Amisulpride (DAN 2163)

Alias: DAN-2163; Solian; Amazeo; Amipride; Amival; Soltus;Aminosultopride; DAN 2163; DAN2163; Deniban; Amisulprida; Sulpitac; Sulprix

Cat No.:V1271 Purity: ≥98%

COA Product Data Instructions for use SDS

Amisulpride (DAN 2163) Chemical Structure CAS No.: 71675-85-9
Product category: Dopamine Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

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J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

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Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information

Product Description

Amisulpride (Solian; Amazeo; Amipride; Amival; Soltus; Aminosultopride; DAN-2163; DAN2163; Deniban; Amisulprida; Sulpitac; Sulprix) is a potent and atypical antipsychotic medication used to treat psychosis in schizophrenia and episodes of mania in bipolar disorders. In Italy, it has also been utilized to treat dysthymia. With Ki values of 2.8±0.4nM for the D2 receptor subtype and 3.2±0.3nM for the D3 receptor subtype, respectively, amisulpride has demonstrated a strong affinity for the cloned and stably transfected human dopamine D2 receptor. It has been observed that amisulpride, with an IC50 value of 21nM, inhibits radioligand binding to native dopamine D2 receptor in rat striatal membranes.

Biological Activity I Assay Protocols (From Reference)

Targets

D₂ Receptor ( IC50 = 2.8 nM ); D₃ Receptor ( IC50 = 3.2 nM )

ln Vitro

In vitro activity: Amisulpride is an unconventional antagonist of the dopamine D₂/D₃ receptor, with a Kis of 2.8 and 3.2 nM for human D₂ and D₃, respectively. The [³H]thymidine incorporation induced by quinpirole is inhibited by amisulpride (100 nM) with an IC50 value of 22±3 nM (n=3). Amisulpride counteracts the inhibitory effects of 7-OH-DPAT in both brain areas and slightly but significantly increases [³H]dopamine release from slices of the rat striatum (S₂/S₁=0.88±0.04 under control conditions, n=6; 1.04±0.08 in the presence of 100 nM Amisulpride, n=4; P<0.05)[1].

ln Vivo

Only the highest dose of Amisulpride (100 mg/kg) significantly reduces dopamine levels in the striatum or limbic system. At doses of 20 and 100 mg/kg, amisulpride dramatically increases the synthesis of dopamine in the rat limbic system and striatum. Amisulpride (0.5 to 75 mg/kg) does not cause an additional rise in dopa accumulation in the striatum, but it does cause a slight acceleration of dopamine synthesis in the limbic system at 75 mg/kg. Amisulpride (10 mg/kg) raises extracellular dopamine levels when compared to vehicle-treated controls. The stimulation-evoked release of dopamine increases in a dose- and time-dependent manner when amisulpride (0.5 to 15 mg/kg s.c.) is administered. Amisulpride (70 mg/kg, p.o.) considerably lengthens swimming behavior in both acute studies [F(3,28)=45.90, p<0.01].[2].

Cell Assay

Amisulpride's functional effects at the dopamine D₃ receptor subtype are evaluated. In summary, [³H]thymidine incorporation measures the mitogenic response induced in NG108-15 neuroblastoma-glioma cells stably transfected with human dopamine D₃ receptor cDNA by adding 10 nM quinpirole in the presence of 1 μM forskolin. When Amisulpride concentrations increase from 0.1 to 100 nM, the antagonism of quinpirole-induced mitogenesis is measured[1].

Animal Protocol

The entire weight of the 64 male Swiss albino mice used ranges from 20 to 30 g. Regular pellet food and unlimited water are provided to the animals. Each group of mice consists of eight mice, and the following is how the drugs are given to the mice: Distilled water (1 mL/kg) was given to Group 1 (control) 23.5, 5 and 1 hours prior to the exam. Amisulpride (70 mg/kg) was administered to Group 3 participants 23.5, 5 and 1 hour prior to the exam[2].

References

[1]. 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.

[2]. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C17H27N3O4S

Molecular Weight

369.48

Exact Mass

369.17

Elemental Analysis

C, 55.26; H, 7.37; N, 11.37; O, 17.32; S, 8.68

CAS #

71675-85-9

Related CAS #

Amisulpride-d5; 1216626-17-3; Amisulpride hydrochloride; 81342-13-4; Amisulpride-d5 N-Oxide; 1794756-15-2

Appearance

Solid powder

SMILES

CCN1CCCC1CNC(=O)C2=CC(=C(C=C2OC)N)S(=O)(=O)CC

InChi Key

NTJOBXMMWNYJFB-UHFFFAOYSA-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)

Chemical Name

4-amino-N-[(1-ethylpyrrolidin-2-yl)methyl]-5-ethylsulfonyl-2-methoxybenzamide

Synonyms

DAN-2163; Solian; Amazeo; Amipride; Amival; Soltus;Aminosultopride; DAN 2163; DAN2163; Deniban; Amisulprida; Sulpitac; Sulprix

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)

DMSO: 50~74 mg/mL (200.3~135.3 mM)

Water: <1 mg/mL

Ethanol: ~74 mg/mL (~200.3 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.77 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.77 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 3: 2.5 mg/mL (6.77 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.7065 mL	13.5325 mL	27.0651 mL
	5 mM	0.5413 mL	2.7065 mL	5.4130 mL
	10 mM	0.2707 mL	1.3533 mL	2.7065 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

Mass

Concentration

Volume

Molecular Weight*

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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

See Example

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.

Concentration (Start)

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Concentration (End)

Volume (End)

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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

Molecular formula

Total molecular weight

g/mol

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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.

Volume (to add to vial)

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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)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

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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.)

% DMSO

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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.

Note： (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.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04128683	Active Recruiting	Drug: amisulpride Drug: bromocriptine	Anorexia Nervosa	University of California, San Diego	October 20, 2020	Early Phase 1
NCT05956600	Not yet recruiting	Drug: Amisulpride 50 MG	Schizophrenia, Treatment- Resistant	University of California, Los Angeles	November 2023	Not Applicable
NCT04341467	Recruiting	Drug: Amisulpride Drug: Olanzapine	BPSD Amisulpride	Tianjin Anding Hospital	December 1, 2019	Not Applicable
NCT05822713	Not yet recruiting	Drug: Amisulpride Drug: Amisulpride Placebo	PONV	Qilu Pharmaceutical (Hainan) Co., Ltd.	April 29, 2023	Phase 3
NCT02926859	Recruiting	Drug: Cannabidiol as add-on Drug: Placebo as add-on	Schizophrenia	Central Institute of Mental Health, Mannheim	Phase 2	April 8, 2017