| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
D2 Receptor ( Ki = 2.8 nM ); D3 Receptor ( Ki = 3.2 nM )
Amisulpride targets dopamine D2 and D3 receptors in the central nervous system. It acts as a selective antagonist at these receptors, with higher affinity for D3 than D2. At low doses, amisulpride preferentially blocks presynaptic dopamine autoreceptors, leading to increased dopamine release and alleviation of negative symptoms. At higher doses, it blocks postsynaptic D2 receptors, alleviating positive symptoms of schizophrenia. Amisulpride has low affinity for other receptors, including serotonin, histamine, and muscarinic receptors. |
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| ln Vitro |
Amisulpride hydrochloride 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 hydrochloride (100 nM) with an IC50 value of 22±3 nM (n=3). Amisulpride hydrochloride 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 hydrochloride, n=4; P<0.05)[1].
In vitro, Amisulpride has been shown to bind selectively to dopamine D2 and D3 receptors with high affinity. It exhibits antagonist activity at these receptors, blocking dopamine-induced signaling. The compound has low affinity for other receptor types, including 5-HT2A, α1-adrenergic, and histamine H1 receptors. This selectivity contributes to its favorable side effect profile, with a low incidence of extrapyramidal symptoms and sedation compared to other antipsychotics. |
| ln Vivo |
Only the highest dose of Amisulpride hydrochloride (100 mg/kg) significantly reduces dopamine levels in the striatum or limbic system. At doses of 20 and 100 mg/kg, Amisulpride hydrochloride dramatically increases the synthesis of dopamine in the rat limbic system and striatum. Amisulpride hydrochloride (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 hydrochloride (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 hydrochloride (0.5 to 15 mg/kg s.c.) is administered. Amisulpride hydrochloride (70 mg/kg, p.o.) considerably lengthens swimming behavior in both acute studies [F(3,28)=45.90, p<0.01].[2]. |
| Enzyme Assay |
In vitro receptor binding assays for Amisulpride typically involve measuring its affinity for dopamine D2 and D3 receptors using radioligand binding. The compound is incubated with membrane preparations from cells expressing the receptors and a radiolabeled ligand. The concentration of Amisulpride required to displace 50% of the radioligand (IC50) is determined, and the Ki value is calculated. The selectivity of Amisulpride for D2 and D3 over other receptors is assessed using similar binding assays with other receptor types.
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| Cell Assay |
Amisulpride hydrochloride'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 hydrochloride concentrations increase from 0.1 to 100 nM, the antagonism of quinpirole-induced mitogenesis is measured[1].
In vitro cell-based studies with Amisulpride typically involve cultured cells expressing dopamine D2 or D3 receptors. The compound's ability to inhibit dopamine-induced signaling is assessed by measuring cAMP accumulation or other downstream signaling events. Cells are treated with Amisulpride at various concentrations in the presence or absence of dopamine. The inhibition of signaling is measured, and the IC50 value is determined. The effect of Amisulpride on receptor internalization and other cellular processes can also be studied. |
| 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 hydrochloride (70 mg/kg) was administered to Group 3 participants 23.5, 5 and 1 hour prior to the exam[2]. |
| ADME/Pharmacokinetics |
Amisulpride is a well-characterized drug with established pharmacokinetic properties. Following oral administration, it is rapidly absorbed from the gastrointestinal tract. Amisulpride has a bioavailability of approximately 48%. It is poorly metabolized in the liver and is excreted unchanged in the urine. The elimination half-life is approximately 12 hours. Amisulpride is not significantly protein-bound. The pharmacokinetic profile of amisulpride is linear and dose-proportional.
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| Toxicity/Toxicokinetics |
Amisulpride is a clinically approved antipsychotic with a well-established safety profile. The most common adverse effects are dose-dependent and include extrapyramidal symptoms (e.g., tremors, rigidity, akathisia), hyperprolactinemia (leading to galactorrhea, amenorrhea, and sexual dysfunction), and weight gain. Insomnia, anxiety, and agitation have also been reported. Amisulpride has a lower risk of metabolic side effects, including weight gain and glucose dysregulation, compared to some other atypical antipsychotics.
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| References |
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| Additional Infomation |
Amisulpride is a clinically approved atypical antipsychotic used for the treatment of schizophrenia and acute psychotic episodes. It is available in various formulations, including tablets and oral solutions. Amisulpride is marketed under various brand names in different countries. It is a prescription medication and is not available over the counter. Amisulpride is classified as a selective dopamine D2/D3 receptor antagonist and is considered a first-line treatment for schizophrenia in some guidelines.
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| Molecular Formula |
C17H28CLN3O4S
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|---|---|
| Molecular Weight |
405.938
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| Exact Mass |
405.148
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| Elemental Analysis |
C, 50.30; H, 6.95; Cl, 8.73; N, 10.35; O, 15.76; S, 7.90
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| CAS # |
81342-13-4
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| Related CAS # |
Amisulpride; 71675-85-9
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| PubChem CID |
10046897
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
26
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| Complexity |
549
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN1C(CNC(C2=CC(S(=O)(CC)=O)=C(N)C=C2OC)=O)CCC1.Cl
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| InChi Key |
XFOYXFDTUMXXFP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H27N3O4S.ClH/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);1H
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| Chemical Name |
4-amino-N-[(1-ethylpyrrolidin-2-yl)methyl]-5-ethylsulfonyl-2-methoxybenzamide;hydrochloride
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| Synonyms |
Barhemsys; Solian; APD421; APD 421; APD-421; Amazeo; Aminosultopride; Amipride; Amival; Deniban; AmisulpridaSoltus; DAN-2163; Sulpitac; Sulprix
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: ~50 mg/mL (~135.3 mM)
H2O: ~0.2 mg/mL (~0.5 mM) |
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| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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 : PEG300 ：Tween 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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4634 mL | 12.3171 mL | 24.6342 mL | |
| 5 mM | 0.4927 mL | 2.4634 mL | 4.9268 mL | |
| 10 mM | 0.2463 mL | 1.2317 mL | 2.4634 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.
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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