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Identification
NameFlupentixol
Accession NumberDB00875  (APRD00388)
TypeSmall Molecule
GroupsApproved, Withdrawn
Description

Flupentixol is an antipsychotic neuroleptic drug. It is a thioxanthene, and therefore closely related to the phenothiazines. Its primary use is as a long acting injection given two or three weekly to people with schizophrenia who have a poor compliance with medication and suffer frequent relapses of illness. It is a D1 and D2 receptor antagonist. It is not approved in the United States.

Structure
Thumb
Synonyms
Flupenthixol
Flupenthixole
Flupentixol
Flupentixol
Flupentixol
Flupentixolo
Flupentixolum
External Identifiers
  • FX 703
  • LC 44
  • LU 5-110
  • N 7009
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Fluanxol 0.5mg - Tabtablet0.5 mgoralLundbeck Canada Inc1995-12-31Not applicableCanada
Fluanxol 3mg - Tabtablet3 mgoralLundbeck Canada Inc1995-12-31Not applicableCanada
Fluanxol Depot 10%- Liq Im 100mg/mlsolution100 mgintramuscularLundbeck Canada Inc1995-12-31Not applicableCanada
Fluanxol Depot 2% -liq Im 20mg/mlsolution20 mgintramuscularLundbeck Canada Inc1995-12-31Not applicableCanada
Fluanxol Depot Inj 100mg/mlliquid100 mgintramuscularMerrell Dow Pharmaceuticals (Canada) Inc., Division Of Mmdc1981-12-311996-09-09Canada
Fluanxol Depot Inj 20mg/mlliquid20 mgintramuscularMerrell Dow Pharmaceuticals (Canada) Inc., Division Of Mmdc1981-12-311996-09-09Canada
Fluanxol Tab 0.5mgtablet0.5 mgoralMerrell Dow Pharmaceuticals (Canada) Inc., Division Of Mmdc1986-12-311996-09-09Canada
Fluanxol Tab 3mgtablet3 mgoralMerrell Dow Pharmaceuticals (Canada) Inc., Division Of Mmdc1986-12-311996-09-09Canada
Flupentixol Decanoate Injection BPsolution100 mgintramuscularSandoz Canada Incorporated2009-08-27Not applicableCanada
Flupentixol Decanoate Injection BPsolution20 mgintramuscularSandoz Canada IncorporatedNot applicableNot applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
DepixolLundbeck A/S
FluanxolLundbeck A/S
JexitJohnson
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Flupentixol decanoate
ThumbNot applicableDBSALT000928
Flupentixol dihydrochloride
ThumbNot applicableDBSALT000929
Categories
UNIIFA0UYH6QUO
CAS number2709-56-0
WeightAverage: 436.533
Monoisotopic: 436.179618801
Chemical FormulaC23H27F3N2OS
InChI KeyInChIKey=DTTVNHWDONBIKE-DVZOWYKESA-N
InChI
InChI=1S/C23H27F3N2OS/c24-23(25,26)17-7-8-22-20(16-17)18(19-4-1-2-6-21(19)30-22)5-3-9-27-10-12-28(13-11-27)14-15-29/h1-2,4-8,16,20,22,29H,3,9-15H2/b18-5-
IUPAC Name
2-(4-{3-[2-(trifluoromethyl)-9,9a-dihydro-4aH-thioxanthen-9-ylidene]propyl}piperazin-1-yl)ethan-1-ol
SMILES
[H]C(CCN1CCN(CCO)CC1)=C1C2C=C(C=CC2SC2=C1C=CC=C2)C(F)(F)F
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as thioxanthenes. These are organic polycyclic compounds containing a thioxanthene moiety, which is an aromatic tricycle derived from xanthene by replacing the oxygen atom with a sulfur atom.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzothiopyrans
Sub Class1-benzothiopyrans
Direct ParentThioxanthenes
Alternative Parents
Substituents
  • Thioxanthene
  • Thiochromane
  • Alkylarylthioether
  • N-alkylpiperazine
  • Benzenoid
  • Thiopyran
  • Piperazine
  • 1,4-diazinane
  • Tertiary aliphatic amine
  • Tertiary amine
  • 1,2-aminoalcohol
  • Azacycle
  • Thioether
  • Alkanolamine
  • Hydrocarbon derivative
  • Primary alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Amine
  • Alkyl halide
  • Alkyl fluoride
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor use in the treatment of schizophrenia and depression
PharmacodynamicsFlupenthixol is an anxiolytic, antidepressive agent and a mood stabilizer. It inhibits the central monoamine receptors, particularly the dopamine D1 and D2 receptors. Therefore, it increases the amount of serotonin and noradrenaline that control mood and thinking, and improves mood.
Mechanism of actionFlupenthixol is a thioxanthene antipsychotic. The mechanism of action of Flupenthixol is not completely understood. Flupenthixol is a powerful antagonist of both D1 and D2 dopamine receptors, and an alpha-adrenergic receptor antagonist. It's antipsychotic activity is thought to be related to blocks postsynaptic dopamine receptors in the CNS.
Related Articles
AbsorptionFairly slow and incomplete after oral administration
Volume of distributionNot Available
Protein bindingHighly bound to plasma proteins (>95%)
Metabolism

Mainly hepatic

Route of eliminationNot Available
Half life19 to 39 hours
ClearanceNot Available
ToxicityLD50=300 mk/kg (Oral in mice); LD50=791 mg/kg (Oral in rats); LD50=87 mk/kg (IV in mice); LD50=37 mg/kg (IV in rats)
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+0.9825
Blood Brain Barrier+0.9778
Caco-2 permeable-0.5438
P-glycoprotein substrateSubstrate0.8762
P-glycoprotein inhibitor IInhibitor0.92
P-glycoprotein inhibitor IIInhibitor0.859
Renal organic cation transporterInhibitor0.5065
CYP450 2C9 substrateNon-substrate0.8084
CYP450 2D6 substrateSubstrate0.804
CYP450 3A4 substrateNon-substrate0.6921
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8933
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorInhibitor0.5657
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7748
Ames testNon AMES toxic0.828
CarcinogenicityNon-carcinogens0.8985
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.8385 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6624
hERG inhibition (predictor II)Inhibitor0.7962
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tabletoral0.5 mg
Tabletoral3 mg
Solutionintramuscular100 mg
Solutionintramuscular20 mg
Liquidintramuscular100 mg
Liquidintramuscular20 mg
Prices
Unit descriptionCostUnit
Fluanxol Depot 100 mg/ml39.79USD ml
Fluanxol Depot 20 mg/ml7.96USD ml
Fluanxol 3 mg Tablet0.59USD tablet
Fluanxol 0.5 mg Tablet0.27USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubility0.000346 mg/mlNot Available
logP4.51HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.003 mg/mLALOGPS
logP4.12ALOGPS
logP3.54ChemAxon
logS-5.2ALOGPS
pKa (Strongest Acidic)15.59ChemAxon
pKa (Strongest Basic)8.51ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area26.71 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity120.93 m3·mol-1ChemAxon
Polarizability45.28 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Smith Kline & French Laboratories; British Patent 925,538; May 8, 1963.
Craig, P.N. and Zirkle, C.L.; U.S. Patent 3,282,930; November 1, 1966; assigned to Smith Kline & French Laboratories.

General ReferencesNot Available
External Links
ATC CodesN05AF01
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AclidiniumAclidinium may increase the anticholinergic activities of Flupentixol.
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Flupentixol.
AmisulprideThe risk or severity of adverse effects can be increased when Flupentixol is combined with Amisulpride.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Flupentixol.
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Flupentixol.
AmphetamineFlupentixol may decrease the stimulatory activities of Amphetamine.
AzelastineFlupentixol 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 Flupentixol.
BenzphetamineFlupentixol may decrease the stimulatory activities of Benzphetamine.
Botulinum Toxin Type AFlupentixol may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BFlupentixol may increase the anticholinergic activities of Botulinum Toxin Type B.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Flupentixol.
BromocriptineThe therapeutic efficacy of Flupentixol can be decreased when used in combination with Bromocriptine.
BuprenorphineFlupentixol may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Flupentixol.
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Flupentixol.
CathinoneFlupentixol may decrease the stimulatory activities of Cathinone.
Cimetropium BromideFlupentixol may increase the anticholinergic activities of Cimetropium Bromide.
CitalopramCitalopram may increase the QTc-prolonging activities of Flupentixol.
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Flupentixol.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Flupentixol.
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Flupentixol.
DesvenlafaxineThe risk or severity of adverse effects can be increased when Desvenlafaxine is combined with Flupentixol.
DextroamphetamineFlupentixol may decrease the stimulatory activities of Dextroamphetamine.
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Flupentixol.
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Flupentixol.
DofetilideDofetilide may increase the QTc-prolonging activities of Flupentixol.
DonepezilDonepezil may increase the central neurotoxic activities of Flupentixol.
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Flupentixol.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Flupentixol.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Flupentixol.
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Flupentixol.
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Flupentixol.
EluxadolineFlupentixol may increase the activities of Eluxadoline.
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Flupentixol.
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Flupentixol.
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Flupentixol.
EscitalopramThe risk or severity of adverse effects can be increased when Escitalopram is combined with Flupentixol.
EthanolFlupentixol may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Flupentixol.
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Flupentixol.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Flupentixol.
FrovatriptanThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Flupentixol.
GalantamineGalantamine may increase the central neurotoxic activities of Flupentixol.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Flupentixol is combined with Glucagon recombinant.
GoserelinGoserelin may increase the QTc-prolonging activities of Flupentixol.
HydrocodoneFlupentixol may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Flupentixol.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Flupentixol.
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Flupentixol.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Flupentixol.
IvabradineIvabradine may increase the QTc-prolonging activities of Flupentixol.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Flupentixol.
LevomilnacipranThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Flupentixol.
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Flupentixol.
LisdexamfetamineFlupentixol may decrease the stimulatory activities of Lisdexamfetamine.
LithiumLithium may increase the neurotoxic activities of Flupentixol.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Flupentixol.
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Flupentixol.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Flupentixol.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Flupentixol.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Flupentixol.
MethamphetamineFlupentixol may decrease the stimulatory activities of Methamphetamine.
MethotrimeprazineFlupentixol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethylphenidateThe risk or severity of adverse effects can be increased when Flupentixol is combined with Methylphenidate.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Flupentixol.
MetyrosineFlupentixol may increase the sedative activities of Metyrosine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Flupentixol.
MilnacipranThe risk or severity of adverse effects can be increased when Milnacipran is combined with Flupentixol.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Flupentixol.
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Flupentixol.
MorphineThe risk or severity of adverse effects can be increased when Flupentixol is combined with Morphine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Flupentixol.
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Flupentixol.
NefazodoneThe risk or severity of adverse effects can be increased when Nefazodone is combined with Flupentixol.
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Flupentixol.
OctreotideOctreotide may increase the QTc-prolonging activities of Flupentixol.
OrphenadrineFlupentixol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeFlupentixol may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Flupentixol is combined with Paroxetine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Flupentixol.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Flupentixol.
PhendimetrazineFlupentixol may decrease the stimulatory activities of Phendimetrazine.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Flupentixol.
PhentermineFlupentixol may decrease the stimulatory activities of Phentermine.
Potassium ChlorideFlupentixol may increase the ulcerogenic activities of Potassium Chloride.
PramlintidePramlintide may increase the anticholinergic activities of Flupentixol.
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Flupentixol.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Flupentixol.
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Flupentixol.
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Flupentixol.
QuinagolideThe therapeutic efficacy of Quinagolide can be decreased when used in combination with Flupentixol.
RamosetronFlupentixol may increase the activities of Ramosetron.
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Flupentixol.
RivastigmineRivastigmine may increase the central neurotoxic activities of Flupentixol.
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Flupentixol.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Flupentixol.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Flupentixol.
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Flupentixol.
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Flupentixol.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Flupentixol.
SulpirideThe risk or severity of adverse effects can be increased when Flupentixol is combined with Sulpiride.
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Flupentixol.
SuvorexantFlupentixol may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TacrineThe therapeutic efficacy of Flupentixol can be decreased when used in combination with Tacrine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Flupentixol.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Tedizolid Phosphate is combined with Flupentixol.
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Flupentixol.
ThalidomideFlupentixol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TiotropiumFlupentixol may increase the anticholinergic activities of Tiotropium.
TopiramateThe risk or severity of adverse effects can be increased when Flupentixol is combined with Topiramate.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Flupentixol.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Flupentixol.
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Flupentixol.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Flupentixol.
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Flupentixol.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Flupentixol.
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Flupentixol.
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Flupentixol.
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Flupentixol.
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Flupentixol.
ZolpidemFlupentixol may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • Avoid alcohol.
  • Take with food to reduce irritation.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. [PubMed:11873706 ]
  3. Ogren SO, Hall H, Kohler C, Magnusson O, Lindbom LO, Angeby K, Florvall L: Remoxipride, a new potential antipsychotic compound with selective antidopaminergic actions in the rat brain. Eur J Pharmacol. 1984 Jul 20;102(3-4):459-74. [PubMed:6149133 ]
  4. Arnt J: Differential effects of classical and newer antipsychotics on the hypermotility induced by two dose levels of D-amphetamine. Eur J Pharmacol. 1995 Sep 5;283(1-3):55-62. [PubMed:7498321 ]
  5. Huettl P, Gerhardt GA, Browning MD, Masserano JM: Effects of dopamine receptor agonists and antagonists on catecholamine release in bovine chromaffin cells. J Pharmacol Exp Ther. 1991 May;257(2):567-74. [PubMed:1674528 ]
  6. Nilsson CL, Ekman A, Hellstrand M, Eriksson E: Inverse agonism at dopamine D2 receptors. Haloperidol-induced prolactin release from GH4C1 cells transfected with the human D2 receptor is antagonized by R(-)-n-propylnorapomorphine, raclopride, and phenoxybenzamine. Neuropsychopharmacology. 1996 Jul;15(1):53-61. [PubMed:8797192 ]
  7. Reimold M, Solbach C, Noda S, Schaefer JE, Bartels M, Beneke M, Machulla HJ, Bares R, Glaser T, Wormstall H: Occupancy of dopamine D(1), D (2) and serotonin (2A) receptors in schizophrenic patients treated with flupentixol in comparison with risperidone and haloperidol. Psychopharmacology (Berl). 2007 Feb;190(2):241-9. Epub 2006 Nov 17. [PubMed:17111172 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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. Reimold M, Solbach C, Noda S, Schaefer JE, Bartels M, Beneke M, Machulla HJ, Bares R, Glaser T, Wormstall H: Occupancy of dopamine D(1), D (2) and serotonin (2A) receptors in schizophrenic patients treated with flupentixol in comparison with risperidone and haloperidol. Psychopharmacology (Berl). 2007 Feb;190(2):241-9. Epub 2006 Nov 17. [PubMed:17111172 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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. 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. Cai G, Gurdal H, Smith C, Wang HY, Friedman E: Inverse agonist properties of dopaminergic antagonists at the D(1A) dopamine receptor: uncoupling of the D(1A) dopamine receptor from G(s) protein. Mol Pharmacol. 1999 Nov;56(5):989-96. [PubMed:10531405 ]
  4. Reimold M, Solbach C, Noda S, Schaefer JE, Bartels M, Beneke M, Machulla HJ, Bares R, Glaser T, Wormstall H: Occupancy of dopamine D(1), D (2) and serotonin (2A) receptors in schizophrenic patients treated with flupentixol in comparison with risperidone and haloperidol. Psychopharmacology (Berl). 2007 Feb;190(2):241-9. Epub 2006 Nov 17. [PubMed:17111172 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
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. Golds PR, Przyslo FR, Strange PG: The binding of some antidepressant drugs to brain muscarinic acetylcholine receptors. Br J Pharmacol. 1980 Mar;68(3):541-9. [PubMed:7052344 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Pyridoxal phosphate binding
Specific Function:
Catalyzes the decarboxylation of L-3,4-dihydroxyphenylalanine (DOPA) to dopamine, L-5-hydroxytryptophan to serotonin and L-tryptophan to tryptamine.
Gene Name:
DDC
Uniprot ID:
P20711
Molecular Weight:
53925.815 Da
References
  1. Zhu MY, Juorio AV, Paterson IA, Boulton AA: Regulation of aromatic L-amino acid decarboxylase in rat striatal synaptosomes: effects of dopamine receptor agonists and antagonists. Br J Pharmacol. 1994 May;112(1):23-30. [PubMed:7913379 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Hait WN, Gesmonde JF, Murren JR, Yang JM, Chen HX, Reiss M: Terfenadine (Seldane): a new drug for restoring sensitivity to multidrug resistant cancer cells. Biochem Pharmacol. 1993 Jan 26;45(2):401-6. [PubMed:8094615 ]
  2. Dey S, Hafkemeyer P, Pastan I, Gottesman MM: A single amino acid residue contributes to distinct mechanisms of inhibition of the human multidrug transporter by stereoisomers of the dopamine receptor antagonist flupentixol. Biochemistry. 1999 May 18;38(20):6630-9. [PubMed:10350482 ]
  3. Hafkemeyer P, Licht T, Pastan I, Gottesman MM: Chemoprotection of hematopoietic cells by a mutant P-glycoprotein resistant to a potent chemosensitizer of multidrug-resistant cancers. Hum Gene Ther. 2000 Mar 1;11(4):555-65. [PubMed:10724034 ]
  4. Yang JM, Vassil A, Hait WN: Involvement of phosphatidylinositol-3-kinase in membrane ruffling induced by P-glycoprotein substrates in multidrug-resistant carcinoma cells. Biochem Pharmacol. 2002 Mar 1;63(5):959-66. [PubMed:11911848 ]
  5. Ford JM, Bruggemann EP, Pastan I, Gottesman MM, Hait WN: Cellular and biochemical characterization of thioxanthenes for reversal of multidrug resistance in human and murine cell lines. Cancer Res. 1990 Mar 15;50(6):1748-56. [PubMed:1968358 ]
  6. Ford JM, Yang JM, Hait WN: Effect of buthionine sulfoximine on toxicity of verapamil and doxorubicin to multidrug resistant cells and to mice. Cancer Res. 1991 Jan 1;51(1):67-72. [PubMed:1988108 ]
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Drug created on June 13, 2005 07:24 / Updated on September 22, 2015 13:36