Zuclopenthixol

Zuclopenthixol Basic information
Product Name:Zuclopenthixol
Synonyms:4-[3-[(9Z)-2-Chloro-9H-thioxanthene-9-ylidene]propyl]-1-piperazineethanol;4-[3-[(Z)-2-Chloro-9H-thioxanthen-9-ylidene]propyl]-1-piperazineethanol;cis-Clopenthixol;(Z)-4-(3-(2-Chlorothioxanthen-9-ylidene)propyl)-1-piperazineethanol;Clopentixol cis-(Z)-;Clopixol;Einecs 258-758-5;Unii-47isu063sg
CAS:53772-83-1
MF:C22H25ClN2OS
MW:400.96
EINECS:258-758-5
Product Categories:Heterocycles;Intermediates & Fine Chemicals;Isotope Labelled Compounds;Pharmaceuticals;Sulfur & Selenium Compounds
Mol File:53772-83-1.mol
Zuclopenthixol Structure
Zuclopenthixol Chemical Properties
Melting point 56-60°C
Boiling point 577.4±50.0 °C(Predicted)
density 1.289±0.06 g/cm3(Predicted)
storage temp. -20°C Freezer, Under Inert Atmosphere
solubility Chloroform (Slightly), Methanol (Slightly)
form Solid
pka14.96±0.10(Predicted)
color White to Off-White
CAS DataBase Reference53772-83-1
Safety Information
MSDS Information
Zuclopenthixol Usage And Synthesis
DescriptionZuclopenthixol is a kind of antipsychotic agent. It is a thioxanthene-based neuroleptic with in vivo action similar to the phenothiazine antipsychotics through antagonizing D1 and D2 dopamine receptors. It has three major formulations form including zuclopenthixol decanoate, zuclopenthixol acetate, and zuclopenthixol dihydrochloride. It can be used for the treatment of schizophrenia and bipolar mania. Besides antagonizing the D1 and D2 dopamine receptors, Zuclopenthixol can also take effect through antagonizing alpha1-adrenergic and 5-HT2 receptors. It can also weakly block the histamine H1 receptor.
DescriptionZuclopenthixol is a dopamine receptor antagonist (Kis = 9.8 and 1.5 nM for D1 and D2 receptors, respectively). It also binds to serotonin (5-HT) receptor subtypes 5-HT2 and 5-HT6, α1-adrenergic, and histamine receptors (Kis = 7.6, 3, 33, and 169 nM, respectively) but not α2-adrenergic receptors (Ki = >4,300 nM). Zuclopenthixol inhibits dopamine-induced accumulation of cAMP in rat striatal homogenates (IC50 = 330 nM; Ki = 16 nM). It decreases stereotypic behavior induced by methylphenidate in mice (ED50 = 0.8 μmol/kg) and by apomorphine in rats and dogs (ED50s = 6.0 and 1.3 μmol/kg, respectively). Zuclopenthixol (0.7 and 1.4 mg/kg, i.p.) administered prior to testing enhances memory retrieval in rats in an inhibitory avoidance task without affecting locomotor activity.
Chemical PropertiesPale Yellow Low Melting Solid
UsesZuclopenthixol is an anti-psychotic drug. It is an inhibitor of coxsackievirus B3. Also, it is an intermediate used in the synthesis of Zuclopenthixol Decanoate (Z701490), which is used in the maintenance treatment of chronic schizophrenic patients. It is one of the three distinct formulations of Zuclopenthixol namely, zuclopenthixol dihydrochloride, zuclopenthixol acetate or Acuphase and zuclopenthixol decanoate.
UsesThe labelled cis(Z)-form of Clopenthixol. Thioxanthene neuroleptic. Antipsychotic.
UsesThe cis(Z)-form of Clopenthixol. Thioxanthene neuroleptic. Antipsychotic.
DefinitionChEBI: The (Z)-isomer of clopenthixol.
Clinical UseAntipsychotic for schizophrenia and other psychoses
Drug interactionsPotentially hazardous interactions with other drugs
Anaesthetics: enhanced hypotensive effects.
Analgesics: increased risk of convulsions with tramadol; enhanced hypotensive and sedative effects with opioids; increased risk of ventricular arrhythmias with methadone.
Anti-arrhythmics: increased risk of ventricular arrhythmias with anti-arrhythmics that prolong the QT interval - avoid with amiodarone and disopyramide.
Antibacterials: increased risk of ventricular arrhythmias with moxifloxacin and parenteral erythromycin - avoid
Antidepressants: increased level of tricyclics; possible increased risk of convulsions with vortioxetine.
Antiepileptics: anticonvulsant effect antagonised.
Antimalarials: avoid concomitant use with artemether/lumefantrine.
Antipsychotics: avoid concomitant use of clozapine with depot preparations in case of neutropenia; possible increased risk of ventricular arrhythmias with risperidone.
Antivirals: concentration possibly increased with ritonavir.
Atomoxetine: increased risk of ventricular arrhythmias.
Anxiolytics and hypnotics: increased sedative effects.
Beta-blockers: increased risk of ventricular arrhythmias with sotalol - avoid.
Cytotoxics: increased risk of ventricular arrhythmias with vandetanib - avoid; increased risk of ventricular arrhythmias with arsenic trioxide.









MetabolismMetabolism of zuclopenthixol is by sulphoxidation, sidechain N-dealkylation and glucuronic acid conjugation.
The sulphoxide metabolites are mainly excreted in the urine while unchanged drug and the dealkylated form tend to be excreted in the faeces.
Referenceshttps://www.drugbank.ca/drugs/DB01624
https://en.wikipedia.org/wiki/Tiabendazole
Zuclopenthixol Preparation Products And Raw materials
EQUILIN Z-VAL-OSU Z-L-Valine NCA Paroxetine Z-TRP-OSU Entacapone Lithium carbonate Prochlorperazine Haloperidol Zuclopenthixol ZUCLOPENTHIXOL DECANOATE Prothixene Chlorprothixene clopenthixol THIOXANTHENE

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