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Zuclopenthixol

CAS No.
53772-83-1
Chemical Name:
Zuclopenthixol
Synonyms
Clopixol;Cisordinol;cis(Z)-Form;Zuclopenthixol;Unii-47isu063sg;Einecs 258-758-5;Zuclopenthixolum;cis-Clopenthixol;(Z)-Clopenthixol;Clopentixol cis-(Z)-
CBNumber:
CB1875393
Molecular Formula:
C22H25ClN2OS
Molecular Weight:
400.96
MDL Number:
MFCD00867744
MOL File:
53772-83-1.mol
MSDS File:
SDS
Last updated:2023-06-08 09:02:10

Zuclopenthixol 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
pka 14.96±0.10(Predicted)
color White to Off-White
CAS DataBase Reference 53772-83-1
FDA UNII 47ISU063SG
ATC code N05AF05

Pharmacokinetic data

Protein binding 98%
Excreted unchanged in urine Minimal (10-20% unchanged drug and metabolites)
Volume of distribution 10-20(L/kg)
Biological half-life 20-24 / -

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P264-P270-P301+P312-P330-P501
NFPA 704
0
2 0

Zuclopenthixol price More Price(8)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 24961 Zuclopenthixol ≥98% 53772-83-1 100mg $62 2024-03-01 Buy
Cayman Chemical 24961 Zuclopenthixol ≥98% 53772-83-1 250mg $142 2024-03-01 Buy
Cayman Chemical 24961 Zuclopenthixol ≥98% 53772-83-1 500mg $270 2024-03-01 Buy
Usbiological 023009 Zuclopenthixol 53772-83-1 5mg $460 2021-12-16 Buy
TRC Z701485 Zuclopenthixol 53772-83-1 25mg $1960 2021-12-16 Buy
Product number Packaging Price Buy
24961 100mg $62 Buy
24961 250mg $142 Buy
24961 500mg $270 Buy
023009 5mg $460 Buy
Z701485 25mg $1960 Buy

Zuclopenthixol Chemical Properties,Uses,Production

Description

Zuclopenthixol 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.

Description

Zuclopenthixol 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.

Chemical Properties

Pale Yellow Low Melting Solid

Uses

Zuclopenthixol 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.

Uses

The labelled cis(Z)-form of Clopenthixol. Thioxanthene neuroleptic. Antipsychotic.

Uses

The cis(Z)-form of Clopenthixol. Thioxanthene neuroleptic. Antipsychotic.

Definition

ChEBI: The (Z)-isomer of clopenthixol.

Clinical Use

Antipsychotic for schizophrenia and other psychoses

Drug interactions

Potentially 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.

Metabolism

Metabolism 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.

References

https://www.drugbank.ca/drugs/DB01624
https://en.wikipedia.org/wiki/Tiabendazole

Zuclopenthixol Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 72)Suppliers
Supplier Tel Email Country ProdList Advantage
Frapp's ChemicalNFTZ Co., Ltd.
+86 (576) 8169-6106 sales@frappschem.com China 885 50
career henan chemical co
+86-0371-86658258 15093356674; factory@coreychem.com China 29826 58
SIMAGCHEM CORP
+86-13806087780 sale@simagchem.com China 17367 58
Dideu Industries Group Limited
+86-29-89586680 +86-15129568250 1026@dideu.com China 29271 58
AFINE CHEMICALS LIMITED
0571-85134551 info@afinechem.com CHINA 15377 58
Dayang Chem (Hangzhou) Co.,Ltd.
571-88938639 +8617705817739 info@dycnchem.com CHINA 52867 58
Alfa Chemistry
+1-5166625404 Info@alfa-chemistry.com United States 21317 58
LEAP CHEM CO., LTD.
+86-852-30606658 market18@leapchem.com China 24738 58
Hangzhou MolCore BioPharmatech Co.,Ltd.
+86-057181025280; +8617767106207 sales@molcore.com China 49739 58
TargetMol Chemicals Inc.
+1-781-999-5354 support@targetmol.com United States 19973 58

View Lastest Price from Zuclopenthixol manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Zuclopenthixol USP/EP/BP pictures 2021-07-24 Zuclopenthixol USP/EP/BP
53772-83-1
US $1.10 / g 1g 99.9% 100 Tons min Dideu Industries Group Limited
Zuclopenthixol pictures 2020-01-13 Zuclopenthixol
53772-83-1
US $9.80 / KG 1KG ≥98% 20 tons Career Henan Chemical Co
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 Zuclopenthixolum Zuclopenthixolum [latin] Zuclopenthixol Succinate Salt Zuclopenthixol succinate Zuclopenthixol cis(Z)-Form Zuclopenthixol (1.0 mg/mL in Methanol) (Z)-Clopenthixol Cisordinol 1-Piperazineethanol, 4-[(3Z)-3-(2-chloro-9H-thioxanthen-9-ylidene)propyl]- Zuclopenthixol Decanoate Impurity 3(Zuclopenthixol Decanoate EP Impurity C) Zuclopenthixol USP/EP/BP inhibit,Dopamine Receptor,Inhibitor,Zuclopenthixol 53772-83-1 C20H19ClN2OSC6H12O4 C32H37D4ClN2O5S2 C26H27D4ClN2O5S Heterocycles Intermediates & Fine Chemicals Isotope Labelled Compounds Pharmaceuticals Sulfur & Selenium Compounds