Mosapramine
Based on 1 Customer Validation
Mosapramine (Clospipramine) is an orally active antipsychotic agent and one of the metabolites of Clocapramine (HY-B2073) after oral absorption. Mosapramine exerts its effects by specifically binding to striatal dopamine D2 receptors and frontal lobe 5-HT2 receptors, with a D2/5-HT2 receptor occupancy ratio of 7.4. Mosapramine induces typical neuropharmacological responses in rat brain regions, including extrapyramidal symptoms, hyperprolactinemia, increased salivation, constipation, and upregulated Fos protein expression. Mosapramine also features a reduced incidence of weight loss. Mosapramine is applicable to research related to schizophrenia.
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- Pureté: 98.58%
- CAS No.: 89419-40-9
- Formule: C28H35ClN4O
- Masse moléculaire:479.06
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
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Activité biologique
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D2 Receptor |
5-HT2 Receptor |
Clospipramine is a metabolite produced by the biotransformation of Clocapramine (HY-B2073) in humans and dogs, and exerts antipsychotic pharmacological effects by regulating neurotransmitters in the central nervous system. Clospipramine can be stably detected in plasma, and changes in its plasma concentration can reflect the in vivo metabolic process of Clocapramine[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mosapramine (1-10 mg/kg; p.o.; single dose) induces a dose-dependent increase in Fos protein-positive neurons in rat brain regions, including the medial prefrontal cortex, nucleus accumbens, and dorsolateral striatum[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 7-8 weeks old, 200-250 g)[2]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:p.o.; single dose
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Result:Produced a significant increase in the number of Fos protein positive neurons in the medial prefrontal cortex and nucleus accumbens, but not in the dorsolateral striatum, at 1 mg/kg and 3 mg/kg compared to vehicle-treated animals.
Produced a significant increase in the number of Fos protein positive neurons in the medial prefrontal cortex, nucleus accumbens, and dorsolateral striatum at 10 mg/kg compared to vehicle-treated animals.
Chemical Information
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CAS No. 89419-40-9
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Appearance Solid
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Masse moléculaire 479.06
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Formule C28H35ClN4O
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Color White to light yellow
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SMILES
O=C1C2(CCN(CCCN3C4=CC(Cl)=CC=C4CCC5=C3C=CC=C5)CC2)N6C(CCCC6)N1
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Synonyms
Clospipramine
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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 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (208.74 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (5.22 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.22 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
[2]. Kishi T, et al. Iminodibenzyl class antipsychotics for schizophrenia: a systematic review and meta-analysis of carpipramine, clocapramine, and mosapramine. Neuropsychiatr Dis Treat. 2014;10:2339-2351. Published 2014 Dec 10. [Content Brief]
[3]. Fujimura M, et al. The effect of the antipsychotic drug mosapramine on the expression of Fos protein in the rat brain: comparison with haloperidol, clozapine and risperidone. Life Sci. 2000;67(23):2865-2872. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0874 mL | 10.4371 mL | 20.8742 mL | 52.1855 mL |
| 5 mM | 0.4175 mL | 2.0874 mL | 4.1748 mL | 10.4371 mL | |
| 10 mM | 0.2087 mL | 1.0437 mL | 2.0874 mL | 5.2186 mL | |
| 15 mM | 0.1392 mL | 0.6958 mL | 1.3916 mL | 3.4790 mL | |
| 20 mM | 0.1044 mL | 0.5219 mL | 1.0437 mL | 2.6093 mL | |
| 25 mM | 0.0835 mL | 0.4175 mL | 0.8350 mL | 2.0874 mL | |
| 30 mM | 0.0696 mL | 0.3479 mL | 0.6958 mL | 1.7395 mL | |
| 40 mM | 0.0522 mL | 0.2609 mL | 0.5219 mL | 1.3046 mL | |
| 50 mM | 0.0417 mL | 0.2087 mL | 0.4175 mL | 1.0437 mL | |
| 60 mM | 0.0348 mL | 0.1740 mL | 0.3479 mL | 0.8698 mL | |
| 80 mM | 0.0261 mL | 0.1305 mL | 0.2609 mL | 0.6523 mL | |
| 100 mM | 0.0209 mL | 0.1044 mL | 0.2087 mL | 0.5219 mL |
Mosapramine Related Classifications
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