| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
The bioavailability of tipride is approximately 75%. With three daily doses, the time to peak concentration (Tmax) is 0.4–1.5 hours, and the steady-state time (Tss) is 24–48 hours. Benzamide and its derivatives are highly water-soluble but are known to cross the blood-brain barrier, thus requiring carrier-mediated transport. Urinary (70% excreted unchanged as tipride) Tipride distributes rapidly and is almost unbound to plasma proteins, resulting in a relatively high volume of distribution of 16.6 L/h. Metabolisms/Metabolites Tipride is minimally metabolized in the human body; 70% of the drug is excreted unchanged in the urine within 24 hours. Only low concentrations of N-desethyltipride and tipride N-oxide were detected; no phase II metabolites were detected. Biological Half-Life 2.9–3.6 hours |
|---|---|
| Toxicity/Toxicokinetics |
Protein Binding
Ignore |
| Additional Infomation |
N-[2-(diethylamino)ethyl]-2-methoxy-5-methylsulfonylbenzamide belongs to the benzamide class of compounds. Tiapril is a selective D2 and D3 dopamine receptor blocker in the brain. A benzamide derivative used as a dopamine antagonist. See also: Tiapril hydrochloride (note moved to).
Drug Indications Tiapril is indicated for the treatment of a variety of neurological and psychiatric disorders, including movement disorders, alcohol withdrawal syndrome, negative symptoms of psychosis, and agitation and aggression in the elderly. Mechanism of Action Tiapril is a selective dopamine D2 and D3 receptor antagonist, offering advantages over other antipsychotics such as haloperidol and risperidone, which bind to multiple targets, including four of the five known dopamine receptor subtypes. Tiapril binds to a variety of receptors, including D1-4 receptors, 5-HT2A and 5-HT2C receptors, α1 and α2 adrenergic receptors, and histamine H1 receptors. Compared to these drugs, tiapril has a relatively low affinity for its target receptors. At the D2 receptor, a concentration of 320 nM can displace 50% of the 3H-rivalipride binding; at the D3 receptor, a concentration of 180 nM can displace 50% of the 3H-rivalipride binding. Pharmacodynamics Tiapril exhibits high regional selectivity for the limbic system. One study found that tiapril's affinity for the limbic system is more than three times that of the striatum, while haloperidol shows almost equal selectivity for both the limbic system and striatum. Another rat study found that tiapril's affinity for the limbic system region—the septum—is more than thirty times that of the striatum. It has moderate efficacy against D2 receptors, with 80% of the receptors occupied even at excessive concentrations of tipride. |
| Molecular Formula |
C15H24N2O4S
|
|---|---|
| Molecular Weight |
328.42706
|
| Exact Mass |
328.146
|
| CAS # |
51012-32-9
|
| Related CAS # |
Tiapride hydrochloride;51012-33-0
|
| PubChem CID |
5467
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.15 g/cm3
|
| Boiling Point |
498.1ºC at 760 mmHg
|
| Melting Point |
120ºC
|
| Flash Point |
255.1ºC
|
| LogP |
2.825
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
22
|
| Complexity |
443
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCN(CCNC(C1=C(OC)C=CC(S(=O)(C)=O)=C1)=O)CC
|
| InChi Key |
JTVPZMFULRWINT-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C15H24N2O4S/c1-5-17(6-2)10-9-16-15(18)13-11-12(22(4,19)20)7-8-14(13)21-3/h7-8,11H,5-6,9-10H2,1-4H3,(H,16,18)
|
| Chemical Name |
N-[2-(diethylamino)ethyl]-2-methoxy-5-methylsulfonylbenzamide
|
| 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 (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
|
|---|---|
| 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 | 3.0448 mL | 15.2239 mL | 30.4479 mL | |
| 5 mM | 0.6090 mL | 3.0448 mL | 6.0896 mL | |
| 10 mM | 0.3045 mL | 1.5224 mL | 3.0448 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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