2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. Amisulpride

Amisulpride  (Synonyms: DAN 2163)

Cat. No.: HY-14545 Purity: 99.92%
SDS COA Handling Instructions

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Amisulpride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively.

For research use only. We do not sell to patients.

Amisulpride Chemical Structure

Amisulpride Chemical Structure

CAS No. : 71675-85-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 106 In-stock
Solution
10 mM * 1 mL in DMSO USD 106 In-stock
Solid
100 mg USD 96 In-stock
200 mg USD 168 In-stock
500 mg USD 306 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Amisulpride:

Amisulpride Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Amisulpride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively.

IC50 & Target

D3 Receptor

 

Cellular Effect
Cell Line Type Value Description References
CHO-K1 IC50
3.04 nM
Compound: Amisulpride
Antagonistic activity at D2 receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of dopamine-induced calcium flux by fluo-4 dye based FLIPR assay
Antagonistic activity at D2 receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of dopamine-induced calcium flux by fluo-4 dye based FLIPR assay
[PMID: 27487565]
In Vitro

Amisulpride is an atypical dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively. Amisulpride (100 nM) inhibits quinpirole-elicited [3H]thymidine incorporation with an IC50 value of 22±3 nM (n=3). Amisulpride 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) and opposes the inhibitory effects of 7-OH-DPAT in both brain areas[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Amisulpride Related Antibodies
In Vivo

Only the highest dose of Amisulpride (100 mg/kg) significantly reduces dopamine levels in the striatum or limbic system. Amisulpride significantly increases the synthesis of dopamine in the rat striatum and limbic system at doses of 20 and 100 mg/kg. Amisulpride (0.5 to 75 mg/kg) fails to provoke an additional increase in dopa accumulation in the striatum but slightly accelerates, at 75 mg/kg, dopamine synthesis in the limbic system. In comparison with vehicle-treated controls, Amisulpride (10 mg/kg) increases extracellular dopamine levels. The administration of Amisulpride (0.5 to 15 mg/kg s.c.) provokes a time- and dose-dependent increase in the stimulation-evoked dopamine release. Amisulpride decreases striatal ACh levels significantly at 30 and 100 mg/kg (87.5% and 56.3% of control levels, respectively)[1]. In both acute study, Amisulpride (70 mg/kg, p.o.) significantly increases the duration of swimming behavior [F(3,28)=45.90, p<0.01][2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

369.48

Formula

C17H27N3O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCN1C(CNC(C2=CC(S(=O)(CC)=O)=C(N)C=C2OC)=O)CCC1
Shipping

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

DMSO : 50 mg/mL (135.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 0.2 mg/mL (0.54 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
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, 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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 (6.77 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 (6.77 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 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

Purity: 99.92%

SDS (393 KB)

COA (252 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

The functional effects of Amisulpride at the dopamine D3 receptor subtype are assessed. Briefly, the mitogenic response elicited in NG108-15 neuroblastoma-glioma cells stably transfected with human dopamine D3 receptor cDNA by the addition of 10 nM quinpirole in the presence of 1 μM forskolin is quantified by the incorporation of [3H]thymidine. Antagonism of quinpirole-induced mitogenesis is measured in the presence of increasing (0.1 to 100 nM) concentrations of Amisulpride[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

A total of 64 male Swiss albino mice weighing between 20 to 30 g are used. The animals are fed with standard pellet diet and water ad libitum. The mice are divided in different groups (n=8 in each group) and drug administration is done as follows: Group 1 (control): distilled water (1 mL/kg) 23.5, 5 and 1 h before the test. Group 3 (Amisulpride): Amisulpride (70 mg/kg) 23.5, 5 and 1 h before the test[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 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
DMSO 1 mM 2.7065 mL 13.5325 mL 27.0651 mL 67.6627 mL
5 mM 0.5413 mL 2.7065 mL 5.4130 mL 13.5325 mL
10 mM 0.2707 mL 1.3533 mL 2.7065 mL 6.7663 mL
15 mM 0.1804 mL 0.9022 mL 1.8043 mL 4.5108 mL
20 mM 0.1353 mL 0.6766 mL 1.3533 mL 3.3831 mL
25 mM 0.1083 mL 0.5413 mL 1.0826 mL 2.7065 mL
30 mM 0.0902 mL 0.4511 mL 0.9022 mL 2.2554 mL
40 mM 0.0677 mL 0.3383 mL 0.6766 mL 1.6916 mL
50 mM 0.0541 mL 0.2707 mL 0.5413 mL 1.3533 mL
60 mM 0.0451 mL 0.2255 mL 0.4511 mL 1.1277 mL
80 mM 0.0338 mL 0.1692 mL 0.3383 mL 0.8458 mL
100 mM 0.0271 mL 0.1353 mL 0.2707 mL 0.6766 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Amisulpride Related Classifications

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    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:

Amisulpride71675-85-9DAN 2163DAN2163DAN-2163Dopamine ReceptorInhibitorinhibitorinhibit

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