| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| Other Sizes |
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| Targets |
D1/2 receptor
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|---|---|
| ln Vitro |
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.
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| ln Vivo |
Animals treated with succinyleptidol (0.2 and 0.4 mg/kg) displayed a pharmacological behavioral profile that included decreased aggression but no locomotor activity. By contrast, the maximum dose (0.4 mg/kg) caused a considerable increase in immobility along with its anti-aggression effect. No resistance against aggressiveness or locomotor activity induced by Zuclopenthixol was seen during subchronic therapy [1]. Zuclopenthixol raised MDA levels considerably at doses of 0.7 and 1.4 mg/kg. The effects of the two dosing levels on brain reserve MDA levels, however, were identical. Animals receiving 1.4 mg/kg of Zuclopenthixol had much lower GSH levels. However, the drug's reduced dosage had no discernible effect. The GSH levels of animals treated with 0.7 or 1.4 mg/kg Zuclopenthixol were considerably greater than those of those treated with SCO. When compared to animals treated natively, the administration of 0.7 mg/kg Zuclopenthixol markedly improved GSHPx activity [2].
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| ADME/Pharmacokinetics |
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. Route of Elimination Primarily in the feces with approximately 10% in the urine. Volume of Distribution 20 L/kg. Clearance approximately 0.9 L/min. Metabolism / Metabolites The metabolism of zuclopenthixol is mainly by sulphoxidation, side chain N-dealkylation and glucuronic acid conjugation. The metabolites are devoid of pharmacological activity. Biological Half-Life 20 hours (range 12-28 hours) for the tablet form, 19 days for the depot form. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Zuclopenthixol is not approved for marketing in the United States, by the U.S. Food and Drug Administration, but is available in other countries. Limited information indicates that maternal oral doses of up to 50 mg daily or depot injections of 72 mg every 2 weeks produce low levels in breastmilk and no detectable short-term adverse effects in the breastfed infants. No long-term data are available. One international guideline recommends that women taking zuclopenthixol not breastfeed. However, a safety scoring system finds zuclopenthixol possible to use cautiously during breastfeeding. Until more data are available, zuclopenthixol should be used with careful infant monitoring during breastfeeding. ◉ Effects in Breastfed Infants Six women received zuclopenthixol during nursing. Five of the women were receiving 4 to 50 mg daily by mouth and one was receiving a depot injection of 72 mg every 2 weeks. Their breastfed infants ranged in age from 3 days to 10 months old, 5 of whom were 2 months or under. No immediate adverse effects such infant drowsiness were noted. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. Drugs and Lactation Database (LactMed) Protein Binding: 98-99% |
| References |
[1]. Khalifa AE, et al. 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.
[2]. Manzaneque JM, et al. 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. [3]. Bryan EJ, et al. Zuclopenthixol dihydrochloride for schizophrenia. Cochrane Database Syst Rev. 2017 Nov 16;11(11):CD005474. |
| Additional Infomation |
See also: Zuclopenthixol (annotation moved to).
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| Molecular Formula |
C22H25N2OSCL.2[HCL]
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|---|---|
| Molecular Weight |
473.88658
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| Exact Mass |
472.09096
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| Elemental Analysis |
C, 55.76; H, 5.74; Cl, 22.44; N, 5.91; O, 3.38; S, 6.77
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| CAS # |
58045-23-1
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| Related CAS # |
Zuclopenthixol;53772-83-1; trans-Clopenthixol dihydrochloride;58045-22-0;Zuclopenthixol-d4 succinate;1246833-97-5;Zuclopenthixol dihydrochloride;58045-23-1; 85721-05-7 (acetate); 53772-83-1; 58045-23-1 (HCl); 64053-00-5 (decanoate)
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| PubChem CID |
6433208
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| Appearance |
Light yellow to yellow solid powder
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| Boiling Point |
577.4ºC at 760 mmHg
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| Flash Point |
303ºC
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| LogP |
4.914
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
509
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CN(CCN1CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl)CCO.Cl.Cl
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| InChi Key |
LPWNZMIBFHMYMX-MHKBYHAFSA-N
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| InChi Code |
InChI=1S/C22H25ClN2OS.2ClH/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;2*1H/b18-5-;;
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| Chemical Name |
2-[4-[(3Z)-3-(2-chlorothioxanthen-9-ylidene)propyl]piperazin-1-yl]ethanol;dihydrochloride
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| Synonyms |
Zuclopenthixol dihydrochloride; 58045-23-1; Zuclopenthixol hydrochloride; Cisordinol; Clopenthixol cis(Z)-form dihydrochloride; Zuclopenthixol (dihydrochloride); DTXSID5045332; 7042692VYN;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1102 mL | 10.5510 mL | 21.1019 mL | |
| 5 mM | 0.4220 mL | 2.1102 mL | 4.2204 mL | |
| 10 mM | 0.2110 mL | 1.0551 mL | 2.1102 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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