You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameThiethylperazine
Accession NumberDB00372  (APRD00323)
TypeSmall Molecule
GroupsWithdrawn
DescriptionA dopamine antagonist that is particularly useful in treating the nausea and vomiting associated with anesthesia, mildly emetic cancer chemotherapy agents, radiation therapy, and toxins. This piperazine phenothiazine does not prevent vertigo or motion sickness. (From AMA Drug Evaluations Annual, 1994, p457)
Structure
Thumb
Synonyms
2-(ethylthio)-10-[3-(4-methylpiperazin-1-yl)propyl]-10H-phenothiazine
Norzine
Thiethylperazin
Thiéthylpérazine
Thiethylperazine
Thiethylperazinum
Tietilperazina
External Identifiers
  • GS 95
  • NSC 130044
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
TorecanKrka
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Thiethylperazine malate
ThumbNot applicableDBSALT001328
Thiethylperazine maleate
ThumbNot applicableDBSALT001059
Categories
UNII8ETK1WAF6R
CAS number1420-55-9
WeightAverage: 399.616
Monoisotopic: 399.180289323
Chemical FormulaC22H29N3S2
InChI KeyXCTYLCDETUVOIP-UHFFFAOYSA-N
InChI
InChI=1S/C22H29N3S2/c1-3-26-18-9-10-22-20(17-18)25(19-7-4-5-8-21(19)27-22)12-6-11-24-15-13-23(2)14-16-24/h4-5,7-10,17H,3,6,11-16H2,1-2H3
IUPAC Name
2-(ethylsulfanyl)-10-[3-(4-methylpiperazin-1-yl)propyl]-10H-phenothiazine
SMILES
CCSC1=CC2=C(SC3=CC=CC=C3N2CCCN2CCN(C)CC2)C=C1
Pharmacology
IndicationFor the treatment or relief of nausea and vomiting.
Structured Indications Not Available
PharmacodynamicsThiethylperazine, an atypical antipsychotic agent, is used to treat both negative and positive symptoms of schizophrenia, acute mania with bipolar disorder, agitation, and psychotic symptoms in dementia. Future uses may include the treatment of obsessive-compulsive disorder and severe behavioral disorders in autism. Structurally and pharmacologically similar to clozapine, Thiethylperazine binds to alpha(1), dopamine, histamine H1, muscarinic, and serotonin type 2 (5-HT2) receptors.
Mechanism of actionThiethylperazine is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors. Thiethylperazine's antipsychotic effect is due to antagonism at dopamine and serotonin type 2 receptors, with greater activity at serotonin 5-HT2 receptors than at dopamine type-2 receptors. This may explain the lack of extrapyramidal effects. Thiethylperazine does not appear to block dopamine within the tubero-infundibular tract, explaining the lower incidence of hyperprolactinemia than with typical antipsychotic agents or risperidone. Antagonism at muscarinic receptors, H1-receptors, and alpha(1)-receptors also occurs with thiethylperazine.
TargetKindPharmacological actionActionsOrganismUniProt ID
D(2) dopamine receptorProteinunknown
antagonist
HumanP14416 details
D(1A) dopamine receptorProteinunknown
antagonist
HumanP21728 details
D(4) dopamine receptorProteinunknown
antagonist
HumanP21917 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein binding60%
MetabolismNot Available
Route of eliminationThiethylperazine is eliminated in the urine.
Half lifeNot Available
ClearanceNot Available
ToxicityManifestations of acute overdosage of TORECAN (thiethylperazine) can be expected to reflect the CNS effects of the drug and include extrapyramidal symptoms (E.P.S), confusion and convulsions with reduced or absent reflexes, respiratory depression and hypotension.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
5'-Deoxy-5'-MethylthioadenosineThe serum concentration of Thiethylperazine can be increased when it is combined with 5'-Deoxy-5'-Methylthioadenosine.Experimental
AcebutololThiethylperazine may increase the hypotensive activities of Acebutolol.Approved
AlfentanilThiethylperazine may increase the hypotensive activities of Alfentanil.Approved, Illicit
AlphacetylmethadolThiethylperazine may increase the hypotensive activities of Alphacetylmethadol.Experimental, Illicit
AlprenololThiethylperazine may increase the hypotensive activities of Alprenolol.Approved, Withdrawn
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of Thiethylperazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Aluminum phosphateAluminum phosphate can cause a decrease in the absorption of Thiethylperazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
AmodiaquineThe serum concentration of Thiethylperazine can be increased when it is combined with Amodiaquine.Approved
AmoxapineThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Amoxapine.Approved
Aop200704Thiethylperazine may increase the hypotensive activities of Aop200704.Investigational
ArotinololThiethylperazine may increase the hypotensive activities of Arotinolol.Approved
ArtemetherThe serum concentration of Thiethylperazine can be increased when it is combined with Artemether.Approved
ArtemisininThe serum concentration of Thiethylperazine can be increased when it is combined with Artemisinin.Investigational
ArtesunateThe serum concentration of Thiethylperazine can be increased when it is combined with Artesunate.Approved
AtenololThiethylperazine may increase the hypotensive activities of Atenolol.Approved
AtovaquoneThe serum concentration of Thiethylperazine can be increased when it is combined with Atovaquone.Approved
BefunololThiethylperazine may increase the hypotensive activities of Befunolol.Experimental
BetaxololThiethylperazine may increase the hypotensive activities of Betaxolol.Approved
Betulinic AcidThe serum concentration of Thiethylperazine can be increased when it is combined with Betulinic Acid.Investigational
BevantololThiethylperazine may increase the hypotensive activities of Bevantolol.Approved
BezitramideThiethylperazine may increase the hypotensive activities of Bezitramide.Experimental, Illicit, Withdrawn
Bismuth SubcitrateBismuth Subcitrate can cause a decrease in the absorption of Thiethylperazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
BisoprololThiethylperazine may increase the hypotensive activities of Bisoprolol.Approved
BopindololThiethylperazine may increase the hypotensive activities of Bopindolol.Approved
BucindololThiethylperazine may increase the hypotensive activities of Bucindolol.Investigational
BufuralolThiethylperazine may increase the hypotensive activities of Bufuralol.Experimental, Investigational
BupranololThiethylperazine may increase the hypotensive activities of Bupranolol.Approved
BuprenorphineThiethylperazine may increase the hypotensive activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
ButorphanolThiethylperazine may increase the hypotensive activities of Butorphanol.Approved, Illicit, Vet Approved
Calcium carbonateCalcium carbonate can cause a decrease in the absorption of Thiethylperazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
CarfentanilThiethylperazine may increase the hypotensive activities of Carfentanil.Illicit, Vet Approved
CarteololThiethylperazine may increase the hypotensive activities of Carteolol.Approved
CarvedilolThiethylperazine may increase the hypotensive activities of Carvedilol.Approved, Investigational
CeliprololThiethylperazine may increase the hypotensive activities of Celiprolol.Approved, Investigational
ChloroquineThe serum concentration of Thiethylperazine can be increased when it is combined with Chloroquine.Approved, Vet Approved
CitalopramThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Citalopram.Approved
ClomipramineThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Clomipramine.Approved, Vet Approved
CodeineThiethylperazine may increase the hypotensive activities of Codeine.Approved, Illicit
DapoxetineThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Dapoxetine.Investigational
DapsoneThe serum concentration of Thiethylperazine can be increased when it is combined with Dapsone.Approved, Investigational
DextromoramideThiethylperazine may increase the hypotensive activities of Dextromoramide.Experimental, Illicit
DextropropoxypheneThiethylperazine may increase the hypotensive activities of Dextropropoxyphene.Approved, Illicit, Withdrawn
DezocineThiethylperazine may increase the hypotensive activities of Dezocine.Approved
DihydroartemisininThe serum concentration of Thiethylperazine can be increased when it is combined with Dihydroartemisinin.Approved
DihydrocodeineThiethylperazine may increase the hypotensive activities of Dihydrocodeine.Approved, Illicit
DihydroetorphineThiethylperazine may increase the hypotensive activities of Dihydroetorphine.Experimental, Illicit
DihydromorphineThiethylperazine may increase the hypotensive activities of Dihydromorphine.Experimental, Illicit
DiphenoxylateThiethylperazine may increase the hypotensive activities of Diphenoxylate.Approved, Illicit
DoxycyclineThe serum concentration of Thiethylperazine can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DPDPEThiethylperazine may increase the hypotensive activities of DPDPE.Investigational
EscitalopramThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Escitalopram.Approved, Investigational
EsmololThiethylperazine may increase the hypotensive activities of Esmolol.Approved
EthylmorphineThiethylperazine may increase the hypotensive activities of Ethylmorphine.Approved, Illicit
EtoperidoneThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Etoperidone.Approved
EtorphineThiethylperazine may increase the hypotensive activities of Etorphine.Illicit, Vet Approved
FenfluramineThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Fenfluramine.Illicit, Withdrawn
FentanylThiethylperazine may increase the hypotensive activities of Fentanyl.Approved, Illicit, Investigational, Vet Approved
FluoxetineThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Fluoxetine.Approved, Vet Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Fluvoxamine.Approved, Investigational
HalofantrineThe serum concentration of Thiethylperazine can be increased when it is combined with Halofantrine.Approved
HeroinThiethylperazine may increase the hypotensive activities of Heroin.Approved, Illicit
HydrocodoneThiethylperazine may increase the hypotensive activities of Hydrocodone.Approved, Illicit
HydromorphoneThiethylperazine may increase the hypotensive activities of Hydromorphone.Approved, Illicit
HydroxychloroquineThe serum concentration of Thiethylperazine can be increased when it is combined with Hydroxychloroquine.Approved
IndalpineThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Indalpine.Investigational, Withdrawn
IndenololThiethylperazine may increase the hypotensive activities of Indenolol.Withdrawn
KetobemidoneThiethylperazine may increase the hypotensive activities of Ketobemidone.Approved
LabetalolThiethylperazine may increase the hypotensive activities of Labetalol.Approved
LevobunololThiethylperazine may increase the hypotensive activities of Levobunolol.Approved
Levomethadyl AcetateThiethylperazine may increase the hypotensive activities of Levomethadyl Acetate.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Levomilnacipran.Approved
LevorphanolThiethylperazine may increase the hypotensive activities of Levorphanol.Approved
LofentanilThiethylperazine may increase the hypotensive activities of Lofentanil.Illicit
Lu AA21004The risk or severity of adverse effects can be increased when Thiethylperazine is combined with Lu AA21004.Investigational
LumefantrineThe serum concentration of Thiethylperazine can be increased when it is combined with Lumefantrine.Approved
MagaldrateMagaldrate can cause a decrease in the absorption of Thiethylperazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Withdrawn
Magnesium carbonateMagnesium carbonate can cause a decrease in the absorption of Thiethylperazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium hydroxideMagnesium hydroxide can cause a decrease in the absorption of Thiethylperazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium oxideMagnesium oxide can cause a decrease in the absorption of Thiethylperazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium TrisilicateMagnesium Trisilicate can cause a decrease in the absorption of Thiethylperazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
MefloquineThe serum concentration of Thiethylperazine can be increased when it is combined with Mefloquine.Approved
MethadoneThiethylperazine may increase the hypotensive activities of Methadone.Approved
Methadyl AcetateThiethylperazine may increase the hypotensive activities of Methadyl Acetate.Approved, Illicit
MetipranololThiethylperazine may increase the hypotensive activities of Metipranolol.Approved
MetoprololThiethylperazine may increase the hypotensive activities of Metoprolol.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Milnacipran.Approved
MizoribineThe serum concentration of Thiethylperazine can be increased when it is combined with Mizoribine.Investigational
MorphineThiethylperazine may increase the hypotensive activities of Morphine.Approved, Investigational
NadololThiethylperazine may increase the hypotensive activities of Nadolol.Approved
NalbuphineThiethylperazine may increase the hypotensive activities of Nalbuphine.Approved
NormethadoneThiethylperazine may increase the hypotensive activities of Normethadone.Approved, Illicit
OlanzapineThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Olanzapine.Approved, Investigational
OpiumThiethylperazine may increase the hypotensive activities of Opium.Approved, Illicit
OxprenololThiethylperazine may increase the hypotensive activities of Oxprenolol.Approved
OxycodoneThiethylperazine may increase the hypotensive activities of Oxycodone.Approved, Illicit, Investigational
OxymorphoneThiethylperazine may increase the hypotensive activities of Oxymorphone.Approved, Investigational, Vet Approved
ParoxetineThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Paroxetine.Approved, Investigational
PenbutololThiethylperazine may increase the hypotensive activities of Penbutolol.Approved, Investigational
PentazocineThiethylperazine may increase the hypotensive activities of Pentazocine.Approved, Vet Approved
PethidineThiethylperazine may increase the hypotensive activities of Pethidine.Approved
PindololThiethylperazine may increase the hypotensive activities of Pindolol.Approved
PiritramideThiethylperazine may increase the hypotensive activities of Piritramide.Investigational
PractololThiethylperazine may increase the hypotensive activities of Practolol.Approved
PrimaquineThe serum concentration of Thiethylperazine can be increased when it is combined with Primaquine.Approved
ProguanilThe serum concentration of Thiethylperazine can be increased when it is combined with Proguanil.Approved
PropranololThiethylperazine may increase the hypotensive activities of Propranolol.Approved, Investigational
PyrimethamineThe serum concentration of Thiethylperazine can be increased when it is combined with Pyrimethamine.Approved, Vet Approved
PyronaridineThe serum concentration of Thiethylperazine can be increased when it is combined with Pyronaridine.Investigational
QuinacrineThe serum concentration of Thiethylperazine can be increased when it is combined with Quinacrine.Approved
QuinidineThe serum concentration of Thiethylperazine can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Thiethylperazine can be increased when it is combined with Quinine.Approved
RadicicolThe serum concentration of Thiethylperazine can be increased when it is combined with Radicicol.Experimental
RemifentanilThiethylperazine may increase the hypotensive activities of Remifentanil.Approved
SertralineThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Sertraline.Approved
SinefunginThe serum concentration of Thiethylperazine can be increased when it is combined with Sinefungin.Experimental
SotalolThiethylperazine may increase the hypotensive activities of Sotalol.Approved
SufentanilThiethylperazine may increase the hypotensive activities of Sufentanil.Approved, Investigational
SulfadoxineThe serum concentration of Thiethylperazine can be increased when it is combined with Sulfadoxine.Approved
SulfametopyrazineThe serum concentration of Thiethylperazine can be increased when it is combined with Sulfametopyrazine.Approved, Withdrawn
tafenoquineThe serum concentration of Thiethylperazine can be increased when it is combined with tafenoquine.Investigational
TapentadolThiethylperazine may increase the hypotensive activities of Tapentadol.Approved
ThiopentalThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Thiopental.Approved, Vet Approved
TimololThiethylperazine may increase the hypotensive activities of Timolol.Approved
TramadolThiethylperazine may increase the hypotensive activities of Tramadol.Approved, Investigational
TrazodoneThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Trazodone.Approved, Investigational
TrimethoprimThe serum concentration of Thiethylperazine can be increased when it is combined with Trimethoprim.Approved, Vet Approved
VilazodoneThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Vilazodone.Approved
VortioxetineThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Vortioxetine.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Thiethylperazine is combined with Zimelidine.Withdrawn
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Maurer H, Pfleger K: Identification of phenothiazine antihistamines and their metabolites in urine. Arch Toxicol. 1988;62(2-3):185-91. [PubMed:2904251 ]
External Links
ATC CodesR06AD03
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9558
Blood Brain Barrier+0.9847
Caco-2 permeable+0.748
P-glycoprotein substrateSubstrate0.8705
P-glycoprotein inhibitor IInhibitor0.8683
P-glycoprotein inhibitor IIInhibitor0.6434
Renal organic cation transporterInhibitor0.715
CYP450 2C9 substrateNon-substrate0.8381
CYP450 2D6 substrateSubstrate0.7491
CYP450 3A4 substrateNon-substrate0.607
CYP450 1A2 substrateInhibitor0.9159
CYP450 2C9 inhibitorNon-inhibitor0.8968
CYP450 2D6 inhibitorInhibitor0.943
CYP450 2C19 inhibitorNon-inhibitor0.5565
CYP450 3A4 inhibitorNon-inhibitor0.7657
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.684
Ames testNon AMES toxic0.885
CarcinogenicityNon-carcinogens0.9366
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5624 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9258
hERG inhibition (predictor II)Inhibitor0.8292
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Novartis pharmaceuticals corp
Packagers
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point62-64 °CPhysProp
boiling point227 °C at 1.00E-02 mm HgPhysProp
water solubility0.0584 mg/LNot Available
logP5.41HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.00487 mg/mLALOGPS
logP5.12ALOGPS
logP4.66ChemAxon
logS-4.9ALOGPS
pKa (Strongest Basic)8.4ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area9.72 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity122.56 m3·mol-1ChemAxon
Polarizability46.53 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
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 organic compounds known as phenothiazines. These are polycyclic aromatic compounds containing a phenothiazine moiety, which is a linear tricyclic system that consists of a two benzene rings joined by a para-thiazine ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzothiazines
Sub ClassPhenothiazines
Direct ParentPhenothiazines
Alternative Parents
Substituents
  • Phenothiazine
  • Alkyldiarylamine
  • Diarylthioether
  • Alkylarylthioether
  • N-alkylpiperazine
  • N-methylpiperazine
  • Benzenoid
  • Piperazine
  • 1,4-diazinane
  • Para-thiazine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Sulfenyl compound
  • Thioether
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

Targets

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. 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. Briani C, Cagnin A, Chierichetti F, Tiberio M, Battistin L, Pizzolato G: Thiethylperazine-induced parkinsonism: in vivo demonstration of dopamine D2 receptors blockade. Eur J Neurol. 2004 Oct;11(10):709-10. [PubMed:15469457 ]
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. 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:
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. 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 ]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23