2. Others Neuronal Signaling GPCR/G Protein
  3. Drug Derivative Dopamine Receptor 5-HT Receptor
  4. Mosapramine

Mosapramine  (Synonyms: Clospipramine)

Cat. No.: HY-106584 Purity: 98.58%
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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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Mosapramine

Mosapramine Chemical Structure

CAS No. : 89419-40-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Mosapramine Related Antibodies

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  • Purity & Documentation

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Description

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[1][2][3].

IC50 & Target

D2 Receptor

 

5-HT2 Receptor

 

In Vitro

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 Related Antibodies
In Vivo

The D2 receptor/5-HT2 receptor occupancy ratio of mosapramine in rat brains is 7.4, a value close to that of first-generation antipsychotic compounds such as chlorpromazine (HY-12708) (4.6) and zotepin (HY-103093) (4.3), but lower than that of clozapine (HY-14539) (49)[1].
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.

Animal Model: Wistar (male, 7-8 weeks old, 200-250 g)[2]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; single dose
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.
Molecular Weight

479.06

Formula

C28H35ClN4O
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C1C2(CCN(CCCN3C4=CC(Cl)=CC=C4CCC5=C3C=CC=C5)CC2)N6C(CCCC6)N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0874 mL 10.4371 mL 20.8742 mL
5 mM 0.4175 mL 2.0874 mL 4.1748 mL
View the 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.

  • Molarity Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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C2

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In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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Mosapramine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Mosapramine89419-40-9ClospipramineDrug DerivativeDopamine Receptor5-HT ReceptorDrug derivativeSerotonin Receptor5-hydroxytryptamine ReceptorFos proteinserotonin 5-HT2 receptorsdopamine D2 receptorsmedial prefrontal cortexnucleus accumbensdorsolateral striatumrat brain regionsschizophreniaextrapyramidal symptomshyperprolactinemiaInhibitorinhibitorinhibit

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