| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Sulpiride targets dopamine D2 and D3 receptors, acting as a selective antagonist. It has a Ki of 4.2 nM for D2 and 15 nM for D3 receptors. Unlike most other neuroleptics which block both dopamine D1 and D2 receptors, sulpiride is more selective and acts primarily as a dopamine D2 antagonist. Sulpiride appears to lack effects on norepinephrine, acetylcholine, serotonin, histamine, or GABA receptors.
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|---|---|
| ln Vitro |
Sulpiride is an orally active dopamine D2/D3 receptor antagonist. It has antipsychotic and antidepressant properties. It can be used to treat schizophrenia or senile dementia without producing major extrapyramidal side effects. Sulpiride can be used in research into anxiety, depression, and breast cancer.
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| ln Vivo |
Sulpiride is used in vivo for the treatment of acute and chronic schizophrenia. It has antidepressant and antiemetic properties. It is used in research into anxiety, depression, and breast cancer. Sulpiride is administered orally.
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| Enzyme Assay |
Sulpiride is a dopamine receptor antagonist, and its in vitro activity is assessed in radioligand binding assays. In a typical assay, the compound is incubated with membranes expressing dopamine receptors and a radiolabeled ligand. The displacement of the radiolabeled ligand is measured, and the Ki is determined.
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| Cell Assay |
Sulpiride is dissolved in DMSO and applied to cultured cells at concentrations ranging from 1 nM to 10 µM. The effect on dopamine receptor signaling is assessed by measuring cAMP accumulation.
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| ADME/Pharmacokinetics |
Sulpiride has a molecular weight of approximately 340 g/mol. It is an orally active compound. The compound is typically stored as a powder at room temperature. Sulpiride is a member of benzamides, a sulfonamide, and an N-alkylpyrrolidine.
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| Toxicity/Toxicokinetics |
Sulpiride has a manageable toxicity profile. Common side effects include extrapyramidal symptoms (such as akathisia, dystonia, and parkinsonism), hyperprolactinemia (leading to galactorrhea and amenorrhea), and weight gain. Sedation and gastrointestinal disturbances are also reported.
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| Additional Infomation |
Sulpiride is a substituted benzamide derivative classified as an atypical antipsychotic agent. It functions primarily as a selective antagonist of dopamine D2 and D3 receptors, with a Ki of 4.2 nM for D2 and 15 nM for D3. Sulpiride is an orally active dopamine D2/D3 receptor antagonist. It is used in research into anxiety, depression, and breast cancer. Sulpiride is indicated for the treatment of acute and chronic schizophrenia.
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| Molecular Formula |
C15H23N3O4S
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|---|---|
| Molecular Weight |
341.426
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| Exact Mass |
341.14
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| CAS # |
15676-16-1
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| PubChem CID |
5355
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Melting Point |
180 - 185ºC
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| Index of Refraction |
1.552
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| LogP |
0.45
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
23
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| Complexity |
505
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C([H])=C([H])C(=C(C=1[H])C(N([H])C([H])([H])C1([H])C([H])([H])C([H])([H])C([H])([H])N1C([H])([H])C([H])([H])[H])=O)OC([H])([H])[H])(N([H])[H])(=O)=O
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| InChi Key |
BGRJTUBHPOOWDU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H23N3O4S/c1-3-18-8-4-5-11(18)10-17-15(19)13-9-12(23(16,20)21)6-7-14(13)22-2/h6-7,9,11H,3-5,8,10H2,1-2H3,(H,17,19)(H2,16,20,21)
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| Chemical Name |
N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-sulfamoylbenzamide
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| Synonyms |
CCRIS 4248; CCRIS4248; CCRIS-4248
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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 : ~100 mg/mL (~292.89 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.32 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 (7.32 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 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9289 mL | 14.6443 mL | 29.2886 mL | |
| 5 mM | 0.5858 mL | 2.9289 mL | 5.8577 mL | |
| 10 mM | 0.2929 mL | 1.4644 mL | 2.9289 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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