| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
Purity: ≥98%
| Targets |
Tiapride HCl targets dopamine D2 and D3 receptors. It acts as a selective antagonist at these receptors, blocking the effects of dopamine in the central nervous system. This antagonism is thought to be responsible for its antipsychotic, antiemetic, and antidyskinetic effects. Unlike many other antipsychotics, it has low affinity for D1 receptors and serotonin receptors.
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| ln Vitro |
In vitro, tiapride HCl demonstrates selective binding to dopamine D2 and D3 receptors in radioligand binding assays. Its affinity for these receptors is in the nanomolar range. It shows low affinity for D1 receptors and other neurotransmitter receptors, confirming its selectivity. Its functional activity is confirmed by its ability to block dopamine-induced signaling in cellular assays.
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| ln Vivo |
In vivo, tiapride HCl is used clinically to manage various conditions. It is effective in treating dyskinesias, agitation, and aggression, particularly in elderly patients with dementia or other neuropsychiatric disorders. It is also used as an antiemetic. Its efficacy in reducing tics in Tourette's syndrome and managing alcohol dependence has also been reported.
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| Enzyme Assay |
In vitro receptor binding assays are used to measure the affinity of tiapride HCl for dopamine D2 and D3 receptors. Competition binding assays with radiolabeled ligands are performed using membrane preparations from cells expressing the receptors. The Ki values are determined, confirming its high affinity and selectivity.
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| Cell Assay |
In vitro cellular assays for tiapride HCl measure its functional antagonism at dopamine receptors. Its ability to inhibit dopamine-induced cAMP production in cells expressing D2 or D3 receptors is assessed. These assays confirm its functional activity as a D2/D3 receptor antagonist.
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| Animal Protocol |
In vivo animal experiments for tiapride HCl are conducted in models of dyskinesia, psychosis, and nausea. Its ability to reduce apomorphine-induced stereotypy and conditioned avoidance responses is measured. Its antiemetic effect is evaluated in models of drug-induced emesis.
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| 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 Tiapride HCl has a molecular weight of 364.89 and a molecular formula of C15H24N2O4S·HCl. It is a white to off-white crystalline powder, soluble in water and ethanol. It should be stored at room temperature. Its pharmacokinetic properties include rapid absorption and a half-life of approximately 3-4 hours. |
| Toxicity/Toxicokinetics |
Protein Binding
Ignore The toxicological profile of tiapride HCl is consistent with other dopamine receptor antagonists. Common side effects include sedation, drowsiness, and extrapyramidal symptoms. It may also cause mild hypotension and anticholinergic effects. It is contraindicated in patients with prolactin-dependent tumors and known hypersensitivity. |
| References |
Nagamine T. Severe Hypoglycemia Associated with Tiapride in an Elderly Patient with Diabetes and Psychosis. Innov Clin Neurosci. 2017 Feb 1;14(1-2):12-13. eCollection 2017 Jan-Feb.
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| 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. Tiapride HCl is a selective dopamine D2 and D3 receptor antagonist. It is also known as Tiapridal and Tiapridex. It is used clinically in some countries for the treatment of dyskinesias, agitation, and aggression in elderly patients, as well as an antiemetic. It is a benzamide-class antipsychotic with a specific receptor profile. |
| Molecular Formula |
C15H25CLN2O4S
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| Molecular Weight |
328.4271
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| Exact Mass |
364.122
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| CAS # |
51012-33-0
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| Related CAS # |
Tiapride;51012-32-9
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| PubChem CID |
5467
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| Appearance |
White to off-white solid powder
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| Density |
1.15 g/cm3
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| Boiling Point |
498.1ºC at 760 mmHg
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| Melting Point |
124 °C
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| Flash Point |
255.1ºC
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| LogP |
3.627
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
22
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| Complexity |
443
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C([H])([H])[H])(C1C([H])=C([H])C(=C(C=1[H])C(N([H])C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H])=O)OC([H])([H])[H])(=O)=O
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| InChi Key |
OTFDPNXIVHBTKW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H24N2O4S.ClH/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);1H
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| Chemical Name |
N-(2-(Diethylamino)ethyl)-2-methoxy-5-(methylsulphonyl)benzamide monohydrochloride
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| Synonyms |
Trade names in Italy (Italprid, Sereprile), Japan (Tialaread, Tiaryl, Tiaprim, Tiaprizal), Chile (Sereprid), Germany (Tiaprid, Tiapridex), and China (Tiapride); Tiapride HCl, Tiapride Hydrochloride;
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
H2O : ≥ 200 mg/mL (~548.11 mM)
DMSO : ~31.25 mg/mL (~85.64 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.62 mg/mL (1.70 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 6.2 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: ≥ 0.62 mg/mL (1.70 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 6.2 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: ≥ 0.62 mg/mL (1.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (274.06 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| 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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