Identification

Name
Zuclopenthixol
Accession Number
DB01624  (DB08919, DB08920)
Type
Small Molecule
Groups
Approved, Investigational
Description

Zuclopenthixol, also known as Zuclopentixol or Zuclopenthixolum, is an antipsychotic agent. Zuclopenthixol is a thioxanthene-based neuroleptic with therapeutic actions similar to the phenothiazine antipsychotics. It is an antagonist at D1 and D2 dopamine receptors. Major brands of zuclopenthixol are Cisordinol, Acuphase, and Clopixol. This drug is a liquid. This compound belongs to the 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. Known drug targets of zuclopenthixol include 5-hydroxytryptamine receptor 2A, D(1B) dopamine receptor, D(2) dopamine receptor, D(1A) dopamine receptor, and alpha-1A adrenergic receptor. It is known that zuclopenthixol is metabolized by Cytochrome P450 2D6. Zuclopenthixol was approved for use in Canada in 2011, but is not approved for use in the United States.

Structure
Thumb
Synonyms
  • cis-Clopenthixol
  • Zuclopenthixol
  • Zuclopenthixolum
  • Zuclopentixol
External IDs
N05AF05
Product Ingredients
IngredientUNIICASInChI Key
Zuclopenthixol acetate349S2ZHF0585721-05-7OXAUOBQMCDIVPQ-IOXNKQMXSA-N
Zuclopenthixol decanoateTSS9KIZ5OG64053-00-5QRUAPADZILXULG-WKIKZPBSSA-N
Zuclopenthixol dihydrochloride7042692VYN58045-23-1LPWNZMIBFHMYMX-MHKBYHAFSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Clopixol - Tab 10mgTablet10 mgOralHoechst Marion Roussel1995-12-311999-08-11Canada
Clopixol - Tab 25mgTablet25 mgOralHoechst Marion Roussel1995-12-311999-08-11Canada
Clopixol - Tab 40mgTablet40 mgOralHoechst Marion Roussel1995-12-311999-08-11Canada
Clopixol Acuphase - Liq Im 50mg/mlLiquid50 mgIntramuscularHoechst Marion Roussel1995-12-311999-08-11Canada
Clopixol Depot - Liq Im 200mg/mlLiquid200 mgIntramuscularHoechst Marion Roussel1995-12-311999-08-11Canada
Clopixol Depot - Liq Im 500mg/mlLiquid500 mgIntramuscularHoechst Marion Roussel1995-12-311999-08-11Canada
Clopixol Depot 200mg/mlSolution200 mgIntramuscularLundbeck Inc.1997-05-02Not applicableCanada
Clopixol Depot 500mg/mlLiquid500 mgIntramuscularLundbeck Inc.Not applicableNot applicableCanada
Clopixol Tablets 10mgTablet10 mgOralLundbeck Inc.1997-05-02Not applicableCanada
Clopixol Tablets 25mgTablet25 mgOralLundbeck Inc.1997-05-02Not applicableCanada
International/Other Brands
Acuphase (H. Lundbeck A/S) / Ciatyl-Z (Bayer Vital) / Cisordinol (H. Lundbeck A/S) / Clopixol (H. Lundbeck A/S)
Categories
UNII
47ISU063SG
CAS number
53772-83-1
Weight
Average: 400.965
Monoisotopic: 400.137611829
Chemical Formula
C22H25ClN2OS
InChI Key
WFPIAZLQTJBIFN-DVZOWYKESA-N
InChI
InChI=1S/C22H25ClN2OS/c23-17-7-8-22-20(16-17)18(19-4-1-2-6-21(19)27-22)5-3-9-24-10-12-25(13-11-24)14-15-26/h1-2,4-8,16,26H,3,9-15H2/b18-5-
IUPAC Name
2-(4-{3-[(9Z)-2-chloro-9H-thioxanthen-9-ylidene]propyl}piperazin-1-yl)ethan-1-ol
SMILES
OCCN1CCN(CC\C=C2\C3=CC=CC=C3SC3=C2C=C(Cl)C=C3)CC1

Pharmacology

Indication

Used in the management of acute psychoses such as mania or schizophrenia. However, the use of zuclopenthixol acetate in psychiatric emergencies as an alternative to standard treatments (haloperidol, clotiapine, etc.) should be cautioned, since well executed and documented trials of zuclopenthixol acetate for this use have yet to be conducted. Zuclopenthixol acetate is not intended for long-term use.

Associated Conditions
Pharmacodynamics

Zuclopenthixol is a thioxanthene with therapeutic actions similar to the phenothiazine antipsychotics. It is an antagonist at D1 and D2 dopamine receptors.

Mechanism of action

Zuclopenthixol is a typical antipsychotic neuroleptic drug of the thioxanthene class. It mainly acts by antagonism of D1 and D2 dopamine receptors. Zuclopenthixol also has high affinity for alpha1-adrenergic and 5-HT2 receptors. It has weaker histamine H1 receptor blocking activity, and even lower affinity for muscarinic cholinergic and alpha2-adrenergic receptors.

TargetActionsOrganism
AD(1A) dopamine receptor
antagonist
Human
AD(1B) dopamine receptor
antagonist
Human
AD(2) dopamine receptor
antagonist
Human
UAlpha-1A adrenergic receptor
antagonist
Human
UAlpha-2A adrenergic receptor
antagonist
Human
U5-hydroxytryptamine receptor 2A
antagonist
Human
UHistamine H1 receptor
antagonist
Human
Absorption

Upon reaching the body water phase, the decanoate ester is slowly released from the oil depot, which is resultantly hydrolyzed to the active substance, zuclopenthixol. The decanoate ester provides a means of slow release since zuclopenthixol itself is a short-acting drug.

Volume of distribution

20 L/kg.

Protein binding

98-99%

Metabolism

The metabolism of zuclopenthixol is mainly by sulphoxidation, side chain N-dealkylation and glucuronic acid conjugation. The metabolites are devoid of pharmacological activity.

Route of elimination

Primarily in the feces with approximately 10% in the urine.

Half life

20 hours (range 12-28 hours) for the tablet form, 19 days for the depot form.

Clearance

approximately 0.9 L/min.

Toxicity

Although there have not been any cases of overdosage reported, the symptoms are likely to be somnolence, coma, extrapyramidal symptoms, convulsions, hypotension, shock, or hyper- or hypothermia.

Neuroleptic malignant syndrome may occur. Zuclopenthixol may potentiate anticholinergic effects of concurrent medications. Zuclopenthixol has a demonstrated antiemetic effect in animals, and may mask signs of toxicity due to other drug overdoses, or may mask symptoms of disease.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Cytochrome P450 2D6CYP2D6*3Not AvailableC alleleEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*4Not AvailableC alleleEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*5Not AvailableWhole-gene deletionEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*6Not Available1707delTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*7Not Available2935A>CEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*8Not Available1758G>TEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*11Not Available883G>CEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*12Not Available124G>AEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*13Not AvailableCYP2D7/2D6 hybrid gene structureEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*14ANot Available1758G>AEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*15Not Available137insT, 137_138insTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*19Not Available2539_2542delAACTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*20Not Available1973_1974insGEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*21Not Available2573insCEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*31Not Available-1770G>A / -1584C>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*36Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*38Not Available2587_2590delGACTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*40Not Available1863_1864ins(TTT CGC CCC)2Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*42Not Available3259_3260insGTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*44Not Available2950G>CEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*47Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*51Not Available-1584C>G / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*56Not Available3201C>TEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*57Not Available100C>T / 310G>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*62Not Available4044C>TEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*68ANot Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*68BNot AvailableSimilar but not identical switch region compared to CYP2D6*68A. Found in tandem arrangement with CYP2D6*4.Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*69Not Available2988G>A / -1426C>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*92Not Available1995delCEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*100Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*101Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details

Interactions

Drug Interactions
DrugInteraction
2,5-Dimethoxy-4-ethylamphetamineZuclopenthixol may decrease the stimulatory activities of 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineZuclopenthixol may decrease the stimulatory activities of 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-MethylenedioxyamphetamineZuclopenthixol may decrease the stimulatory activities of 3,4-Methylenedioxyamphetamine.
4-Bromo-2,5-dimethoxyamphetamineZuclopenthixol may decrease the stimulatory activities of 4-Bromo-2,5-dimethoxyamphetamine.
4-MethoxyamphetamineZuclopenthixol may decrease the vasoconstricting activities of 4-Methoxyamphetamine.
7-NitroindazoleThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with 7-Nitroindazole.
AbirateroneThe serum concentration of Zuclopenthixol can be increased when it is combined with Abiraterone.
AcebutololAcebutolol may increase the orthostatic hypotensive activities of Zuclopenthixol.
AcepromazineZuclopenthixol may increase the antihypertensive activities of Acepromazine.
AceprometazineThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Aceprometazine.
Food Interactions
Not Available

References

General References
  1. Khalifa AE: Zuclopenthixol facilitates memory retrieval in rats: possible involvement of noradrenergic and serotonergic mechanisms. Pharmacol Biochem Behav. 2003 Jul;75(4):755-62. [PubMed:12957216]
  2. Fond G, Macgregor A, Tamouza R, Hamdani N, Meary A, Leboyer M, Dubremetz JF: Comparative analysis of anti-toxoplasmic activity of antipsychotic drugs and valproate. Eur Arch Psychiatry Clin Neurosci. 2014 Mar;264(2):179-83. doi: 10.1007/s00406-013-0413-4. Epub 2013 Jun 15. [PubMed:23771405]
  3. Jayakody K, Gibson RC, Kumar A, Gunadasa S: Zuclopenthixol acetate for acute schizophrenia and similar serious mental illnesses. Cochrane Database Syst Rev. 2012 Apr 18;4:CD000525. doi: 10.1002/14651858.CD000525.pub3. [PubMed:22513898]
  4. Nielsen MK, Johansen SS: Simultaneous determination of 25 common pharmaceuticals in whole blood using ultra-performance liquid chromatography-tandem mass spectrometry. J Anal Toxicol. 2012 Sep;36(7):497-506. doi: 10.1093/jat/bks054. Epub 2012 Jun 19. [PubMed:22718540]
  5. Khalifa AE: Pro-oxidant activity of zuclopenthixol in vivo: differential effect of the drug on brain oxidative status of scopolamine-treated rats. Hum Exp Toxicol. 2004 Aug;23(9):439-45. [PubMed:15497819]
  6. Hood S, Orr K, Bennett L, Davies S: Severe laryngeal dystonia in a patient receiving zuclopenthixol "Acuphase" and fluoxetine. Australas Psychiatry. 2010 Apr;18(2):174-6. doi: 10.3109/10398560903473686. [PubMed:20175668]
  7. Link [Link]
  8. Link [Link]
External Links
Human Metabolome Database
HMDB0015561
KEGG Drug
D03556
PubChem Compound
5311507
PubChem Substance
46507341
ChemSpider
4470984
BindingDB
79209
ChEBI
51364
ChEMBL
CHEMBL53904
Therapeutic Targets Database
DAP000845
PharmGKB
PA452629
Drugs.com
Drugs.com Drug Page
Wikipedia
Zuclopenthixol
ATC Codes
N05AF05 — Zuclopenthixol
AHFS Codes
  • 28:16.08.32 — Thioxanthenes
FDA label
Download (229 KB)
MSDS
Download (568 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
3Unknown StatusTreatmentPsychosis Nos/Other1
4CompletedTreatmentSchizoaffective Disorders / Schizophrenia and Disorders With Psychotic Features / Schizophrenic Disorders1
4TerminatedTreatmentBipolar Disorder (BD)1
Not AvailableCompletedNot AvailableBipolar Disorder (BD) / Psychotic Disorder NOS / Schizoaffective Disorders / Schizophrenic Disorders / Type 2 Diabetes Mellitus1
Not AvailableCompletedDiagnosticSchizophrenic Disorders1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
TabletOral40 mg
LiquidIntramuscular50 mg
LiquidIntramuscular200 mg
LiquidIntramuscular500 mg
SolutionIntramuscular200 mg
TabletOral10 mg
TabletOral25 mg
SolutionIntramuscular50 mg
Prices
Unit descriptionCostUnit
Clopixol Acuphase 50 mg/ml16.52USD ml
Clopixol Depot 200 mg/ml16.52USD ml
Clopixol 25 mg Tablet1.06USD tablet
Clopixol 10 mg Tablet0.42USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)~50http://www.lundbeck.com/upload/ca/en/files/pdf/product_monograph/Clopixol_PM_MKT_ctrl_148975_13SEPT2011_CLN_eng.pdf
water solubilityslighthttp://www.lundbeck.com/upload/ca/en/files/pdf/product_monograph/Clopixol_PM_MKT_ctrl_148975_13SEPT2011_CLN_eng.pdf
Predicted Properties
PropertyValueSource
Water Solubility0.0026 mg/mLALOGPS
logP4.46ALOGPS
logP4.22ChemAxon
logS-5.2ALOGPS
pKa (Strongest Acidic)15.59ChemAxon
pKa (Strongest Basic)8.43ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area26.71 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity127 m3·mol-1ChemAxon
Polarizability45.29 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9443
Blood Brain Barrier+0.9676
Caco-2 permeable-0.5313
P-glycoprotein substrateSubstrate0.8762
P-glycoprotein inhibitor IInhibitor0.8736
P-glycoprotein inhibitor IIInhibitor0.7439
Renal organic cation transporterInhibitor0.5829
CYP450 2C9 substrateNon-substrate0.7898
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateNon-substrate0.6722
CYP450 1A2 substrateInhibitor0.9106
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorInhibitor0.7518
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8213
Ames testNon AMES toxic0.7617
CarcinogenicityNon-carcinogens0.9029
BiodegradationNot ready biodegradable0.9954
Rat acute toxicity2.8877 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.6099
hERG inhibition (predictor II)Inhibitor0.7023
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (140 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzothiopyrans
Sub Class
1-benzothiopyrans
Direct Parent
Thioxanthenes
Alternative Parents
Diarylthioethers / N-alkylpiperazines / Benzenoids / Aryl chlorides / Trialkylamines / 1,2-aminoalcohols / Azacyclic compounds / Primary alcohols / Organopnictogen compounds / Organochlorides
show 1 more
Substituents
Thioxanthene / Diarylthioether / Aryl thioether / N-alkylpiperazine / Aryl chloride / Aryl halide / 1,4-diazinane / Piperazine / Benzenoid / Tertiary aliphatic amine
show 17 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
clopenthixol (CHEBI:51364)

Targets

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
Uniprot Name
D(1A) dopamine receptor
Molecular Weight
49292.765 Da
References
  1. Lublin H, Gerlach J, Hagert U, Meidahl B, Molbjerg C, Pedersen V, Rendtorff C, Tolvanen E: Zuclopenthixol, a combined dopamine D1/D2 antagonist, versus haloperidol, a dopamine D2 antagonist, in tardive dyskinesia. Eur Neuropsychopharmacol. 1991 Dec;1(4):541-8. [PubMed:1822319]
  2. Manzaneque JM, Navarro JF: An ethopharmacological assessment of the effects of zuclopenthixol on agonistic interactions in male mice. Methods Find Exp Clin Pharmacol. 1999 Jan-Feb;21(1):11-5. [PubMed:10222441]
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
DRD5
Uniprot ID
P21918
Uniprot Name
D(1B) dopamine receptor
Molecular Weight
52950.5 Da
References
  1. Lublin H, Gerlach J, Hagert U, Meidahl B, Molbjerg C, Pedersen V, Rendtorff C, Tolvanen E: Zuclopenthixol, a combined dopamine D1/D2 antagonist, versus haloperidol, a dopamine D2 antagonist, in tardive dyskinesia. Eur Neuropsychopharmacol. 1991 Dec;1(4):541-8. [PubMed:1822319]
  2. Manzaneque JM, Navarro JF: An ethopharmacological assessment of the effects of zuclopenthixol on agonistic interactions in male mice. Methods Find Exp Clin Pharmacol. 1999 Jan-Feb;21(1):11-5. [PubMed:10222441]
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
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Gareri P, De Fazio P, Stilo M, Ferreri G, De Sarro G: Conventional and atypical antipsychotics in the elderly : a review. Clin Drug Investig. 2003;23(5):287-322. [PubMed:17535043]
  2. Lublin H, Gerlach J, Hagert U, Meidahl B, Molbjerg C, Pedersen V, Rendtorff C, Tolvanen E: Zuclopenthixol, a combined dopamine D1/D2 antagonist, versus haloperidol, a dopamine D2 antagonist, in tardive dyskinesia. Eur Neuropsychopharmacol. 1991 Dec;1(4):541-8. [PubMed:1822319]
  3. Nyberg S, Farde L, Bartfai A, Halldin C: Central D2 receptor occupancy and effects of zuclopenthixol acetate in humans. Int Clin Psychopharmacol. 1995 Nov;10(4):221-7. [PubMed:8748043]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
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) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
Molecular Weight
51486.005 Da
References
  1. Khalifa AE: Zuclopenthixol facilitates memory retrieval in rats: possible involvement of noradrenergic and serotonergic mechanisms. Pharmacol Biochem Behav. 2003 Jul;75(4):755-62. [PubMed:12957216]
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 oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 Da
References
  1. Khalifa AE: Zuclopenthixol facilitates memory retrieval in rats: possible involvement of noradrenergic and serotonergic mechanisms. Pharmacol Biochem Behav. 2003 Jul;75(4):755-62. [PubMed:12957216]
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-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 Da
References
  1. Nyberg S, Farde L, Bartfai A, Halldin C: Central D2 receptor occupancy and effects of zuclopenthixol acetate in humans. Int Clin Psychopharmacol. 1995 Nov;10(4):221-7. [PubMed:8748043]
  2. Gjerden P, Slordal L, Bramness JG: Association between the use of anticholinergic antiparkinson drugs and safety and receptor drug-binding profiles of antipsychotic agents. Eur J Clin Pharmacol. 2009 Dec;65(12):1229-35. doi: 10.1007/s00228-009-0696-6. [PubMed:19644682]
  3. Khalifa AE: Zuclopenthixol facilitates memory retrieval in rats: possible involvement of noradrenergic and serotonergic mechanisms. Pharmacol Biochem Behav. 2003 Jul;75(4):755-62. [PubMed:12957216]
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 catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. Link [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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Davies SJ, Westin AA, Castberg I, Lewis G, Lennard MS, Taylor S, Spigset O: Characterisation of zuclopenthixol metabolism by in vitro and therapeutic drug monitoring studies. Acta Psychiatr Scand. 2010 Dec;122(6):444-53. doi: 10.1111/j.1600-0447.2010.01619.x. Epub 2010 Oct 12. [PubMed:20946203]

Drug created on August 29, 2007 14:18 / Updated on October 16, 2018 08:37