Zuclopenthixol
Based on 1 publication(s) in Google Scholar
Zuclopenthixol ((Z)-Clopenthixol) is a thioxanthene derivative which acts as a mixed dopamine D1/D2 receptor antagonist.
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- Pureté: 98.08%
- CAS No.: 53772-83-1
- Formule: C22H25ClN2OS
- Masse moléculaire:400.96
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Zuclopenthixol
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Activité biologique
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D2 Receptor |
Administration of Zuclopenthixol (0.7 and 1.4 mg/kg) significantly elevate MDA level compared to respective controls. Nevertheless, there is no difference between the two dose levels with respect to their effect on rat brain MDA level. Post hoc pairwise comparisons between the means of groups (n=12) receiving different dose levels of Zuclopenthixol reveal that administration of 1.4 mg/kg of Zuclopenthixol significantly reduces GSH level compared to both vehicle-treated and Zuclopenthixol (0.7 mg/kg)-treated animals (P<0.001). Nevertheless, the lower dose of the drug does not affect rat brain GSH level. Animals receiving 0.7 or 1.4 mg/kg of Zuclopenthixol exhibits significantly higher GSH levels than SCO treated animals. Administration of 0.7 mg/kg of Zuclopenthixol significantly elevated GSHPx activity compared to vehicle treated animals[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 53772-83-1
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Appearance Solid
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Masse moléculaire 400.96
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Formule C22H25ClN2OS
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Color Light yellow to yellow
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SMILES
OCCN1CCN(CC/C=C2C3=C(SC4=C\2C=CC=C4)C=CC(Cl)=C3)CC1
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Synonyms
(Z)-Clopenthixol
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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ACS Pharmacol Transl Sci
2020 Oct 14;3(6):1278-1292. PMID: 33330842
Solvant et solubilité
DMSO : 200 mg/mL (498.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (12.47 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.86 mg/mL (7.13 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.86 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (28.6 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
Mice[1]
Zuclopenthixol (0.025-0.4 mg/kg) is administered acutely or subchronically for 10 days, on agonistic behavior elicited by isolation in male mice. Individually housed mice are exposed to anosmic "standard opponents" 30 min after the drug administration, and encounters are videotaped and evaluated using an ethologically based analysis[1].
Rats[2]
Male albino rats of Wistar strain weighing 200-250 g are used. They are kept in a temperature of 23-25°C with alternating 12-hour light and dark cycles and allowed free access to food and water. Animals are divided into six groups (n=6). Two groups receive two dose levels of Zuclopenthixol (0.7 and 1.4 mg/kg i.p.) 60 min and SCO (1.4 mg/kg i.p.) 30 min before decapitation. A third group of rats is injected with saline, with the same content of ethanol (20% v/v) and vegetable oil (2.8% v/v) in the test solution, 60 min and then SCO (1.4 mg/kg i.p.) 30 min before decapitation. The forth and fifth groups of rats receive two dose levels of Zuclopenthixol (0.7 and 1.4 mg/kg i.p.) 60 min and saline 30 min before decapitation. A control group of six animals is given saline, with the same content of ethanol (20% v/v) and vegetable oil (2.8% v/v) in the test solution, 60 min and then saline 30 min before decapitation and is run concurrently with drug-treated groups[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. 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. [Content Brief]
[2]. 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.4940 mL | 12.4701 mL | 24.9401 mL | 62.3504 mL |
| 5 mM | 0.4988 mL | 2.4940 mL | 4.9880 mL | 12.4701 mL | |
| 10 mM | 0.2494 mL | 1.2470 mL | 2.4940 mL | 6.2350 mL | |
| 15 mM | 0.1663 mL | 0.8313 mL | 1.6627 mL | 4.1567 mL | |
| 20 mM | 0.1247 mL | 0.6235 mL | 1.2470 mL | 3.1175 mL | |
| 25 mM | 0.0998 mL | 0.4988 mL | 0.9976 mL | 2.4940 mL | |
| 30 mM | 0.0831 mL | 0.4157 mL | 0.8313 mL | 2.0783 mL | |
| 40 mM | 0.0624 mL | 0.3118 mL | 0.6235 mL | 1.5588 mL | |
| 50 mM | 0.0499 mL | 0.2494 mL | 0.4988 mL | 1.2470 mL | |
| 60 mM | 0.0416 mL | 0.2078 mL | 0.4157 mL | 1.0392 mL | |
| 80 mM | 0.0312 mL | 0.1559 mL | 0.3118 mL | 0.7794 mL | |
| 100 mM | 0.0249 mL | 0.1247 mL | 0.2494 mL | 0.6235 mL |
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