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Amisulpride-d5 (amisulpride d5)

Cat No.:V71769 Purity: ≥98%
Amisulpride-d5 is the deuterium labelled form of Amisulpride.
Amisulpride-d5 (amisulpride d5)
Amisulpride-d5 (amisulpride d5) Chemical Structure CAS No.: 1216626-17-3
Product category: Dopamine Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
Other Sizes

Other Forms of Amisulpride-d5 (amisulpride d5):

  • Amisulpride-d5 N-Oxide (amisulpride d5 (N-oxide))
  • Amisulpride N-oxide
  • Aramisulpride hydrochloride
  • Desmethyl amisulpride-d5 hydrobromide
  • Amisulpride (DAN 2163)
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Amisulpride-d5 is the deuterium labelled form of Amisulpride. Amisulpride is a dopamine D2/D3 receptor antagonist (inhibitor) with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively.
Amisulpride-d5 is a deuterium-labeled form of amisulpride, an atypical antipsychotic. Amisulpride is a dopamine D2/D3 receptor antagonist with Ki values of 2.8 and 3.2 nM for the human D2 and D3 receptors, respectively. The deuterated form is used as an internal standard in analytical methods for the quantification of amisulpride.
Biological Activity I Assay Protocols (From Reference)
Targets
Amisulpride-d5 targets the dopamine D2 and D3 receptors, acting as an antagonist, similar to its non-deuterated parent compound. The deuterated compound is used as an analytical internal standard and is not intended for pharmacological use.
ln Vitro
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
Amisulpride-d5 is not pharmacologically active in its own right; it serves as an analytical internal standard. It exhibits the same physicochemical properties as native amisulpride, including similar chromatographic behavior and ionization efficiency. The compound is used to correct for matrix effects, extraction efficiency, and instrument variability in quantitative analyses. Amisulpride-d5 is used in cell culture experiments as an internal standard for measuring amisulpride concentrations in cell lysates or media. Cells are treated with the deuterated compound at known concentrations, and samples are analyzed by LC-MS/MS. The internal standard corrects for variations in sample preparation and instrument response.
ln Vivo
In vivo, Amisulpride-d5 is used as an internal standard for quantifying amisulpride concentrations in plasma and other biological fluids. It is added to samples prior to analysis. The compound enables accurate measurement of amisulpride levels in pharmacokinetic and therapeutic drug monitoring studies.
Enzyme Assay
Cell-free receptor binding assays are not applicable for Amisulpride-d5 as it is not a pharmacologically active compound. However, the deuterated standard is used in analytical method development for amisulpride quantification. Validation experiments demonstrate that it exhibits identical chromatographic retention time and ionization efficiency as the non-deuterated compound.
Cell Assay
Cellular assays using Amisulpride-d5 are limited to its use as an analytical internal standard. Cells are cultured and treated with the compound at known concentrations, followed by sample preparation and LC-MS/MS analysis. The compound is used to validate analytical methods for amisulpride quantification in cellular models.
ADME/Pharmacokinetics
As an internal standard, Amisulpride-d5 exhibits identical pharmacokinetic behavior to the non-deuterated compound. It is used in LC-MS/MS methods to measure amisulpride concentrations in plasma and other biological fluids. The deuterated compound enables accurate and reliable quantification.
Toxicity/Toxicokinetics
Amisulpride-d5 is not a therapeutic agent and toxicity studies are not applicable. It is used in trace amounts as an analytical internal standard. Standard laboratory safety practices for handling chemical reference standards should be followed.
References

[1]. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

[2]. Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity. J Pharmacol Exp Ther. 1997 Jan;280(1):83-97.

[3]. Evaluation of antidepressant like property of amisulpride per se and its comparison with fluoxetine and olanzapine using forced swimming test in albino mice. Acta Pol Pharm. 2009 May-Jun;66(3):327-31.

Additional Infomation
Amisulpride-d5 is a deuterium-labeled form of amisulpride, used as an analytical internal standard. It is essential for pharmaceutical and biochemical research, particularly in studies involving antipsychotic drug quantification. The compound is not intended for therapeutic use.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H22D5N3O4S
Molecular Weight
374.51
Exact Mass
374.203
CAS #
1216626-17-3
Related CAS #
Amisulpride;71675-85-9
PubChem CID
45273902
Appearance
White to off-white solid powder
Density
1.2±0.1 g/cm3
Boiling Point
558.9±50.0 °C at 760 mmHg
Melting Point
103-105°C
Flash Point
291.8±30.1 °C
Vapour Pressure
0.0±1.5 mmHg at 25°C
Index of Refraction
1.546
LogP
1.6
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
7
Heavy Atom Count
25
Complexity
549
Defined Atom Stereocenter Count
0
SMILES
[2H]C([2H])([2H])C([2H])([2H])N1CCCC1CNC(=O)C2=CC(=C(C=C2OC)N)S(=O)(=O)CC
InChi Key
NTJOBXMMWNYJFB-SGEUAGPISA-N
InChi Code
InChI=1S/C17H27N3O4S/c1-4-20-8-6-7-12(20)11-19-17(21)13-9-16(25(22,23)5-2)14(18)10-15(13)24-3/h9-10,12H,4-8,11,18H2,1-3H3,(H,19,21)/i1D3,4D2
Chemical Name
4-amino-5-ethylsulfonyl-2-methoxy-N-[[1-(1,1,2,2,2-pentadeuterioethyl)pyrrolidin-2-yl]methyl]benzamide
HS Tariff Code
2934.99.9001
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 Data
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.6702 mL 13.3508 mL 26.7016 mL
5 mM 0.5340 mL 2.6702 mL 5.3403 mL
10 mM 0.2670 mL 1.3351 mL 2.6702 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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