| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
D1/2 receptor
|
|---|---|
| ln Vitro |
Zuclopenthixol decanoate is a member of thioxanthenes. Zuclopenthixol decanoate prevented or postponed relapses when compared to other depots (NNT 8, CI 5-53). However, zuclopenthixol decanoate may induce more adverse effects (NNH 5, CI 3-31) although it decreases need for anticholinergic medication when compared to a group of other depot preparations (NNT 9, CI 5-38). For the risk of leaving the study early, there was also a trend for benefit to those allocated to zuclopenthixol decanoate. None of the studies reported outcomes on service utilisation, costs, or quality of life[2].
|
| ln Vivo |
Zuclopenthixol is a thioxanthene derivative which acts as a mixed dopamine D1/D2 receptor antagonist. Although the antiaggressive action of neuroleptic drugs is well known, the effects of zuclopenthixol on agonistic interactions have not been explored and there are no studies comparing acute and subchronic effects of this compound on aggression in rodents. In this work, we examined the action of zuclopenthixol (0.025-0.4 mg/kg), administered acutely or subchronically for 10 days, on agonistic behavior elicited by isolation in male mice. Individually housed mice were exposed to anosmic "standard opponents" 30 min after the drug administration, and encounters were videotaped and evaluated using an ethologically based analysis. After acute treatment, zuclopenthixol (0.2 and 0.4 mg/kg)-treated animals exhibited ethopharmacological profiles characterized by a decrease in offensive behaviors without impairment of motor activity (0.2 mg/kg). In contrast, the antiaggressive action of the highest dose used (0.4 mg/kg) was accompanied by a marked increase of immobility. After subchronic treatment, no tolerance to zuclopenthixol antiaggressive or motor activity was observed. Overall, this behavioral profile is similar to that observed with other typical neuroleptics.[1]
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| References |
|
| Additional Infomation |
Zuclopenthixol decanoate is a member of thioxanthenes.
|
| Molecular Formula |
C32H43N2O2SCL
|
|---|---|
| Molecular Weight |
555.21402
|
| Exact Mass |
554.273
|
| Elemental Analysis |
C, 69.23; H, 7.81; Cl, 6.38; N, 5.05; O, 5.76; S, 5.77
|
| CAS # |
64053-00-5
|
| Related CAS # |
53772-83-1;58045-23-1 (HCl);85721-05-7 (acetate);64053-00-5 (decanoate); trans-Clopenthixol dihydrochloride;58045-22-0;Zuclopenthixol-d4 succinate;1246833-97-5;Zuclopenthixol dihydrochloride;58045-23-1; 85721-05-7 (acetate); 58045-23-1 (HCl)
|
| PubChem CID |
6450333
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.152g/cm3
|
| Boiling Point |
662.7ºC at 760mmHg
|
| Flash Point |
354.6ºC
|
| Index of Refraction |
1.593
|
| LogP |
7.803
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
15
|
| Heavy Atom Count |
38
|
| Complexity |
726
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCCCCCCCCC(OCCN1CCN(CC/C=C2\C3=CC=CC=C3SC3C=CC(=CC\2=3)Cl)CC1)=O
|
| InChi Key |
QRUAPADZILXULG-WKIKZPBSSA-N
|
| InChi Code |
InChI=1S/C32H43ClN2O2S/c1-2-3-4-5-6-7-8-15-32(36)37-24-23-35-21-19-34(20-22-35)18-11-13-27-28-12-9-10-14-30(28)38-31-17-16-26(33)25-29(27)31/h9-10,12-14,16-17,25H,2-8,11,15,18-24H2,1H3/b27-13-
|
| Chemical Name |
2-[4-[(3Z)-3-(2-chlorothioxanthen-9-ylidene)propyl]piperazin-1-yl]ethyl decanoate
|
| Synonyms |
Zuclopenthixol decanoate; 64053-00-5; Clopixol Depot; TSS9KIZ5OG; UNII-TSS9KIZ5OG; 2-[4-[(3Z)-3-(2-chlorothioxanthen-9-ylidene)propyl]piperazin-1-yl]ethyl decanoate; Decanoic acid, 2-(4-(3-(2-chloro-9H-thioxanthen-9-ylidene)propyl)-1-piperazinyl)ethyl ester, (Z)-; Decanoic acid, 2-[4-[(3Z)-3-(2-chloro-9H-thioxanthen-9-ylidene)propyl]-1-piperazinyl]ethyl ester; Decanoic acid, 2-[4-[3-(2-chloro-9H-thioxanthen-9-ylidene)propyl]-1-piperazinyl]ethyl ester, (Z)-; 9H-Thioxanthene, decanoic acid deriv.; Zuclopenthixol decanoate; 2-[4-[3-[(9Z)-2-Chloro-9H-thioxanthen-9-ylidene]propyl]piperazin-1-yl]ethyl decanoate;
|
| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| 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
|
|---|---|
| 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 | 1.8011 mL | 9.0056 mL | 18.0112 mL | |
| 5 mM | 0.3602 mL | 1.8011 mL | 3.6022 mL | |
| 10 mM | 0.1801 mL | 0.9006 mL | 1.8011 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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