| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vivo |
Sultopride, also known as LIN-1418, is a dopamine D2 receptor selective antagonist. In the striatum, nucleus accumbens, and medial prefrontal cortex, rats treated with sulpiride and sulpiride had greater DOPAC and HVA levels than rats in the control group. The rats treated with sulpiride had increased levels of DOPAC and HVA in the striatum compared to the animals not treated with sulpiride (p<0.05). Rats treated with sulpiride had greater DOPAC levels in the nucleus accumbens than rats not treated with sulpiride (p<0.05). DOPAC and HVA levels were higher in the striatum or nucleus accumbens of sultopride-treated rats than in the medial prefrontal cortex (p<0.05) [1].
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Excretion of amisulpride into breastmilk is higher than with other pharmacologically similar drugs. Most information on amisulpride is with continuous oral use as a psychotherapeutic agent. For these uses, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.[1-3] After a single dose for post-operative nausea and vomiting, the manufacturer suggests waiting 48 hours before resuming breastfeeding; however, with a half-life of 4 to 5 hours, a waiting period of 12 to 24 hours should be adequate to avoid large amounts being excreted into breastmilk. ◉ Effects in Breastfed Infants A 13-month-old infant was partially breastfed by a mother who was taking amisulpride 400 mg, fluvoxamine 200 mg, and azathioprine 150 mg daily, and was using nicotine chewing gum for smoking cessation. The mother had been taking amisulpride for 9 days; the duration of the other medications was not stated. A pediatric examination found the infant to be developing well.[5] A woman with long-standing schizophrenia was treated with amisulpride 400 mg and haloperidol 5 mg daily throughout most of her pregnancy and during breastfeeding (extent not stated). Follow-up of the breastfed infant for 13 months by a pediatrician found no adverse effects and normal development of the infant.[7] ◉ Effects on Lactation and Breastmilk Amisulpride increases serum prolactin and may cause galactorrhea at a higher rate than other psychotropic drugs.[8-16] The prolactin level in a mother with established lactation may not affect her ability to breastfeed. |
| References |
[1]. Moriuchi K, et al. Differences in effects of sultopride and sulpiride on dopamine turnover in rat brain. Neurochem Res. 1995 Jan;20(1):95-9
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| Additional Infomation |
Sultopride is a member of salicylamides.
Sultopride is used in Japan, Hong Kong, and Europe to treat schizophrenia. It is of the drug class atypical antipsychotics. A benzamide derivative that is used as an antipsychotic agent for the treatment of schizophrenia. It is also used as an antidepressive agent. |
| Molecular Formula |
C17H26N2O4S
|
|---|---|
| Molecular Weight |
354.46
|
| Exact Mass |
354.161
|
| CAS # |
53583-79-2
|
| Related CAS # |
Sultopride hydrochloride;23694-17-9
|
| PubChem CID |
5357
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.16g/cm3
|
| Boiling Point |
530ºC at 760mmHg
|
| Flash Point |
274.3ºC
|
| LogP |
3.112
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
24
|
| Complexity |
517
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(NCC1N(CC)CCC1)C2=CC(S(=O)(CC)=O)=CC=C2OC
|
| InChi Key |
UNRHXEPDKXPRTM-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H26N2O4S/c1-4-19-10-6-7-13(19)12-18-17(20)15-11-14(24(21,22)5-2)8-9-16(15)23-3/h8-9,11,13H,4-7,10,12H2,1-3H3,(H,18,20)
|
| Chemical Name |
N-[(1-ethylpyrrolidin-2-yl)methyl]-5-ethylsulfonyl-2-methoxybenzamide
|
| Synonyms |
LIN-1418; LIN 1418; Sultopride
|
| 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)
|
| 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
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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 | 2.8212 mL | 14.1060 mL | 28.2119 mL | |
| 5 mM | 0.5642 mL | 2.8212 mL | 5.6424 mL | |
| 10 mM | 0.2821 mL | 1.4106 mL | 2.8212 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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