| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Dopamine D2 receptor in the brain. Timiperone shows strong affinity for dopamine D2 receptors and exerts receptor blocking effects. It promotes dopamine metabolic turnover in the brain.
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|---|---|
| ln Vitro |
Timiperone shows strong affinity for brain dopamine D2 receptors. It exerts antipsychotic activity and inhibits stereotyped behavior in animal models. The compound promotes dopamine metabolic turnover in the brain through receptor blockade. It also increases serum prolactin levels due to dopamine receptor antagonism in the pituitary.
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| ln Vivo |
In vivo, Timiperone treatment in mice increases both the porphyrin content of the Harderian gland and serum prolactin levels. It exhibits strong anti-methamphetamine and anti-apomorphine effects. The compound shows potent antipsychotic effects in animal models of psychiatric disorders. Specific dosing regimens are not detailed in publicly available literature.
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| Enzyme Assay |
Dopamine D2 receptor binding affinity is assessed using in vitro radioligand binding assays with membrane preparations from brain tissue or cells expressing recombinant D2 receptors. Competitive binding with [3H]spiperone or [3H]raclopride is measured. IC50 and Ki values are calculated from displacement curves.
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| Cell Assay |
Cellular activity is evaluated in cell lines expressing dopamine D2 receptors. Receptor-mediated signaling such as cAMP inhibition or calcium mobilization is measured. Prolactin secretion is assessed in pituitary cell cultures. Antipsychotic activity is evaluated in behavioral models including inhibition of apomorphine-induced stereotypy and conditioned avoidance response.
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| Animal Protocol |
In vivo pharmacology is studied in rodent models. Timiperone is administered via intraperitoneal or oral routes. Behavioral assays including stereotypy inhibition, catalepsy, and conditioned avoidance are performed. Harderian gland porphyrin content and serum prolactin levels are measured as pharmacodynamic markers. Dosing typically ranges from 0.1-10 mg/kg.
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| ADME/Pharmacokinetics |
Timiperone has a molecular formula of C22H24FN3OS and molecular weight of 397.51. It is soluble in DMSO. The compound is a butyrophenone derivative. Detailed pharmacokinetic parameters including half-life, oral bioavailability, and metabolic pathways are available in clinical pharmacology literature but not detailed in public search results.
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| Toxicity/Toxicokinetics |
Safety data indicate Timiperone is a pharmaceutical agent with established safety profiles from clinical use. Common side effects associated with butyrophenone antipsychotics include extrapyramidal symptoms, sedation, and hyperprolactinemia. The compound should be handled with appropriate safety precautions as a potent active pharmaceutical ingredient.
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| Additional Infomation |
Timiperone is an aromatic ketone.
Timiperone is an approved antipsychotic medication used clinically in some countries for the treatment of schizophrenia and bipolar disorder. It belongs to the butyrophenone class, similar to haloperidol. The compound exerts its therapeutic effects through dopamine D2 receptor antagonism. It is not approved in all regions and availability may vary. |
| Molecular Formula |
C22H24FN3OS
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|---|---|
| Molecular Weight |
397.51
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| Exact Mass |
397.162
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| CAS # |
57648-21-2
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| PubChem CID |
3033151
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.31
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| Boiling Point |
560.8ºC at 760 mmHg
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| Melting Point |
201-203ºC
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| Flash Point |
293ºC
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| Index of Refraction |
1.664
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| LogP |
5.075
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
558
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C(N2C(=S)NC3C2=CC=CC=3)CCN(CCCC(C2C=CC(F)=CC=2)=O)C1
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| InChi Key |
YDLQKLWVKKFPII-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H24FN3OS/c23-17-9-7-16(8-10-17)21(27)6-3-13-25-14-11-18(12-15-25)26-20-5-2-1-4-19(20)24-22(26)28/h1-2,4-5,7-10,18H,3,6,11-15H2,(H,24,28)
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| Chemical Name |
1-(4-fluorophenyl)-4-[4-(2-sulfanylidene-3H-benzimidazol-1-yl)piperidin-1-yl]butan-1-one
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| Synonyms |
Tolopelon; Timiperonum; Timiperone
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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) |
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 | 2.5157 mL | 12.5783 mL | 25.1566 mL | |
| 5 mM | 0.5031 mL | 2.5157 mL | 5.0313 mL | |
| 10 mM | 0.2516 mL | 1.2578 mL | 2.5157 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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