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Identification
NameAmoxapine
Accession NumberDB00543  (APRD00142)
TypeSmall Molecule
GroupsApproved
Description

Amoxapine, the N-demethylated derivative of the antipsychotic agent loxapine, is a dibenzoxazepine-derivative tricyclic antidepressant (TCA). TCAs are structurally similar to phenothiazines. They contain a tricyclic ring system with an alkyl amine substituent on the central ring. In non-depressed individuals, amoxapine does not affect mood or arousal, but may cause sedation. In depressed individuals, amoxapine exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. In addition, TCAs down-regulate cerebral cortical β-adrenergic receptors and sensitize post-synaptic serotonergic receptors with chronic use. The antidepressant effects of TCAs are thought to be due to an overall increase in serotonergic neurotransmission. TCAs also block histamine H1 receptors, α1-adrenergic receptors and muscarinic receptors, which accounts for their sedative, hypotensive and anticholinergic effects (e.g. blurred vision, dry mouth, constipation, urinary retention), respectively. See toxicity section below for a complete listing of side effects. Amoxapine may be used to treat neurotic and reactive depressive disorders, endogenous and psychotic depression, and mixed symptoms of depression and anxiety or agitation.

Structure
Thumb
Synonyms
2-Chloro-11-(1-piperazinyl)dibenz(b,F)(1,4)oxazepine
Amoxapin
Amoxapina
Amoxapinum
Amoxepine
Desmethylloxapin
External Identifiers
  • CL 67772
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Asendin - Tab 100mgtablet100 mgoralWyeth Ayerst Canada Inc.1999-04-122002-06-10Canada
Asendin - Tab 25mgtablet25 mgoralWyeth Ayerst Canada Inc.1997-02-042000-08-02Canada
Asendin - Tab 50mgtablet50 mgoralWyeth Ayerst Canada Inc.1997-04-292001-12-12Canada
Asendin Tab 100mgtablet100 mgoralLederle Cyanamid Canada Inc.1981-12-311999-04-12Canada
Asendin Tab 25mgtablet25 mgoralLederle Cyanamid Canada Inc.1981-12-311997-08-14Canada
Asendin Tab 50mgtablet50 mgoralLederle Cyanamid Canada Inc.1981-12-311999-04-12Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Amoxapinetablet25 mg/1oralActavis Pharma, Inc.1992-08-28Not applicableUs
Amoxapinetablet50 mg/1oralPhysicians Total Care, Inc.2011-05-12Not applicableUs
Amoxapinetablet150 mg/1oralActavis Pharma, Inc.1992-08-28Not applicableUs
Amoxapinetablet100 mg/1oralActavis Pharma, Inc.1992-08-28Not applicableUs
Amoxapinetablet50 mg/1oralActavis Pharma, Inc.1992-08-28Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AdisenKun Wha
AmolifeNot Available
AmoxanWyeth KK
AsendinNot Available
AsendisNot Available
DéfanylEisai
DemoloxWyeth
OxaminePsyco Remedies
OxcapNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIR63VQ857OT
CAS number14028-44-5
WeightAverage: 313.781
Monoisotopic: 313.098189856
Chemical FormulaC17H16ClN3O
InChI KeyInChIKey=QWGDMFLQWFTERH-UHFFFAOYSA-N
InChI
InChI=1S/C17H16ClN3O/c18-12-5-6-15-13(11-12)17(21-9-7-19-8-10-21)20-14-3-1-2-4-16(14)22-15/h1-6,11,19H,7-10H2
IUPAC Name
13-chloro-10-(piperazin-1-yl)-2-oxa-9-azatricyclo[9.4.0.0³,⁸]pentadeca-1(11),3,5,7,9,12,14-heptaene
SMILES
ClC1=CC2=C(OC3=CC=CC=C3N=C2N2CCNCC2)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as dibenzoxazepines. These are compounds containing a dibenzoxazepine moiety, which consists of two benzene connected by an oxazepine ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzoxazepines
Sub ClassDibenzoxazepines
Direct ParentDibenzoxazepines
Alternative Parents
Substituents
  • Dibenzoxazepine
  • Diaryl ether
  • Imidolactam
  • Benzenoid
  • Piperazine
  • 1,4-diazinane
  • Aryl halide
  • Aryl chloride
  • Tertiary amine
  • Oxacycle
  • Azacycle
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Secondary amine
  • Ether
  • Secondary aliphatic amine
  • Carboxylic acid amidine
  • Amidine
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the relief of symptoms of depression in patients with neurotic or reactive depressive disorders as well as endogenous and psychotic depressions. May also be used to treat depression accompanied by anxiety or agitation.
PharmacodynamicsAmoxapine is a tricyclic antidepressant of the dibenzoxazepine class, chemically distinct from the dibenzodiazepines, dibenzocycloheptenes, and dibenzoxepines. It has a mild sedative component to its action. The mechanism of its clinical action in man is not well understood. In animals, amoxapine reduced the uptake of nor-epinephirine and serotonin and blocked the response of dopamine receptors to dopamine. Amoxapine is not a monoamine oxidase inhibitor. Clinical studies have demonstrated that amoxapine has a more rapid onset of action than either amitriptyline or imipramine
Mechanism of actionAmoxapine acts by decreasing the reuptake of norepinephrine and serotonin (5-HT).
Related Articles
AbsorptionRapidly and almost completely absorbed from the GI tract. Peak plasma concentrations occur within 1-2 hours of oral administration of a single dose.
Volume of distribution

Widely distributed in body tissues with highest concentrations found in lungs, spleen, kidneys, heart, and brain. Lower concentrations can be detected in testes and muscle.

Protein bindingIn vitro tests show that amoxapine binding to human plasma proteins is approximately 90%.
Metabolism

Amoxapine is almost completely metabolized in the liver to its major metabolite, 8-hydroxyamoxapine, and a minor metabolite, 7-hydroxyamoxapine. Both metabolites are phamacologically inactive and have half-lives of approximately 30 and 6.5 hours, respectively.

SubstrateEnzymesProduct
Amoxapine
Not Available
7-hydroxyamoxapineDetails
Amoxapine
Not Available
8-hydroxyamoxapineDetails
Route of elimination60-69% of a single orally administered dose of amoxapine is excreted in urine, principally as conjugated metabolites. 7-18% of the dose is excrete feces mainly as unconjugated metabolites. Less than 5% of the dose is excreted as unchanged drug in urine.
Half life8 hours
ClearanceNot Available
ToxicityToxic manifestations of amoxapine overdosage differ significantly from those of other tricyclic antidepressants. Serious cardiovascular effects are seldom if ever observed. However, CNS effects, particularly grand mal convulsions, occur frequently, and treatment should be directed primarily toward prevention or control of seizures. Status epilepticus may develop and constitutes a neurologic emergency. Coma and acidosis are other serious complications of substantial amoxapine overdosage in some cases. Renal failure may develop two to five days after toxic overdose in patients who may appear otherwise recovered. Acute tubular necrosis with rhabdomuolysis and myolobinurla is the most common renal complication in such cases. This reaction probably occurs in less than 5% of overdose cases, and typically in those who have experienced multiple seizures.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9928
Blood Brain Barrier+0.988
Caco-2 permeable-0.5488
P-glycoprotein substrateSubstrate0.8068
P-glycoprotein inhibitor IInhibitor0.7622
P-glycoprotein inhibitor IIInhibitor0.8387
Renal organic cation transporterInhibitor0.6414
CYP450 2C9 substrateNon-substrate0.7682
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.5168
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8308
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5472
Ames testNon AMES toxic0.7277
CarcinogenicityNon-carcinogens0.8159
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.9781 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.6376
hERG inhibition (predictor II)Inhibitor0.7874
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Sandoz inc
  • Watson laboratories inc
  • Lederle laboratories div american cyanamid co
Packagers
Dosage forms
FormRouteStrength
Tabletoral100 mg/1
Tabletoral150 mg/1
Tabletoral25 mg/1
Tabletoral50 mg/1
Tabletoral100 mg
Tabletoral25 mg
Tabletoral50 mg
Prices
Unit descriptionCostUnit
Amoxapine 30 150 mg tablet Bottle82.15USD bottle
Amoxapine 150 mg tablet2.63USD tablet
Amoxapine 100 mg tablet1.7USD tablet
Amoxapine 50 mg tablet1.02USD tablet
Amoxapine 25 mg tablet0.63USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point175-176Howell, C.F., Hardy, R.A., Jr. and Quinones, N.Q.; US. Patent 3,663,696; May 16, 1972; assigned to American Cyanamid Company Howell, C.F., Hardy, R.A., Jr. and Quinones, N.Q.; U.S. Patent 3,681,357; August 1, 1972; assigned to American Cyanamid Company
logP3.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.171 mg/mLALOGPS
logP2.82ALOGPS
logP3.08ChemAxon
logS-3.3ALOGPS
pKa (Strongest Basic)8.83ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area36.86 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity89.82 m3·mol-1ChemAxon
Polarizability32.82 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-052b-4490000000-6bbd0d2c0c8fe332c636View in MoNA
References
Synthesis Reference

Howell, C.F., Hardy, R.A., Jr. and Quinones, N.Q.; US. Patent 3,663,696; May 16, 1972; assigned to American Cyanamid Company
Howell, C.F., Hardy, R.A., Jr. and Quinones, N.Q.; U.S. Patent 3,681,357; August 1, 1972; assigned to American Cyanamid Company

US3663696
General ReferencesNot Available
External Links
ATC CodesN06AA17
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Amoxapine can be increased when it is combined with Abiraterone.
AcepromazineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Acepromazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Acetophenazine.
AclidiniumAclidinium may increase the anticholinergic activities of Amoxapine.
AltretamineAltretamine may increase the orthostatic hypotensive activities of Amoxapine.
AmisulprideThe risk or severity of adverse effects can be increased when Amoxapine is combined with Amisulpride.
AmphetamineAmoxapine may increase the stimulatory activities of Amphetamine.
AripiprazoleThe risk or severity of adverse effects can be increased when Amoxapine is combined with Aripiprazole.
AzelastineAmoxapine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Amoxapine.
BatimastatThe serum concentration of Amoxapine can be increased when it is combined with Batimastat.
BenzquinamideThe risk or severity of adverse effects can be increased when Amoxapine is combined with Benzquinamide.
Botulinum Toxin Type AAmoxapine may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BAmoxapine may increase the anticholinergic activities of Botulinum Toxin Type B.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.
BuprenorphineAmoxapine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ButabarbitalThe metabolism of Amoxapine can be increased when combined with Butabarbital.
ButethalThe metabolism of Amoxapine can be increased when combined with Butethal.
CarbamazepineThe metabolism of Amoxapine can be increased when combined with Carbamazepine.
CarphenazineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Carphenazine.
CathinoneAmoxapine may increase the stimulatory activities of Cathinone.
ChlormezanoneThe risk or severity of adverse effects can be increased when Amoxapine is combined with Chlormezanone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Chlorpromazine.
ChlorpropamideAmoxapine may increase the hypoglycemic activities of Chlorpropamide.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Amoxapine is combined with Chlorprothixene.
CimetidineThe metabolism of Amoxapine can be decreased when combined with Cimetidine.
Cimetropium BromideAmoxapine may increase the anticholinergic activities of Cimetropium Bromide.
CinacalcetThe serum concentration of Amoxapine can be increased when it is combined with Cinacalcet.
CitalopramThe risk or severity of adverse effects can be increased when Amoxapine is combined with Citalopram.
ClozapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Clozapine.
CobicistatThe serum concentration of Amoxapine can be increased when it is combined with Cobicistat.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Amoxapine.
DarunavirThe serum concentration of Amoxapine can be increased when it is combined with Darunavir.
DesmopressinThe risk or severity of adverse effects can be increased when Amoxapine is combined with Desmopressin.
DexmethylphenidateThe risk or severity of adverse effects can be increased when Dexmethylphenidate is combined with Amoxapine.
DicoumarolAmoxapine may increase the anticoagulant activities of Dicoumarol.
DipivefrinThe therapeutic efficacy of Dipivefrin can be decreased when used in combination with Amoxapine.
DofetilideAmoxapine may increase the QTc-prolonging activities of Dofetilide.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.
DuloxetineDuloxetine may increase the serotonergic activities of Amoxapine.
EluxadolineAmoxapine may increase the activities of Eluxadoline.
EscitalopramThe risk or severity of adverse effects can be increased when Amoxapine is combined with Escitalopram.
EthanolAmoxapine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FencamfamineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Fencamfamine.
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Amoxapine.
FlupentixolThe risk or severity of adverse effects can be increased when Amoxapine is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Amoxapine is combined with Fluspirilene.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Amoxapine.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Amoxapine is combined with Glucagon recombinant.
GoserelinAmoxapine may increase the QTc-prolonging activities of Goserelin.
GranisetronGranisetron may increase the serotonergic activities of Amoxapine.
HaloperidolThe risk or severity of adverse effects can be increased when Amoxapine is combined with Haloperidol.
HeptabarbitalThe metabolism of Amoxapine can be increased when combined with Heptabarbital.
HexobarbitalThe metabolism of Amoxapine can be increased when combined with Hexobarbital.
HydrocodoneAmoxapine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Amoxapine.
Ioflupane I 123Amoxapine may decrease effectiveness of Ioflupane I 123 as a diagnostic agent.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Amoxapine.
IsoflurophateThe serum concentration of Amoxapine can be increased when it is combined with Isoflurophate.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Amoxapine.
LeuprolideAmoxapine may increase the QTc-prolonging activities of Leuprolide.
LinezolidLinezolid may increase the serotonergic activities of Amoxapine.
LiothyronineLiothyronine may increase the arrhythmogenic activities of Amoxapine.
LithiumLithium may increase the neurotoxic activities of Amoxapine.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Amoxapine.
LoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Loxapine.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.
MesoridazineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Mesoridazine.
MethohexitalThe metabolism of Amoxapine can be increased when combined with Methohexital.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Methotrimeprazine.
Methylene blueAmoxapine may increase the serotonergic activities of Methylene blue.
MethylphenidateThe risk or severity of adverse effects can be increased when Methylphenidate is combined with Amoxapine.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Amoxapine.
MetyrosineAmoxapine may increase the sedative activities of Metyrosine.
MianserinMianserin may increase the anticholinergic activities of Amoxapine.
MidodrineAmoxapine may increase the activities of Midodrine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Amoxapine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.
MirabegronThe risk or severity of adverse effects can be increased when Amoxapine is combined with Mirabegron.
MolindoneThe risk or severity of adverse effects can be increased when Amoxapine is combined with Molindone.
MorphineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Morphine.
MoxonidineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Amoxapine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.
NicorandilAmoxapine may increase the hypotensive activities of Nicorandil.
OlanzapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Olanzapine.
OndansetronThe risk or severity of adverse effects can be increased when Amoxapine is combined with Ondansetron.
OrciprenalineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Orciprenaline.
OrphenadrineAmoxapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PaliperidoneThe risk or severity of adverse effects can be increased when Amoxapine is combined with Paliperidone.
PanobinostatThe serum concentration of Amoxapine can be increased when it is combined with Panobinostat.
ParaldehydeAmoxapine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Paroxetine is combined with Amoxapine.
Peginterferon alfa-2bThe serum concentration of Amoxapine can be decreased when it is combined with Peginterferon alfa-2b.
PentobarbitalThe metabolism of Amoxapine can be increased when combined with Pentobarbital.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.
PerphenazineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Perphenazine.
PhenelzinePhenelzine may increase the serotonergic activities of Amoxapine.
PimozideThe risk or severity of adverse effects can be increased when Amoxapine is combined with Pimozide.
PiperacetazineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Piperacetazine.
Potassium ChlorideAmoxapine may increase the ulcerogenic activities of Potassium Chloride.
PramipexoleAmoxapine may increase the sedative activities of Pramipexole.
PramlintidePramlintide may increase the anticholinergic activities of Amoxapine.
PrimidoneThe metabolism of Amoxapine can be increased when combined with Primidone.
ProchlorperazineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Prochlorperazine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Amoxapine.
PromazineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Promazine.
QuetiapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Quetiapine.
QuinidineAmoxapine may increase the QTc-prolonging activities of Quinidine.
RamosetronAmoxapine may increase the activities of Ramosetron.
RemoxiprideThe risk or severity of adverse effects can be increased when Amoxapine is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Reserpine.
RisperidoneThe risk or severity of adverse effects can be increased when Amoxapine is combined with Risperidone.
RitonavirThe metabolism of Amoxapine can be decreased when combined with Ritonavir.
RopiniroleAmoxapine may increase the sedative activities of Ropinirole.
RotigotineAmoxapine may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Amoxapine.
SecobarbitalThe metabolism of Amoxapine can be increased when combined with Secobarbital.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Amoxapine.
SertindoleThe risk or severity of adverse effects can be increased when Amoxapine is combined with Sertindole.
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Amoxapine.
SimeprevirThe serum concentration of Amoxapine can be increased when it is combined with Simeprevir.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.
St. John's WortThe metabolism of Amoxapine can be increased when combined with St. John's Wort.
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Amoxapine.
SuvorexantAmoxapine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TacrineThe therapeutic efficacy of Amoxapine can be decreased when used in combination with Tacrine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Amoxapine.
TerbinafineThe metabolism of Amoxapine can be decreased when combined with Terbinafine.
ThalidomideAmoxapine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThioridazineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Amoxapine is combined with Thiothixene.
TiclopidineThe metabolism of Amoxapine can be decreased when combined with Ticlopidine.
TiotropiumAmoxapine may increase the anticholinergic activities of Tiotropium.
TopiramateThe risk or severity of adverse effects can be increased when Amoxapine is combined with Topiramate.
TramadolAmoxapine may increase the neuroexcitatory activities of Tramadol.
TranylcypromineTranylcypromine may increase the serotonergic activities of Amoxapine.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Amoxapine.
TrifluoperazineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Triflupromazine.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Amoxapine.
Valproic AcidThe serum concentration of Amoxapine can be increased when it is combined with Valproic Acid.
YohimbineThe serum concentration of Yohimbine can be increased when it is combined with Amoxapine.
ZiprasidoneThe risk or severity of adverse effects can be increased when Amoxapine is combined with Ziprasidone.
ZolpidemAmoxapine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Amoxapine is combined with Zuclopenthixol.
Food Interactions
  • Avoid alcohol.
  • Take with food to reduce irritation.

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Norepinephrine:sodium symporter activity
Specific Function:
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A2
Uniprot ID:
P23975
Molecular Weight:
69331.42 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. Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [PubMed:9537821 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Serotonin:sodium symporter activity
Specific Function:
Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into the pre-synaptic terminal for re-utilization. Plays a key role in mediating regulation of the availability of serotonin to other receptors of serotonergic systems. Terminates the action of serotonin an...
Gene Name:
SLC6A4
Uniprot ID:
P31645
Molecular Weight:
70324.165 Da
References
  1. Spurlock G, Buckland P, O'Donovan M, McGuffin P: Lack of effect of antidepressant drugs on the levels of mRNAs encoding serotonergic receptors, synthetic enzymes and 5HT transporter. Neuropharmacology. 1994 Mar-Apr;33(3-4):433-40. [PubMed:7984281 ]
  2. Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [PubMed:9537821 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Potassium channel regulator activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name:
DRD2
Uniprot ID:
P14416
Molecular Weight:
50618.91 Da
References
  1. Wei HB, Niu XY: [Comparison of the affinities of amoxapine and loxapine for various receptors in rat brain and the receptor down-regulation after chronic administration]. Yao Xue Xue Bao. 1990;25(12):881-5. [PubMed:1966571 ]
  2. Nasu R, Matsuo H, Takanaga H, Ohtani H, Sawada Y: Quantitative prediction of catalepsy induced by amoxapine, cinnarizine and cyclophosphamide in mice. Biopharm Drug Dispos. 2000 May;21(4):129-38. [PubMed:11180191 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name:
DRD1
Uniprot ID:
P21728
Molecular Weight:
49292.765 Da
References
  1. Nasu R, Matsuo H, Takanaga H, Ohtani H, Sawada Y: Quantitative prediction of catalepsy induced by amoxapine, cinnarizine and cyclophosphamide in mice. Biopharm Drug Dispos. 2000 May;21(4):129-38. [PubMed:11180191 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 Da
References
  1. Richelson E, Nelson A: Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro. J Pharmacol Exp Ther. 1984 Jul;230(1):94-102. [PubMed:6086881 ]
  2. Buckley NA, McManus PR: Can the fatal toxicity of antidepressant drugs be predicted with pharmacological and toxicological data? Drug Saf. 1998 May;18(5):369-81. [PubMed:9589848 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. Wei HB, Niu XY: [Comparison of the affinities of amoxapine and loxapine for various receptors in rat brain and the receptor down-regulation after chronic administration]. Yao Xue Xue Bao. 1990;25(12):881-5. [PubMed:1966571 ]
  2. Buckley NA, McManus PR: Can the fatal toxicity of antidepressant drugs be predicted with pharmacological and toxicological data? Drug Saf. 1998 May;18(5):369-81. [PubMed:9589848 ]
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. Richelson E: Antimuscarinic and other receptor-blocking properties of antidepressants. Mayo Clin Proc. 1983 Jan;58(1):40-6. [PubMed:6130192 ]
  2. Buckley NA, McManus PR: Can the fatal toxicity of antidepressant drugs be predicted with pharmacological and toxicological data? Drug Saf. 1998 May;18(5):369-81. [PubMed:9589848 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By si...
Gene Name:
GABRA1
Uniprot ID:
P14867
Molecular Weight:
51801.395 Da
References
  1. Buckley NA, McManus PR: Can the fatal toxicity of antidepressant drugs be predicted with pharmacological and toxicological data? Drug Saf. 1998 May;18(5):369-81. [PubMed:9589848 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Virus receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates...
Gene Name:
HTR2A
Uniprot ID:
P28223
Molecular Weight:
52602.58 Da
References
  1. Palvimaki EP, Roth BL, Majasuo H, Laakso A, Kuoppamaki M, Syvalahti E, Hietala J: Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor. Psychopharmacology (Berl). 1996 Aug;126(3):234-40. [PubMed:8876023 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modul...
Gene Name:
HTR2C
Uniprot ID:
P28335
Molecular Weight:
51820.705 Da
References
  1. Glusa E, Pertz HH: Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT(2B) receptors. Br J Pharmacol. 2000 Jun;130(3):692-8. [PubMed:10821800 ]
  2. Goodman, Louis Sanford;Brunton, Laurence L.;Chabner, Bruce;Knollman, Bjorn (2011). The Pharmacological Basis of Therapeutics (12th ed.). McGraw-Hill Professional Publishing. [ISBN:978-0-07-162442-8 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase. It has a high affinity for tricyclic psychotropic drugs (By similarity). Controls pyramidal neurons migration during corticogenesis, through...
Gene Name:
HTR6
Uniprot ID:
P50406
Molecular Weight:
46953.625 Da
References
  1. Roth BL, Craigo SC, Choudhary MS, Uluer A, Monsma FJ Jr, Shen Y, Meltzer HY, Sibley DR: Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J Pharmacol Exp Ther. 1994 Mar;268(3):1403-10. [PubMed:7908055 ]
  2. Goodman, Louis Sanford;Brunton, Laurence L.;Chabner, Bruce;Knollman, Bjorn (2011). The Pharmacological Basis of Therapeutics (12th ed.). McGraw-Hill Professional Publishing. [ISBN:978-0-07-162442-8 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase.
Gene Name:
HTR7
Uniprot ID:
P34969
Molecular Weight:
53554.43 Da
References
  1. Roth BL, Craigo SC, Choudhary MS, Uluer A, Monsma FJ Jr, Shen Y, Meltzer HY, Sibley DR: Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J Pharmacol Exp Ther. 1994 Mar;268(3):1403-10. [PubMed:7908055 ]
  2. Goodman, Louis Sanford;Brunton, Laurence L.;Chabner, Bruce;Knollman, Bjorn (2011). The Pharmacological Basis of Therapeutics (12th ed.). McGraw-Hill Professional Publishing. [ISBN:978-0-07-162442-8 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name:
DRD3
Uniprot ID:
P35462
Molecular Weight:
44224.335 Da
References
  1. Burstein ES, Ma J, Wong S, Gao Y, Pham E, Knapp AE, Nash NR, Olsson R, Davis RE, Hacksell U, Weiner DM, Brann MR: Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist. J Pharmacol Exp Ther. 2005 Dec;315(3):1278-87. Epub 2005 Aug 31. [PubMed:16135699 ]
  2. Goodman, Louis Sanford;Brunton, Laurence L.;Chabner, Bruce;Knollman, Bjorn (2011). The Pharmacological Basis of Therapeutics (12th ed.). McGraw-Hill Professional Publishing. [ISBN:978-0-07-162442-8 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Sh3 domain binding
Specific Function:
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins which inhibit adenylyl cyclase. Modulates the circadian rhythm of contrast sensitivity by regulating the rhythmic expression of NPAS2 in the retinal ganglion cells (By similarity).
Gene Name:
DRD4
Uniprot ID:
P21917
Molecular Weight:
48359.86 Da
References
  1. Burstein ES, Ma J, Wong S, Gao Y, Pham E, Knapp AE, Nash NR, Olsson R, Davis RE, Hacksell U, Weiner DM, Brann MR: Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist. J Pharmacol Exp Ther. 2005 Dec;315(3):1278-87. Epub 2005 Aug 31. [PubMed:16135699 ]
  2. Goodman, Louis Sanford;Brunton, Laurence L.;Chabner, Bruce;Knollman, Bjorn (2011). The Pharmacological Basis of Therapeutics (12th ed.). McGraw-Hill Professional Publishing. [ISBN:978-0-07-162442-8 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Histamine receptor activity
Specific Function:
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
Molecular Weight:
55783.61 Da
References
  1. Richelson E, Nelson A: Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro. J Pharmacol Exp Ther. 1984 Jul;230(1):94-102. [PubMed:6086881 ]
Kind
Protein group
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Components:
NameUniProt IDDetails
Alpha-1A adrenergic receptorP35348 Details
Alpha-1B adrenergic receptorP35368 Details
Alpha-1D adrenergic receptorP25100 Details
References
  1. Richelson E, Nelson A: Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro. J Pharmacol Exp Ther. 1984 Jul;230(1):94-102. [PubMed:6086881 ]
  2. Goodman, Louis Sanford;Brunton, Laurence L.;Chabner, Bruce;Knollman, Bjorn (2011). The Pharmacological Basis of Therapeutics (12th ed.). McGraw-Hill Professional Publishing. [ISBN:978-0-07-162442-8 ]
Kind
Protein group
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.
Components:
NameUniProt IDDetails
Muscarinic acetylcholine receptor M1P11229 Details
Muscarinic acetylcholine receptor M2P08172 Details
Muscarinic acetylcholine receptor M3P20309 Details
Muscarinic acetylcholine receptor M4P08173 Details
Muscarinic acetylcholine receptor M5P08912 Details
References
  1. Richelson E, Nelson A: Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro. J Pharmacol Exp Ther. 1984 Jul;230(1):94-102. [PubMed:6086881 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins ...
Gene Name:
HTR2B
Uniprot ID:
P41595
Molecular Weight:
54297.41 Da
References
  1. Glusa E, Pertz HH: Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT(2B) receptors. Br J Pharmacol. 2000 Jun;130(3):692-8. [PubMed:10821800 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Voltage-gated potassium channel activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses in neurons. It is a cation-specific, but otherwise relatively nonselective, ion channel.
Gene Name:
HTR3A
Uniprot ID:
P46098
Molecular Weight:
55279.835 Da
References
  1. Gozlan H, Saddiki-Traki F, Merahi N, Laguzzi R, Hamon M: [Preclinical pharmacology of amoxapine and amitriptyline. Implications of serotoninergic and opiodergic systems in their central effect in rats]. Encephale. 1991 Dec;17 Spec No 3:415-22. [PubMed:1666997 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
Molecular Weight:
46106.335 Da
References
  1. Gozlan H, Saddiki-Traki F, Merahi N, Laguzzi R, Hamon M: [Preclinical pharmacology of amoxapine and amitriptyline. Implications of serotoninergic and opiodergic systems in their central effect in rats]. Encephale. 1991 Dec;17 Spec No 3:415-22. [PubMed:1666997 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of ...
Gene Name:
HTR1B
Uniprot ID:
P28222
Molecular Weight:
43567.535 Da
References
  1. Gozlan H, Saddiki-Traki F, Merahi N, Laguzzi R, Hamon M: [Preclinical pharmacology of amoxapine and amitriptyline. Implications of serotoninergic and opiodergic systems in their central effect in rats]. Encephale. 1991 Dec;17 Spec No 3:415-22. [PubMed:1666997 ]
Kind
Protein group
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol.
Components:
NameUniProt IDDetails
Alpha-2A adrenergic receptorP08913 Details
Alpha-2B adrenergic receptorP18089 Details
Alpha-2C adrenergic receptorP18825 Details
References
  1. Richelson E, Nelson A: Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro. J Pharmacol Exp Ther. 1984 Jul;230(1):94-102. [PubMed:6086881 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Histamine receptor activity
Specific Function:
The H4 subclass of histamine receptors could mediate the histamine signals in peripheral tissues. Displays a significant level of constitutive activity (spontaneous activity in the absence of agonist).
Gene Name:
HRH4
Uniprot ID:
Q9H3N8
Molecular Weight:
44495.375 Da
References
  1. Lim HD, van Rijn RM, Ling P, Bakker RA, Thurmond RL, Leurs R: Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther. 2005 Sep;314(3):1310-21. Epub 2005 Jun 9. [PubMed:15947036 ]
Kind
Protein group
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By similarity).
Components:
NameUniProt IDDetails
Gamma-aminobutyric acid receptor subunit alpha-1P14867 Details
Gamma-aminobutyric acid receptor subunit alpha-2P47869 Details
Gamma-aminobutyric acid receptor subunit alpha-3P34903 Details
Gamma-aminobutyric acid receptor subunit alpha-4P48169 Details
Gamma-aminobutyric acid receptor subunit alpha-5P31644 Details
Gamma-aminobutyric acid receptor subunit alpha-6Q16445 Details
Gamma-aminobutyric acid receptor subunit beta-1P18505 Details
Gamma-aminobutyric acid receptor subunit beta-2P47870 Details
Gamma-aminobutyric acid receptor subunit beta-3P28472 Details
Gamma-aminobutyric acid receptor subunit deltaO14764 Details
Gamma-aminobutyric acid receptor subunit epsilonP78334 Details
Gamma-aminobutyric acid receptor subunit gamma-1Q8N1C3 Details
Gamma-aminobutyric acid receptor subunit gamma-2P18507 Details
Gamma-aminobutyric acid receptor subunit gamma-3Q99928 Details
Gamma-aminobutyric acid receptor subunit piO00591 Details
Gamma-aminobutyric acid receptor subunit thetaQ9UN88 Details
References
  1. Wei HB, Niu XY: [Comparison of the affinities of amoxapine and loxapine for various receptors in rat brain and the receptor down-regulation after chronic administration]. Yao Xue Xue Bao. 1990;25(12):881-5. [PubMed:1966571 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Monoamine transmembrane transporter activity
Specific Function:
Amine transporter. Terminates the action of dopamine by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A3
Uniprot ID:
Q01959
Molecular Weight:
68494.255 Da
References
  1. Goodman, Louis Sanford;Brunton, Laurence L.;Chabner, Bruce;Knollman, Bjorn (2011). The Pharmacological Basis of Therapeutics (12th ed.). McGraw-Hill Professional Publishing. [ISBN:978-0-07-162442-8 ]
  2. PDSP Ki Database [Link]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Shin HC, Kim HR, Cho HJ, Yi H, Cho SM, Lee DG, Abd El-Aty AM, Kim JS, Sun D, Amidon GL: Comparative gene expression of intestinal metabolizing enzymes. Biopharm Drug Dispos. 2009 Nov;30(8):411-21. doi: 10.1002/bdd.675. [PubMed:19746353 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
no
General Function:
Not Available
Specific Function:
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction.
Gene Name:
ORM1
Uniprot ID:
P02763
Molecular Weight:
23511.38 Da
References
  1. Ferry DG, Caplan NB, Cubeddu LX: Interaction between antidepressants and alpha 1-adrenergic receptor antagonists on the binding to alpha 1-acid glycoprotein. J Pharm Sci. 1986 Feb;75(2):146-9. [PubMed:2870173 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on April 21, 2016 10:11