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Pentolinium.Experimental
AcebutololPentolinium may increase the hypotensive activities of Acebutolol.Approved
AclidiniumPentolinium may increase the anticholinergic activities of Aclidinium.Approved
AlcuroniumThe risk or severity of adverse effects can be increased when Pentolinium is combined with Alcuronium.Experimental
AlfentanilThe risk or severity of adverse effects can be increased when Pentolinium is combined with Alfentanil.Approved, Illicit
AlfuzosinAlfuzosin may increase the hypotensive activities of Pentolinium.Approved, Investigational
AliskirenPentolinium may increase the hypotensive activities of Aliskiren.Approved, Investigational
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Pentolinium is combined with Alphacetylmethadol.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Alphaprodine.Illicit
AlprenololAlprenolol may increase the hypotensive activities of Pentolinium.Approved, Withdrawn
AmbenoniumThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Ambenonium.Approved
AmbrisentanPentolinium may increase the hypotensive activities of Ambrisentan.Approved, Investigational
AmifostinePentolinium may increase the hypotensive activities of Amifostine.Approved, Investigational
AmlodipineAmlodipine may increase the hypotensive activities of Pentolinium.Approved
AmphetamineAmphetamine may increase the hypotensive activities of Pentolinium.Approved, Illicit
Anisotropine MethylbromideThe risk or severity of adverse effects can be increased when Anisotropine Methylbromide is combined with Pentolinium.Approved
AtenololAtenolol may increase the hypotensive activities of Pentolinium.Approved
AtracuriumThe risk or severity of adverse effects can be increased when Pentolinium is combined with Atracurium.Experimental, Investigational
Atracurium besylateThe risk or severity of adverse effects can be increased when Atracurium besylate is combined with Pentolinium.Approved
AtropineThe risk or severity of adverse effects can be increased when Atropine is combined with Pentolinium.Approved, Vet Approved
AvanafilAvanafil may increase the antihypertensive activities of Pentolinium.Approved
BenactyzineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Benactyzine.Withdrawn
BenazeprilBenazepril may increase the hypotensive activities of Pentolinium.Approved, Investigational
BendroflumethiazideThe serum concentration of Bendroflumethiazide can be increased when it is combined with Pentolinium.Approved
BenmoxinBenmoxin may increase the hypotensive activities of Pentolinium.Withdrawn
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Pentolinium.Approved
BepridilPentolinium may increase the hypotensive activities of Bepridil.Approved, Withdrawn
BetaxololBetaxolol may increase the hypotensive activities of Pentolinium.Approved
BethanidineBethanidine may increase the hypotensive activities of Pentolinium.Approved
BezitramideThe risk or severity of adverse effects can be increased when Pentolinium is combined with Bezitramide.Experimental, Illicit, Withdrawn
BietaserpineBietaserpine may increase the hypotensive activities of Pentolinium.Experimental
BimatoprostBimatoprost may increase the hypotensive activities of Pentolinium.Approved, Investigational
BiperidenThe risk or severity of adverse effects can be increased when Biperiden is combined with Pentolinium.Approved, Investigational
BisoprololBisoprolol may increase the hypotensive activities of Pentolinium.Approved
BornaprineThe risk or severity of adverse effects can be increased when Bornaprine is combined with Pentolinium.Experimental
BosentanBosentan may increase the hypotensive activities of Pentolinium.Approved, Investigational
Botulinum Toxin Type APentolinium may increase the anticholinergic activities of Botulinum Toxin Type A.Approved, Investigational
Botulinum Toxin Type BPentolinium may increase the anticholinergic activities of Botulinum Toxin Type B.Approved
BQ-123Pentolinium may increase the hypotensive activities of BQ-123.Investigational
BretyliumPentolinium may increase the hypotensive activities of Bretylium.Approved
BrimonidineBrimonidine may increase the antihypertensive activities of Pentolinium.Approved
BrofaromineBrofaromine may increase the hypotensive activities of Pentolinium.Experimental
BupranololPentolinium may increase the hypotensive activities of Bupranolol.Approved
BuprenorphineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
ButorphanolThe risk or severity of adverse effects can be increased when Pentolinium is combined with Butorphanol.Approved, Illicit, Vet Approved
ButylscopolamineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Scopolamine butylbromide.Approved, Vet Approved
CadralazineCadralazine may increase the hypotensive activities of Pentolinium.Experimental
CafedrinePentolinium may increase the hypotensive activities of Cafedrine.Investigational
CandesartanPentolinium may increase the hypotensive activities of Candesartan.Experimental
Candesartan cilexetilCandesartan cilexetil may increase the hypotensive activities of Pentolinium.Approved
CandoxatrilCandoxatril may increase the hypotensive activities of Pentolinium.Experimental
CaptoprilPentolinium may increase the hypotensive activities of Captopril.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Pentolinium is combined with Carfentanil.Illicit, Investigational, Vet Approved
CaroxazoneCaroxazone may increase the hypotensive activities of Pentolinium.Withdrawn
CarteololCarteolol may increase the hypotensive activities of Pentolinium.Approved
CarvedilolPentolinium may increase the hypotensive activities of Carvedilol.Approved, Investigational
CeliprololPentolinium may increase the hypotensive activities of Celiprolol.Approved, Investigational
ChlorothiazideThe serum concentration of Chlorothiazide can be increased when it is combined with Pentolinium.Approved, Vet Approved
ChlorphenoxamineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Chlorphenoxamine.Withdrawn
ChlorthalidoneThe serum concentration of Chlorthalidone can be increased when it is combined with Pentolinium.Approved
CicletaninePentolinium may increase the hypotensive activities of Cicletanine.Investigational
CilazaprilPentolinium may increase the hypotensive activities of Cilazapril.Approved
CimetropiumPentolinium may increase the anticholinergic activities of Cimetropium.Experimental, Investigational
ClonidineClonidine may increase the hypotensive activities of Pentolinium.Approved
CloranololPentolinium may increase the hypotensive activities of Cloranolol.Experimental
CodeineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Codeine.Approved, Illicit
CoumaphosThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Coumaphos.Vet Approved
CryptenamineCryptenamine may increase the hypotensive activities of Pentolinium.Approved
CyclopenthiazideThe serum concentration of Cyclopenthiazide can be increased when it is combined with Pentolinium.Experimental
CyclopentolateThe risk or severity of adverse effects can be increased when Cyclopentolate is combined with Pentolinium.Approved
CyclothiazideCyclothiazide may increase the hypotensive activities of Pentolinium.Approved
DarifenacinThe risk or severity of adverse effects can be increased when Darifenacin is combined with Pentolinium.Approved, Investigational
DebrisoquinDebrisoquin may increase the hypotensive activities of Pentolinium.Approved, Investigational
DecamethoniumThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Decamethonium.Approved
DelaprilPentolinium may increase the hypotensive activities of Delapril.Experimental
DemecariumThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Demecarium.Approved
DeserpidinePentolinium may increase the hypotensive activities of Deserpidine.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Pentolinium.Approved, Investigational
DexetimideThe risk or severity of adverse effects can be increased when Dexetimide is combined with Pentolinium.Withdrawn
DextromoramideThe risk or severity of adverse effects can be increased when Pentolinium is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Pentolinium is combined with Dextropropoxyphene.Approved, Illicit, Investigational, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Dezocine.Approved, Investigational
DiazoxideDiazoxide may increase the hypotensive activities of Pentolinium.Approved
DichlorvosThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Dichlorvos.Vet Approved
DicyclomineThe risk or severity of adverse effects can be increased when Dicyclomine is combined with Pentolinium.Approved
diethylnorsperminePentolinium may increase the hypotensive activities of diethylnorspermine.Investigational
DihydralazineDihydralazine may increase the hypotensive activities of Pentolinium.Investigational
DihydrocodeineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Dihydrocodeine.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Dihydromorphine.Experimental, Illicit
DiltiazemDiltiazem may increase the hypotensive activities of Pentolinium.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Pentolinium is combined with Diphenoxylate.Approved, Illicit
DistigmineThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Distigmine.Experimental
DonepezilThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Donepezil.Approved
DorzolamideDorzolamide may increase the hypotensive activities of Pentolinium.Approved
DoxazosinDoxazosin may increase the hypotensive activities of Pentolinium.Approved
DPDPEThe risk or severity of adverse effects can be increased when Pentolinium is combined with DPDPE.Experimental
DronabinolPentolinium may increase the tachycardic activities of Dronabinol.Approved, Illicit
EchothiophateThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Echothiophate.Approved
EdrophoniumThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Edrophonium.Approved
EfonidipinePentolinium may increase the hypotensive activities of Efonidipine.Approved, Investigational
EluxadolinePentolinium may increase the constipating activities of Eluxadoline.Approved
EmeproniumThe risk or severity of adverse effects can be increased when Pentolinium is combined with Emepronium.Experimental
EnalaprilEnalapril may increase the hypotensive activities of Pentolinium.Approved, Vet Approved
EnalaprilatPentolinium may increase the hypotensive activities of Enalaprilat.Approved
EndralazineEndralazine may increase the hypotensive activities of Pentolinium.Experimental
EpanololPentolinium may increase the hypotensive activities of Epanolol.Experimental
EpoprostenolPentolinium may increase the hypotensive activities of Epoprostenol.Approved
EprosartanEprosartan may increase the hypotensive activities of Pentolinium.Approved
EtanautineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Etanautine.Experimental
EthopropazineThe risk or severity of adverse effects can be increased when Ethopropazine is combined with Pentolinium.Approved
EthylmorphineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Ethylmorphine.Approved, Illicit
EtorphineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Etorphine.Illicit, Vet Approved
EtybenzatropineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Etybenzatropine.Experimental
FelodipineFelodipine may increase the hypotensive activities of Pentolinium.Approved, Investigational
FenoldopamFenoldopam may increase the hypotensive activities of Pentolinium.Approved
FentanylThe risk or severity of adverse effects can be increased when Pentolinium is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FenthionThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Fenthion.Vet Approved
Ferulic acidPentolinium may increase the hypotensive activities of Ferulic acid.Experimental
FesoterodineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Fesoterodine.Approved
FosinoprilFosinopril may increase the hypotensive activities of Pentolinium.Approved
FurazolidoneFurazolidone may increase the hypotensive activities of Pentolinium.Approved, Investigational, Vet Approved
GalantamineThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Galantamine.Approved
GallamineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Gallamine.Experimental
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Pentolinium.Approved
Glucagon recombinantThe risk or severity of adverse effects can be increased when Pentolinium is combined with Glucagon recombinant.Approved
GlycopyrroniumPentolinium may increase the anticholinergic activities of Glycopyrronium.Approved, Investigational, Vet Approved
GuanabenzGuanabenz may increase the hypotensive activities of Pentolinium.Approved, Investigational
GuanadrelGuanadrel may increase the hypotensive activities of Pentolinium.Approved
GuanazodinePentolinium may increase the hypotensive activities of Guanazodine.Experimental
GuanethidinePentolinium may increase the hypotensive activities of Guanethidine.Approved
GuanfacineGuanfacine may increase the hypotensive activities of Pentolinium.Approved, Investigational
GuanoclorPentolinium may increase the hypotensive activities of Guanoclor.Experimental
GuanoxabenzPentolinium may increase the hypotensive activities of Guanoxabenz.Experimental
GuanoxanPentolinium may increase the hypotensive activities of Guanoxan.Experimental
HarmalineHarmaline may increase the hypotensive activities of Pentolinium.Experimental
HeroinThe risk or severity of adverse effects can be increased when Pentolinium is combined with Heroin.Approved, Illicit, Investigational
HexamethoniumThe risk or severity of adverse effects can be increased when Pentolinium is combined with Hexamethonium.Experimental
HomatropineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Homatropine.Approved
Huperzine AThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Huperzine A.Investigational
HydracarbazineHydracarbazine may increase the hypotensive activities of Pentolinium.Experimental
HydralazineHydralazine may increase the hypotensive activities of Pentolinium.Approved
HydrochlorothiazideThe serum concentration of Hydrochlorothiazide can be increased when it is combined with Pentolinium.Approved, Vet Approved
HydrocodoneThe risk or severity of adverse effects can be increased when Pentolinium is combined with Hydrocodone.Approved, Illicit
HydroflumethiazideThe serum concentration of Hydroflumethiazide can be increased when it is combined with Pentolinium.Approved, Investigational
HydromorphoneThe risk or severity of adverse effects can be increased when Pentolinium is combined with Hydromorphone.Approved, Illicit
HyoscyamineThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Pentolinium.Approved
IloprostIloprost may increase the hypotensive activities of Pentolinium.Approved, Investigational
ImidaprilPentolinium may increase the hypotensive activities of Imidapril.Investigational
IndapamideThe serum concentration of Indapamide can be increased when it is combined with Pentolinium.Approved
IndenololPentolinium may increase the hypotensive activities of Indenolol.Withdrawn
IndoraminIndoramin may increase the hypotensive activities of Pentolinium.Withdrawn
IpidacrineThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Ipidacrine.Experimental
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Pentolinium.Approved
IproclozideIproclozide may increase the hypotensive activities of Pentolinium.Withdrawn
IproniazidIproniazid may increase the hypotensive activities of Pentolinium.Withdrawn
IrbesartanIrbesartan may increase the hypotensive activities of Pentolinium.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Pentolinium.Approved
IsoflurophateThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Isoflurophate.Approved, Investigational, Withdrawn
IsradipineIsradipine may increase the hypotensive activities of Pentolinium.Approved
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Pentolinium.Investigational
KetanserinKetanserin may increase the hypotensive activities of Pentolinium.Investigational
KetobemidoneThe risk or severity of adverse effects can be increased when Pentolinium is combined with Ketobemidone.Approved, Investigational
LabetalolLabetalol may increase the hypotensive activities of Pentolinium.Approved
LacidipinePentolinium may increase the hypotensive activities of Lacidipine.Approved, Investigational
LatanoprostLatanoprost may increase the hypotensive activities of Pentolinium.Approved, Investigational
LercanidipineLercanidipine may increase the hypotensive activities of Pentolinium.Approved, Investigational
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Pentolinium is combined with Levomethadyl Acetate.Approved, Investigational
LevorphanolThe risk or severity of adverse effects can be increased when Pentolinium is combined with Levorphanol.Approved
LinsidominePentolinium may increase the hypotensive activities of Linsidomine.Experimental
LisinoprilLisinopril may increase the hypotensive activities of Pentolinium.Approved, Investigational
LofentanilThe risk or severity of adverse effects can be increased when Pentolinium is combined with Lofentanil.Illicit
LofexidinePentolinium may increase the hypotensive activities of Lofexidine.Approved, Investigational
LosartanLosartan may increase the hypotensive activities of Pentolinium.Approved
MacitentanPentolinium may increase the hypotensive activities of Macitentan.Approved
MalathionThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Malathion.Approved, Investigational
ManidipinePentolinium may increase the hypotensive activities of Manidipine.Approved, Investigational
MazaticolThe risk or severity of adverse effects can be increased when Pentolinium is combined with Mazaticol.Experimental
MebanazineMebanazine may increase the hypotensive activities of Pentolinium.Withdrawn
MecamylamineThe risk or severity of adverse effects can be increased when Mecamylamine is combined with Pentolinium.Approved
MefloquineThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Mefloquine.Approved
MemantineThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Memantine.Approved, Investigational
MeptazinolThe risk or severity of adverse effects can be increased when Pentolinium is combined with Meptazinol.Experimental
MethadoneThe risk or severity of adverse effects can be increased when Pentolinium is combined with Methadone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Pentolinium is combined with Methadyl Acetate.Approved, Illicit
Methanesulfonyl FluorideThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Methanesulfonyl Fluoride.Investigational
MethanthelineThe risk or severity of adverse effects can be increased when Methantheline is combined with Pentolinium.Approved, Investigational
MethoserpidinePentolinium may increase the hypotensive activities of Methoserpidine.Experimental
MethyclothiazideThe serum concentration of Methyclothiazide can be increased when it is combined with Pentolinium.Approved
MethyldopaMethyldopa may increase the hypotensive activities of Pentolinium.Approved
Methylene blueMethylene blue may increase the hypotensive activities of Pentolinium.Approved, Investigational
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Pentolinium.Approved, Investigational
Methylscopolamine bromideThe risk or severity of adverse effects can be increased when Pentolinium is combined with Methylscopolamine bromide.Approved
MetipranololPentolinium may increase the hypotensive activities of Metipranolol.Approved
MetixeneThe risk or severity of adverse effects can be increased when Pentolinium is combined with Metixene.Approved
MetoclopramideThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Metoclopramide.Approved, Investigational
MetolazoneThe serum concentration of Metolazone can be increased when it is combined with Pentolinium.Approved
MetoprololMetoprolol may increase the hypotensive activities of Pentolinium.Approved, Investigational
MetyrosinePentolinium may increase the hypotensive activities of Metyrosine.Approved
MianserinMianserin may increase the anticholinergic activities of Pentolinium.Approved, Investigational
MibefradilPentolinium may increase the hypotensive activities of Mibefradil.Investigational, Withdrawn
MinaprineThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Minaprine.Approved
MinoxidilMinoxidil may increase the hypotensive activities of Pentolinium.Approved
MirabegronThe risk or severity of adverse effects can be increased when Pentolinium is combined with Mirabegron.Approved
MirodenafilMirodenafil may increase the antihypertensive activities of Pentolinium.Investigational
MoclobemideMoclobemide may increase the hypotensive activities of Pentolinium.Approved
MoexiprilMoexipril may increase the hypotensive activities of Pentolinium.Approved
MolsidomineMolsidomine may increase the hypotensive activities of Pentolinium.Approved, Investigational
MorphineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Morphine.Approved, Investigational
MoxonidineMoxonidine may increase the hypotensive activities of Pentolinium.Approved, Investigational
MuzoliminePentolinium may increase the hypotensive activities of Muzolimine.Experimental
NabilonePentolinium may increase the tachycardic activities of Nabilone.Approved, Investigational
NadololPentolinium may increase the hypotensive activities of Nadolol.Approved
NaftopidilPentolinium may increase the hypotensive activities of Naftopidil.Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Nalbuphine.Approved
NebivololPentolinium may increase the hypotensive activities of Nebivolol.Approved, Investigational
NeostigmineThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Neostigmine.Approved, Vet Approved
NialamideNialamide may increase the hypotensive activities of Pentolinium.Withdrawn
NicardipineNicardipine may increase the hypotensive activities of Pentolinium.Approved
NicomorphineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Nicomorphine.Experimental
NicorandilPentolinium may increase the hypotensive activities of Nicorandil.Approved, Investigational
NiguldipinePentolinium may increase the hypotensive activities of Niguldipine.Experimental
NilvadipinePentolinium may increase the hypotensive activities of Nilvadipine.Approved, Investigational
NimodipineNimodipine may increase the hypotensive activities of Pentolinium.Approved
NisoldipineNisoldipine may increase the hypotensive activities of Pentolinium.Approved
NitrendipineNitrendipine may increase the hypotensive activities of Pentolinium.Approved, Investigational
NitroprussideNitroprusside may increase the hypotensive activities of Pentolinium.Approved
NormethadoneThe risk or severity of adverse effects can be increased when Pentolinium is combined with Normethadone.Approved, Illicit
ObinutuzumabPentolinium may increase the hypotensive activities of Obinutuzumab.Approved
OctamoxinOctamoxin may increase the hypotensive activities of Pentolinium.Withdrawn
OlmesartanOlmesartan may increase the hypotensive activities of Pentolinium.Approved, Investigational
OmapatrilatOmapatrilat may increase the hypotensive activities of Pentolinium.Investigational
OpiumThe risk or severity of adverse effects can be increased when Pentolinium is combined with Opium.Approved, Illicit
OrphenadrineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Orphenadrine.Approved
OtiloniumThe risk or severity of adverse effects can be increased when Pentolinium is combined with Otilonium.Experimental, Investigational
OxitropiumThe risk or severity of adverse effects can be increased when Pentolinium is combined with Oxitropium.Investigational
OxprenololPentolinium may increase the hypotensive activities of Oxprenolol.Approved
OxybutyninThe risk or severity of adverse effects can be increased when Oxybutynin is combined with Pentolinium.Approved, Investigational
OxycodoneThe risk or severity of adverse effects can be increased when Pentolinium is combined with Oxycodone.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Pentolinium is combined with Oxymorphone.Approved, Investigational, Vet Approved
OxyphenoniumThe risk or severity of adverse effects can be increased when Oxyphenonium is combined with Pentolinium.Approved
PancuroniumThe risk or severity of adverse effects can be increased when Pentolinium is combined with Pancuronium.Approved
ParaoxonThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Paraoxon.Experimental
PargylinePargyline may increase the hypotensive activities of Pentolinium.Approved
PenbutololPentolinium may increase the hypotensive activities of Penbutolol.Approved, Investigational
PentazocineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Pentazocine.Approved, Vet Approved
PentoxifyllinePentoxifylline may increase the hypotensive activities of Pentolinium.Approved, Investigational
PerindoprilPerindopril may increase the hypotensive activities of Pentolinium.Approved
PethidineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Pethidine.Approved
PhenazocineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Phenazocine.Experimental
PhenelzinePhenelzine may increase the hypotensive activities of Pentolinium.Approved
PhenglutarimideThe risk or severity of adverse effects can be increased when Phenglutarimide is combined with Pentolinium.Experimental
PheniprazinePheniprazine may increase the hypotensive activities of Pentolinium.Withdrawn
PhenoperidineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Phenoperidine.Experimental
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Pentolinium.Approved
PhenoxypropazinePhenoxypropazine may increase the hypotensive activities of Pentolinium.Withdrawn
PhentolaminePhentolamine may increase the hypotensive activities of Pentolinium.Approved
PhysostigmineThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Physostigmine.Approved
PinacidilPinacidil may increase the hypotensive activities of Pentolinium.Withdrawn
PindololPindolol may increase the hypotensive activities of Pentolinium.Approved
PipecuroniumThe risk or severity of adverse effects can be increased when Pentolinium is combined with Pipecuronium.Approved
PirenzepineThe risk or severity of adverse effects can be increased when Pirenzepine is combined with Pentolinium.Approved
PiritramideThe risk or severity of adverse effects can be increased when Pentolinium is combined with Piritramide.Investigational
PirlindolePirlindole may increase the hypotensive activities of Pentolinium.Approved
PivhydrazinePivhydrazine may increase the hypotensive activities of Pentolinium.Withdrawn
Platelet Activating FactorPentolinium may increase the hypotensive activities of Platelet Activating Factor.Experimental
PolythiazideThe serum concentration of Polythiazide can be increased when it is combined with Pentolinium.Approved
Potassium ChloridePentolinium may increase the ulcerogenic activities of Potassium Chloride.Approved, Withdrawn
PramlintidePramlintide may increase the anticholinergic activities of Pentolinium.Approved, Investigational
PrazosinPrazosin may increase the hypotensive activities of Pentolinium.Approved
ProcarbazineProcarbazine may increase the hypotensive activities of Pentolinium.Approved
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Pentolinium.Approved
PropanthelineThe risk or severity of adverse effects can be increased when Propantheline is combined with Pentolinium.Approved
PropiverineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Propiverine.Approved, Investigational
PropranololPropranolol may increase the hypotensive activities of Pentolinium.Approved, Investigational
PyridostigmineThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Pyridostigmine.Approved
QuinaprilQuinapril may increase the hypotensive activities of Pentolinium.Approved, Investigational
QuinethazoneThe serum concentration of Quinethazone can be increased when it is combined with Pentolinium.Approved
QuinidineThe risk or severity of adverse effects can be increased when Quinidine is combined with Pentolinium.Approved
QuinineQuinine may increase the hypotensive activities of Pentolinium.Approved
RamiprilRamipril may increase the hypotensive activities of Pentolinium.Approved
RamosetronPentolinium may increase the constipating activities of Ramosetron.Approved, Investigational
RasagilineRasagiline may increase the hypotensive activities of Pentolinium.Approved
RemifentanilThe risk or severity of adverse effects can be increased when Pentolinium is combined with Remifentanil.Approved
RemikirenRemikiren may increase the hypotensive activities of Pentolinium.Approved
RescinnaminePentolinium may increase the hypotensive activities of Rescinnamine.Approved
ReserpineReserpine may increase the hypotensive activities of Pentolinium.Approved, Investigational
RilmenidineRilmenidine may increase the hypotensive activities of Pentolinium.Investigational
RiociguatPentolinium may increase the hypotensive activities of Riociguat.Approved
RituximabPentolinium may increase the hypotensive activities of Rituximab.Approved
RivastigmineThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Rivastigmine.Approved, Investigational
SafrazineSafrazine may increase the hypotensive activities of Pentolinium.Withdrawn
SaprisartanPentolinium may increase the hypotensive activities of Saprisartan.Experimental
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Pentolinium.Approved
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Pentolinium.Approved, Investigational
SelegilineSelegiline may increase the hypotensive activities of Pentolinium.Approved, Investigational, Vet Approved
SelexipagPentolinium may increase the hypotensive activities of Selexipag.Approved
SildenafilSildenafil may increase the antihypertensive activities of Pentolinium.Approved, Investigational
SitaxentanPentolinium may increase the hypotensive activities of Sitaxentan.Approved, Investigational, Withdrawn
SolifenacinThe risk or severity of adverse effects can be increased when Pentolinium is combined with Solifenacin.Approved
SpiraprilPentolinium may increase the hypotensive activities of Spirapril.Approved
SufentanilThe risk or severity of adverse effects can be increased when Pentolinium is combined with Sufentanil.Approved, Investigational
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Pentolinium.Approved, Investigational
TacrineThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Tacrine.Investigational, Withdrawn
TadalafilTadalafil may increase the antihypertensive activities of Pentolinium.Approved, Investigational
TalinololPentolinium may increase the hypotensive activities of Talinolol.Investigational
TapentadolThe risk or severity of adverse effects can be increased when Pentolinium is combined with Tapentadol.Approved
TelmisartanTelmisartan may increase the hypotensive activities of Pentolinium.Approved, Investigational
TemocaprilPentolinium may increase the hypotensive activities of Temocapril.Experimental, Investigational
TerlipressinPentolinium may increase the hypotensive activities of Terlipressin.Approved, Investigational
TetrahydropalmatinePentolinium may increase the hypotensive activities of Tetrahydropalmatine.Investigational
TheodrenalinePentolinium may increase the hypotensive activities of Theodrenaline.Investigational
TibolonePentolinium may increase the hypotensive activities of Tibolone.Approved, Investigational
TicrynafenPentolinium may increase the hypotensive activities of Ticrynafen.Withdrawn
TilidineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Tilidine.Experimental
TimololTimolol may increase the hypotensive activities of Pentolinium.Approved
TiotropiumPentolinium may increase the anticholinergic activities of Tiotropium.Approved
TolazolineTolazoline may increase the hypotensive activities of Pentolinium.Approved, Vet Approved
TolonidinePentolinium may increase the hypotensive activities of Tolonidine.Experimental
ToloxatoneToloxatone may increase the hypotensive activities of Pentolinium.Approved
TolterodineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Pentolinium.Approved, Investigational
TopiramateThe risk or severity of adverse effects can be increased when Pentolinium is combined with Topiramate.Approved
TorasemideTorasemide may increase the hypotensive activities of Pentolinium.Approved
TramadolThe risk or severity of adverse effects can be increased when Pentolinium is combined with Tramadol.Approved, Investigational
TrandolaprilTrandolapril may increase the hypotensive activities of Pentolinium.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Pentolinium.Experimental
TranylcypromineTranylcypromine may increase the hypotensive activities of Pentolinium.Approved
TravoprostTravoprost may increase the hypotensive activities of Pentolinium.Approved
TreprostinilTreprostinil may increase the hypotensive activities of Pentolinium.Approved, Investigational
TrichlorfonThe therapeutic efficacy of Pentolinium can be decreased when used in combination with Trichlorfon.Vet Approved
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Pentolinium.Approved, Vet Approved
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Pentolinium.Approved
TrimazosinTrimazosin may increase the hypotensive activities of Pentolinium.Experimental
TrimethaphanThe risk or severity of adverse effects can be increased when Pentolinium is combined with Trimethaphan.Approved, Investigational
TropatepineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Tropatepine.Experimental
TropicamideThe risk or severity of adverse effects can be increased when Tropicamide is combined with Pentolinium.Approved
TrospiumThe risk or severity of adverse effects can be increased when Trospium is combined with Pentolinium.Approved
TubocurarineThe risk or severity of adverse effects can be increased when Pentolinium is combined with Tubocurarine.Approved
UdenafilUdenafil may increase the antihypertensive activities of Pentolinium.Approved, Investigational
UmeclidiniumPentolinium may increase the anticholinergic activities of Umeclidinium.Approved
UnoprostonePentolinium may increase the hypotensive activities of Unoprostone.Approved
UrapidilUrapidil may increase the hypotensive activities of Pentolinium.Investigational
ValsartanValsartan may increase the hypotensive activities of Pentolinium.Approved, Investigational
VardenafilVardenafil may increase the antihypertensive activities of Pentolinium.Approved
VecuroniumThe risk or severity of adverse effects can be increased when Pentolinium is combined with Vecuronium.Approved
VincaminePentolinium may increase the hypotensive activities of Vincamine.Experimental
VinpocetinePentolinium may increase the hypotensive activities of Vinpocetine.Investigational
XipamidePentolinium may increase the hypotensive activities of Xipamide.Experimental
XylometazolinePentolinium may increase the hypotensive activities of Xylometazoline.Approved
YohimbineYohimbine may decrease the antihypertensive activities of Pentolinium.Approved, Vet Approved
ZofenoprilPentolinium may increase the hypotensive activities of Zofenopril.Experimental
Food Interactions
Not Available

References

General References
Not Available
External Links
Human Metabolome Database
HMDB15222
PubChem Compound
5850
PubChem Substance
46507977
ChemSpider
5641
BindingDB
50084945
ChEBI
347401
ChEMBL
CHEMBL1271
Therapeutic Targets Database
DAP001144
PharmGKB
PA164777033
MSDS
Download (61.6 KB)

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)213 °C (tartrate salt)Not Available
Predicted Properties
PropertyValueSource
Water Solubility1.16e-05 mg/mLALOGPS
logP-2.3ALOGPS
logP-6.3ChemAxon
logS-7.4ALOGPS
Physiological Charge2ChemAxon
Hydrogen Acceptor Count0ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area0 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity99.03 m3·mol-1ChemAxon
Polarizability31.36 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.9722
Blood Brain Barrier+0.9922
Caco-2 permeable+0.6627
P-glycoprotein substrateSubstrate0.5993
P-glycoprotein inhibitor INon-inhibitor0.9697
P-glycoprotein inhibitor IINon-inhibitor0.8383
Renal organic cation transporterInhibitor0.6294
CYP450 2C9 substrateNon-substrate0.8782
CYP450 2D6 substrateNon-substrate0.607
CYP450 3A4 substrateNon-substrate0.5941
CYP450 1A2 substrateNon-inhibitor0.9834
CYP450 2C9 inhibitorNon-inhibitor0.9533
CYP450 2D6 inhibitorNon-inhibitor0.9312
CYP450 2C19 inhibitorNon-inhibitor0.9348
CYP450 3A4 inhibitorNon-inhibitor0.9943
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9857
Ames testNon AMES toxic0.758
CarcinogenicityNon-carcinogens0.8783
BiodegradationReady biodegradable0.7183
Rat acute toxicity2.7632 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7283
hERG inhibition (predictor II)Non-inhibitor0.7476
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as n-alkylpyrrolidines. These are compounds containing a pyrrolidine moiety that is substituted at the N1-position with an alkyl group. Pyrrolidine is a five-membered saturated aliphatic heterocycle with one nitrogen atom and four carbon atoms.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Pyrrolidines
Sub Class
N-alkylpyrrolidines
Direct Parent
N-alkylpyrrolidines
Alternative Parents
Tetraalkylammonium salts / Azacyclic compounds / Organopnictogen compounds / Organic salts / Hydrocarbon derivatives / Amines / Organic cations
Substituents
N-alkylpyrrolidine / Tetraalkylammonium salt / Quaternary ammonium salt / Azacycle / Organic nitrogen compound / Organopnictogen compound / Hydrocarbon derivative / Organic salt / Organonitrogen compound / Amine
Molecular Framework
Aliphatic heteromonocyclic compounds
External Descriptors
organic cation (CHEBI:347401)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Receptor binding
Specific Function
Ionotropic receptor with a probable role in the modulation of auditory stimuli. Agonist binding may induce an extensive change in conformation that affects all subunits and leads to opening of an i...
Gene Name
CHRNA10
Uniprot ID
Q9GZZ6
Uniprot Name
Neuronal acetylcholine receptor subunit alpha-10
Molecular Weight
49704.295 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. McKay DB, Burkman AM: Nicotinic and nonnicotinic receptor-mediated actions of vinblastine. Proc Soc Exp Biol Med. 1993 Jul;203(3):372-6. [PubMed:8516349]
  4. Cachelin AB, Rust G: Beta-subunits co-determine the sensitivity of rat neuronal nicotinic receptors to antagonists. Pflugers Arch. 1995 Jan;429(3):449-51. [PubMed:7761270]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Ligand-gated ion channel activity
Specific Function
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
Gene Name
CHRNA3
Uniprot ID
P32297
Uniprot Name
Neuronal acetylcholine receptor subunit alpha-3
Molecular Weight
57479.54 Da
References
  1. Cachelin AB, Rust G: Beta-subunits co-determine the sensitivity of rat neuronal nicotinic receptors to antagonists. Pflugers Arch. 1995 Jan;429(3):449-51. [PubMed:7761270]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Ligand-gated ion channel activity
Specific Function
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
Gene Name
CHRNB4
Uniprot ID
P30926
Uniprot Name
Neuronal acetylcholine receptor subunit beta-4
Molecular Weight
56378.985 Da
References
  1. Cachelin AB, Rust G: Beta-subunits co-determine the sensitivity of rat neuronal nicotinic receptors to antagonists. Pflugers Arch. 1995 Jan;429(3):449-51. [PubMed:7761270]

Drug created on June 13, 2005 07:24 / Updated on December 01, 2017 17:13