Identification
NameTropicamide
Accession NumberDB00809  (APRD00287)
TypeSmall Molecule
GroupsApproved
Description

One of the muscarinic antagonists with pharmacologic action similar to atropine and used mainly as an ophthalmic parasympatholytic or mydriatic. [PubChem]

Structure
Thumb
Synonyms
Mydriacyl
Tropicamid
Tropicamida
Tropicamide
Tropicamidum
External IDs Ro 1-7683
Product Ingredients Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Minims Tropicamide 1%Solution / drops1 %OphthalmicValeant Canada Lp Valeant Canada S.E.C.1995-12-31Not applicableCanada
MydriacylSolution0.5 %OphthalmicNovartis1951-12-31Not applicableCanada
MydriacylSolution1 %OphthalmicNovartis1969-12-31Not applicableCanada
Odan-tropicamideSolution1 %OphthalmicOdan Laboratories Ltd1985-12-31Not applicableCanada
Odan-tropicamideSolution0.5 %OphthalmicOdan Laboratories Ltd1985-12-31Not applicableCanada
PMS-tropicamide Oph Sltn 1%Solution / drops1 %OphthalmicPharmascience Inc1992-12-311996-09-09Canada
R.O.-tropamideLiquid10 mgOphthalmicRichmond Pharmaceuticals1992-12-311997-08-11Canada
TropicamideSolution1 %OphthalmicEberth Pharmaceuticals Inc1994-12-31Not applicableCanada
TropicamideSolution0.5 %OphthalmicEberth Pharmaceuticals Inc1994-12-31Not applicableCanada
Tropicamide 1% - Liq Oph 10mg/mlLiquid10 mgOphthalmicRivex Ophthalmics Inc.1997-09-152003-07-28Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
MydriacylSolution / drops10 mg/mLOphthalmicAlcon, Inc.1959-04-01Not applicableUs
MydriacylSolution / drops10 mg/mLOphthalmicAlcon, Inc.1959-04-01Not applicableUs
TropicamideSolution / drops5 mg/mLOphthalmicBauch & Lomb Incorporated1994-07-27Not applicableUs
TropicamideSolution / drops5 mg/mLOphthalmicAkorn2000-09-29Not applicableUs
TropicamideSolution / drops10 mg/mLOphthalmicSandoz2000-06-13Not applicableUs
TropicamideSolution / drops10 mg/mLOphthalmicHenry Schein2015-05-13Not applicableUs
TropicamideSolution / drops10 mg/mLOphthalmicAkorn2000-09-29Not applicableUs
TropicamideSolution / drops10 mg/mLOphthalmicBauch & Lomb Incorporated1994-07-27Not applicableUs
TropicamideSolution / drops5 mg/mLOphthalmicSandoz2000-06-09Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
BetterTaiwan Biotech
CamideIbn Sina
CiclomidrinLatinofarma
DilateIncepta
EyetropApex
LoseminOasis
MidaxRompharm
MidricSanbe
Minims TropicamideBausch & Lomb
MydralOcusoft
MydramideFischer
MydriaticumCiba Vision
MydricolUnimed
Ocu-TropicOcumed
TropicacylAkorn
Brand mixtures
NameLabellerIngredients
Diophenyl-T SolutionSandoz Canada Incorporated
ParemydAkorn
Phenyltrope Oph SolnSandoz Canada Incorporated
Categories
UNIIN0A3Z5XTC6
CAS number1508-75-4
WeightAverage: 284.3529
Monoisotopic: 284.152477894
Chemical FormulaC17H20N2O2
InChI KeyBGDKAVGWHJFAGW-UHFFFAOYSA-N
InChI
InChI=1S/C17H20N2O2/c1-2-19(12-14-8-10-18-11-9-14)17(21)16(13-20)15-6-4-3-5-7-15/h3-11,16,20H,2,12-13H2,1H3
IUPAC Name
N-ethyl-3-hydroxy-2-phenyl-N-(pyridin-4-ylmethyl)propanamide
SMILES
CCN(CC1=CC=NC=C1)C(=O)C(CO)C1=CC=CC=C1
Pharmacology
Indication

Indicated to induce mydriasis (dilation of the pupil) and cycloplegia (paralysis of the ciliary muscle of the eye) in diagnostic procedures, such as measurement of refractive errors and examination of the fundus of the eye.

Structured Indications Not Available
Pharmacodynamics

Tropicamide belongs to the group of medicines called anti-muscarinics. Tropicamide blocks the receptors in the muscles of the eye (muscarinic receptors). These receptors are involved controlling the pupil size and the shape of the lens. By blocking these receptors, tropicamide produces dilatation of the pupil (mydriasis) and prevents the eye from accommodating for near vision (cycloplegia). Tropicamide is given as eye drops to dilate the pupil and relax the lens so that eye examinations can be carried out thoroughly.

Mechanism of action

Tropicamide binds to and blocks the receptors in the muscles of the eye (muscarinic receptor M4). Tropicamide acts by blocking the responses of the iris sphincter muscle to the iris and ciliary muscles to cholinergic stimulation, producing dilation of the pupil and paralysis of the ciliary muscle.

TargetKindPharmacological actionActionsOrganismUniProt ID
Muscarinic acetylcholine receptor M4Proteinyes
antagonist
HumanP08173 details
Muscarinic acetylcholine receptor M1Proteinunknown
antagonist
HumanP11229 details
Muscarinic acetylcholine receptor M2Proteinunknown
antagonist
HumanP08172 details
Muscarinic acetylcholine receptor M3Proteinunknown
antagonist
HumanP20309 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein binding

45%

MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
Toxicity

Overdose can casue dry mouth, blurred vision, photophobia, hallucinations and rapid/irregular pulse.

Affected organisms
  • Humans and other mammals
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe therapeutic efficacy of Tropicamide can be decreased when used in combination with 1,10-Phenanthroline.Experimental
AclidiniumAclidinium may increase the anticholinergic activities of Tropicamide.Approved
AlfentanilThe risk or severity of adverse effects can be increased when Tropicamide is combined with Alfentanil.Approved, Illicit
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Tropicamide is combined with Alphacetylmethadol.Experimental, Illicit
AmbenoniumThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Ambenonium.Approved
Anisotropine MethylbromideThe risk or severity of adverse effects can be increased when Anisotropine Methylbromide is combined with Tropicamide.Approved
Atracurium besylateThe risk or severity of adverse effects can be increased when Atracurium besylate is combined with Tropicamide.Approved
AtropineThe risk or severity of adverse effects can be increased when Atropine is combined with Tropicamide.Approved, Vet Approved
BenactyzineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Benactyzine.Withdrawn
BendroflumethiazideThe serum concentration of Bendroflumethiazide can be increased when it is combined with Tropicamide.Approved
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Tropicamide.Approved
BezitramideThe risk or severity of adverse effects can be increased when Tropicamide is combined with Bezitramide.Experimental, Illicit, Withdrawn
BiperidenThe risk or severity of adverse effects can be increased when Tropicamide is combined with Biperiden.Approved
Botulinum Toxin Type ATropicamide may increase the anticholinergic activities of Botulinum Toxin Type A.Approved, Investigational
Botulinum Toxin Type BTropicamide may increase the anticholinergic activities of Botulinum Toxin Type B.Approved
BuprenorphineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
ButorphanolThe risk or severity of adverse effects can be increased when Tropicamide is combined with Butorphanol.Approved, Illicit, Vet Approved
CarfentanilThe risk or severity of adverse effects can be increased when Tropicamide is combined with Carfentanil.Illicit, Vet Approved
ChlorothiazideThe serum concentration of Chlorothiazide can be increased when it is combined with Tropicamide.Approved, Vet Approved
ChlorphenoxamineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Chlorphenoxamine.Withdrawn
ChlorthalidoneThe serum concentration of Chlorthalidone can be increased when it is combined with Tropicamide.Approved
CimetropiumTropicamide may increase the anticholinergic activities of Cimetropium.Experimental
CodeineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Codeine.Approved, Illicit
CyclopentolateThe risk or severity of adverse effects can be increased when Tropicamide is combined with Cyclopentolate.Approved
DarifenacinThe risk or severity of adverse effects can be increased when Darifenacin is combined with Tropicamide.Approved, Investigational
DecamethoniumThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Decamethonium.Approved
DemecariumThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Demecarium.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Desloratadine.Approved, Investigational
DexetimideThe risk or severity of adverse effects can be increased when Tropicamide is combined with Dexetimide.Withdrawn
DextromoramideThe risk or severity of adverse effects can be increased when Tropicamide is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Tropicamide is combined with Dextropropoxyphene.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Dezocine.Approved
DicyclomineThe risk or severity of adverse effects can be increased when Dicyclomine is combined with Tropicamide.Approved
DihydrocodeineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Dihydrocodeine.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Dihydromorphine.Experimental, Illicit
DiphenoxylateThe risk or severity of adverse effects can be increased when Tropicamide is combined with Diphenoxylate.Approved, Illicit
DonepezilThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Donepezil.Approved
DronabinolTropicamide may increase the tachycardic activities of Dronabinol.Approved, Illicit
EchothiophateThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Echothiophate.Approved
EdrophoniumThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Edrophonium.Approved
EluxadolineTropicamide may increase the constipating activities of Eluxadoline.Approved
EthopropazineThe risk or severity of adverse effects can be increased when Ethopropazine is combined with Tropicamide.Approved
EthylmorphineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Ethylmorphine.Approved, Illicit
EtorphineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Etorphine.Illicit, Vet Approved
FentanylThe risk or severity of adverse effects can be increased when Tropicamide is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Fesoterodine.Approved
GalantamineThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Galantamine.Approved
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Tropicamide.Approved
Ginkgo bilobaThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Ginkgo biloba.Approved, Nutraceutical
Glucagon recombinantThe risk or severity of adverse effects can be increased when Tropicamide is combined with Glucagon recombinant.Approved
GlycopyrroniumTropicamide may increase the anticholinergic activities of Glycopyrronium.Approved, Investigational, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Tropicamide is combined with Heroin.Approved, Illicit
HexamethoniumThe risk or severity of adverse effects can be increased when Tropicamide is combined with Hexamethonium.Experimental
Huperzine AThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Huperzine A.Investigational
HydrochlorothiazideThe serum concentration of Hydrochlorothiazide can be increased when it is combined with Tropicamide.Approved, Vet Approved
HydrocodoneThe risk or severity of adverse effects can be increased when Tropicamide is combined with Hydrocodone.Approved, Illicit
HydroflumethiazideThe serum concentration of Hydroflumethiazide can be increased when it is combined with Tropicamide.Approved
HydromorphoneThe risk or severity of adverse effects can be increased when Tropicamide is combined with Hydromorphone.Approved, Illicit
HyoscyamineThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Tropicamide.Approved
IndapamideThe serum concentration of Indapamide can be increased when it is combined with Tropicamide.Approved
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Tropicamide.Approved
IsoflurophateThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Isoflurophate.Approved, Withdrawn
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Tropicamide.Investigational
KetobemidoneThe risk or severity of adverse effects can be increased when Tropicamide is combined with Ketobemidone.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Tropicamide is combined with Levomethadyl Acetate.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Tropicamide is combined with Levorphanol.Approved
LofentanilThe risk or severity of adverse effects can be increased when Tropicamide is combined with Lofentanil.Illicit
MalathionThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Malathion.Approved, Investigational
MecamylamineThe risk or severity of adverse effects can be increased when Mecamylamine is combined with Tropicamide.Approved
MefloquineThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Mefloquine.Approved
MemantineThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Memantine.Approved, Investigational
MethadoneThe risk or severity of adverse effects can be increased when Tropicamide is combined with Methadone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Tropicamide is combined with Methadyl Acetate.Approved, Illicit
MethanthelineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Methantheline.Approved
MethyclothiazideThe serum concentration of Methyclothiazide can be increased when it is combined with Tropicamide.Approved
MetixeneThe risk or severity of adverse effects can be increased when Tropicamide is combined with Metixene.Approved
MetolazoneThe serum concentration of Metolazone can be increased when it is combined with Tropicamide.Approved
MianserinMianserin may increase the anticholinergic activities of Tropicamide.Approved
MinaprineThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Minaprine.Approved
MirabegronThe risk or severity of adverse effects can be increased when Tropicamide is combined with Mirabegron.Approved
MorphineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Morphine.Approved, Investigational
NabiloneTropicamide may increase the tachycardic activities of Nabilone.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Nalbuphine.Approved
NeostigmineThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Neostigmine.Approved, Vet Approved
NormethadoneThe risk or severity of adverse effects can be increased when Tropicamide is combined with Normethadone.Approved, Illicit
OpiumThe risk or severity of adverse effects can be increased when Tropicamide is combined with Opium.Approved, Illicit
OrphenadrineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Orphenadrine.Approved
OxybutyninThe risk or severity of adverse effects can be increased when Tropicamide is combined with Oxybutynin.Approved, Investigational
OxycodoneThe risk or severity of adverse effects can be increased when Tropicamide is combined with Oxycodone.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Tropicamide is combined with Oxymorphone.Approved, Investigational, Vet Approved
OxyphenoniumThe risk or severity of adverse effects can be increased when Oxyphenonium is combined with Tropicamide.Approved
PancuroniumThe risk or severity of adverse effects can be increased when Tropicamide is combined with Pancuronium.Approved
PentazocineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Pentazocine.Approved, Vet Approved
PentoliniumThe risk or severity of adverse effects can be increased when Tropicamide is combined with Pentolinium.Approved
PethidineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Pethidine.Approved
PhysostigmineThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Physostigmine.Approved
PipecuroniumThe risk or severity of adverse effects can be increased when Tropicamide is combined with Pipecuronium.Approved
PirenzepineThe risk or severity of adverse effects can be increased when Pirenzepine is combined with Tropicamide.Approved
PolythiazideThe serum concentration of Polythiazide can be increased when it is combined with Tropicamide.Approved
Potassium ChlorideTropicamide may increase the ulcerogenic activities of Potassium Chloride.Approved, Withdrawn
PramlintidePramlintide may increase the anticholinergic activities of Tropicamide.Approved, Investigational
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Tropicamide.Approved
PropanthelineThe risk or severity of adverse effects can be increased when Propantheline is combined with Tropicamide.Approved
PyridostigmineThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Pyridostigmine.Approved
QuinethazoneThe serum concentration of Quinethazone can be increased when it is combined with Tropicamide.Approved
QuinidineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Quinidine.Approved
RamosetronTropicamide may increase the constipating activities of Ramosetron.Approved
RemifentanilThe risk or severity of adverse effects can be increased when Tropicamide is combined with Remifentanil.Approved
RivastigmineThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Rivastigmine.Approved, Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Tropicamide.Approved
Scopolamine butylbromideThe risk or severity of adverse effects can be increased when Tropicamide is combined with Scopolamine butylbromide.Approved
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Tropicamide.Approved, Investigational
SolifenacinThe risk or severity of adverse effects can be increased when Tropicamide is combined with Solifenacin.Approved
SufentanilThe risk or severity of adverse effects can be increased when Tropicamide is combined with Sufentanil.Approved, Investigational
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Tropicamide.Approved
TacrineThe therapeutic efficacy of Tropicamide can be decreased when used in combination with Tacrine.Withdrawn
TapentadolThe risk or severity of adverse effects can be increased when Tropicamide is combined with Tapentadol.Approved
TiotropiumTropicamide may increase the anticholinergic activities of Tiotropium.Approved
TolterodineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Tolterodine.Approved, Investigational
TopiramateThe risk or severity of adverse effects can be increased when Tropicamide is combined with Topiramate.Approved
TramadolThe risk or severity of adverse effects can be increased when Tropicamide is combined with Tramadol.Approved, Investigational
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Tropicamide.Approved, Vet Approved
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Tropicamide.Approved
TrimethaphanThe risk or severity of adverse effects can be increased when Tropicamide is combined with Trimethaphan.Approved
TrospiumThe risk or severity of adverse effects can be increased when Trospium is combined with Tropicamide.Approved
TubocurarineThe risk or severity of adverse effects can be increased when Tropicamide is combined with Tubocurarine.Approved
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Tropicamide.Approved
VecuroniumThe risk or severity of adverse effects can be increased when Tropicamide is combined with Vecuronium.Approved
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesS01FA06S01FA56
AHFS Codes
  • 52:24.00
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (73.1 KB)
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
1RecruitingPreventionIntraocular Pressure1
2CompletedTreatmentSialorrhea Secondary to Parkinson's Disease1
3CompletedTreatmentCataracts1
3CompletedTreatmentEye Diseases1
4Active Not RecruitingTreatmentCorneal Transplant / Grafting, Corneal / Keratoplasty, Lamellar / Transplantation, Cornea / Transplantation, Corneal1
4CompletedDiagnosticPreterm Infants1
4Unknown StatusDiagnosticRefractive Errors1
4Unknown StatusPreventionMyopia1
Not AvailableCompletedNot AvailableFabry's Disease1
Not AvailableCompletedTreatmentCataracts1
Pharmacoeconomics
Manufacturers
  • Alcon laboratories inc
  • Pharmafair inc
  • Akorn inc
  • Alcon universal ltd
  • Bausch and lomb pharmaceuticals inc
  • Miza pharmaceuticals usa inc
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
Solution / dropsOphthalmic10 mg/mL
SolutionOphthalmic0.5 %
SolutionOphthalmic1 %
SolutionOphthalmic
Solution / dropsOphthalmic1 %
LiquidOphthalmic10 mg
Solution / dropsOphthalmic5 mg/mL
Prices
Unit descriptionCostUnit
Tropicamide powder72.83USD g
Mydriacyl 1% Solution 15ml Bottle59.84USD bottle
Tropicamide 0.5% Solution 15ml Bottle17.99USD bottle
Tropicamide 1% Solution 15ml Bottle17.75USD bottle
Mydriacyl 1% Solution 3ml Bottle17.28USD bottle
Tropicamide 1% Solution 3ml Bottle13.99USD bottle
Tropicamide 1% Solution 2ml Bottle7.99USD bottle
Mydriacyl 1% eye drops5.54USD ml
Tropicamide 1% eye drops2.52USD ml
Paremyd eye drops1.28USD ml
Mydriacyl 1 % Solution1.21USD ml
Tropicamide 0.5% eye drops1.06USD ml
Mydriacyl 0.5 % Solution0.94USD ml
Tropicacyl 1% eye drops0.71USD ml
Tropicacyl 0.5% eye drops0.67USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point (°C)96.5 °CPhysProp
logP1.3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.375 mg/mLALOGPS
logP1.42ALOGPS
logP1.38ChemAxon
logS-2.9ALOGPS
pKa (Strongest Acidic)15.18ChemAxon
pKa (Strongest Basic)5.02ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area53.43 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity82.53 m3·mol-1ChemAxon
Polarizability29.78 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9943
Blood Brain Barrier+0.9777
Caco-2 permeable+0.5986
P-glycoprotein substrateNon-substrate0.5777
P-glycoprotein inhibitor INon-inhibitor0.8947
P-glycoprotein inhibitor IINon-inhibitor0.9442
Renal organic cation transporterNon-inhibitor0.6694
CYP450 2C9 substrateNon-substrate0.7731
CYP450 2D6 substrateNon-substrate0.7878
CYP450 3A4 substrateNon-substrate0.7241
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorInhibitor0.895
CYP450 2D6 inhibitorNon-inhibitor0.923
CYP450 2C19 inhibitorNon-inhibitor0.8184
CYP450 3A4 inhibitorInhibitor0.796
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6008
Ames testNon AMES toxic0.6905
CarcinogenicityNon-carcinogens0.7473
BiodegradationNot ready biodegradable0.8754
Rat acute toxicity2.4857 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9686
hERG inhibition (predictor II)Non-inhibitor0.8009
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Spectra
Mass Spec (NIST)Download (8.19 KB)
Spectra
Spectrum TypeDescriptionSplash Key
LC-MS/MSLC-MS/MS Spectrum - , positivesplash10-000i-0290000000-8c6533b9c36099d52c7cView in MoNA
LC-MS/MSLC-MS/MS Spectrum - , positivesplash10-000i-1390000000-cf89fdf233a948aed049View in MoNA
LC-MS/MSLC-MS/MS Spectrum - , positivesplash10-0a4r-4930000000-ca3db93b017c3a6fb89bView in MoNA
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 chemical entities known as phenylacetamides. These are amide derivatives of phenylacetic acids.
KingdomChemical entities
Super ClassOrganic compounds
ClassBenzenoids
Sub ClassBenzene and substituted derivatives
Direct ParentPhenylacetamides
Alternative ParentsPyridines and derivatives / Tertiary carboxylic acid amides / Heteroaromatic compounds / Azacyclic compounds / Primary alcohols / Organopnictogen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds
SubstituentsPhenylacetamide / Pyridine / Tertiary carboxylic acid amide / Heteroaromatic compound / Carboxamide group / Azacycle / Organoheterocyclic compound / Carboxylic acid derivative / Hydrocarbon derivative / Organic oxygen compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Guanyl-nucleotide exchange factor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is inhibition of adenylate cyclase.
Gene Name:
CHRM4
Uniprot ID:
P08173
Molecular Weight:
53048.65 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. Betz AJ, McLaughlin PJ, Burgos M, Weber SM, Salamone JD: The muscarinic receptor antagonist tropicamide suppresses tremulous jaw movements in a rodent model of parkinsonian tremor: possible role of M4 receptors. Psychopharmacology (Berl). 2007 Oct;194(3):347-59. Epub 2007 Jun 27. [PubMed:17594079 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Phosphatidylinositol phospholipase c activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM1
Uniprot ID:
P11229
Molecular Weight:
51420.375 Da
References
  1. Betz AJ, McLaughlin PJ, Burgos M, Weber SM, Salamone JD: The muscarinic receptor antagonist tropicamide suppresses tremulous jaw movements in a rodent model of parkinsonian tremor: possible role of M4 receptors. Psychopharmacology (Berl). 2007 Oct;194(3):347-59. Epub 2007 Jun 27. [PubMed:17594079 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled acetylcholine receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then trigge...
Gene Name:
CHRM2
Uniprot ID:
P08172
Molecular Weight:
51714.605 Da
References
  1. Betz AJ, McLaughlin PJ, Burgos M, Weber SM, Salamone JD: The muscarinic receptor antagonist tropicamide suppresses tremulous jaw movements in a rodent model of parkinsonian tremor: possible role of M4 receptors. Psychopharmacology (Berl). 2007 Oct;194(3):347-59. Epub 2007 Jun 27. [PubMed:17594079 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM3
Uniprot ID:
P20309
Molecular Weight:
66127.445 Da
References
  1. Betz AJ, McLaughlin PJ, Burgos M, Weber SM, Salamone JD: The muscarinic receptor antagonist tropicamide suppresses tremulous jaw movements in a rodent model of parkinsonian tremor: possible role of M4 receptors. Psychopharmacology (Berl). 2007 Oct;194(3):347-59. Epub 2007 Jun 27. [PubMed:17594079 ]
Drug created on June 13, 2005 07:24 / Updated on June 11, 2017 15:43