| Size | Price | Stock | Qty |
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| 10mg |
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| 1g | |||
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| Targets |
Dopamine D2 receptor. Ordopidine is a dopamine D2 receptor antagonist. Dopamine D2 receptors are G protein-coupled receptors that play a critical role in the regulation of motor function, reward, motivation, and cognition. By antagonizing D2 receptors, Ordopidine modulates dopaminergic signaling. The compound is a dopaminergic stabilizer that can inhibit hyperactivity caused by psychostimulants and stimulate behavior in states of hypoactivity. Ordopidine significantly increases the level of dopamine and noradrenalin in the forebrain and concurrently inhibits the over-activity. This dual action of stabilizing dopaminergic tone makes Ordopidine a potential therapeutic agent for Parkinson's disease and psychosis.
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| ln Vitro |
Ordopidine is a dopamine D2 receptor antagonist that can inhibit hyperactivity caused by psychostimulants and stimulate behavior in states of hypoactivity. The compound significantly increases the level of dopamine and noradrenalin in the forebrain and concurrently inhibits the over-activity. Ordopidine has potential applications in treating a range of neuropsychiatric disorders due to its dopaminergic stabilizing effects. The compound's activity has been characterized in receptor binding and functional assays measuring D2 receptor antagonism. Ordopidine is a small molecule dopaminergic stabilizer developed for Parkinson's disease and psychosis.
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| ln Vivo |
Ordopidine has been studied in vivo in animal models and clinical trials. The compound is a dopaminergic stabilizer that can inhibit hyperactivity caused by psychostimulants and stimulate behavior in states of hypoactivity. Ordopidine significantly increases the level of dopamine and noradrenalin in the forebrain and concurrently inhibits the over-activity. In May 2016, Phase-I clinical trials in Parkinson's disease in Germany was discontinued. The compound reached Phase II clinical trials. Detailed pharmacokinetic and pharmacodynamic data are available from preclinical and clinical studies. Ordopidine is for research use only and is not for human therapeutic use.
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| Enzyme Assay |
Dopamine D2 receptor binding assays are performed using membranes prepared from cells expressing recombinant D2 receptors or from striatal tissue. Radioligand binding studies use [³H]-spiperone or [³H]-raclopride as labeled ligands. Membrane preparations are incubated with varying concentrations of Ordopidine and a fixed concentration of radioligand in binding buffer (50 mM Tris-HCl pH 7.4, 120 mM NaCl, 5 mM KCl, 2 mM CaCl₂, 1 mM MgCl₂) for 60-120 minutes at room temperature. Non-specific binding is determined using excess haloperidol. Bound radioactivity is measured by scintillation counting after filtration through GF/B filters. IC50 and Ki values are calculated by non-linear regression. Functional assays measure D2 receptor-mediated inhibition of cAMP accumulation.
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| Cell Assay |
Cellular D2 receptor antagonism is evaluated in cell lines expressing recombinant D2 receptors (e.g., HEK-293 cells). Cells are cultured in appropriate media at 37°C with 5% CO₂ and treated with Ordopidine at various concentrations. Functional assays measure receptor-mediated inhibition of cAMP accumulation (Gi-coupled receptor) in response to dopamine or other agonists. The compound's antagonist activity is assessed by its ability to inhibit dopamine-induced inhibition of cAMP. Cell viability is assessed using MTT or LDH assays. Each experiment includes known dopamine receptor antagonists (e.g., haloperidol) as positive controls and vehicle controls.
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| Animal Protocol |
In vivo efficacy of Ordopidine was evaluated in animal models of Parkinson's disease and psychosis, and in clinical trials. The compound is administered orally or intraperitoneally at doses determined by preclinical studies. In animal models, behavioral assessments include tests of motor function and psychostimulant-induced hyperactivity. Dopamine and noradrenalin levels in the forebrain are measured by HPLC. In May 2016, Phase-I clinical trials in Parkinson's disease in Germany was discontinued. The compound reached Phase II clinical trials. Sample sizes in clinical trials typically range from 20-100 patients per group.
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| ADME/Pharmacokinetics |
Molecular Weight: 285.38. Formula: C14H20FNO2S. CAS No.: 871351-60-9. IUPAC Name: 1-ethyl-4-(2-fluoro-3-(methylsulfonyl)phenyl)piperidine. Synonyms: ACR325, ACR-325. Appearance: Solid. Purity: Typically >98%. Solubility: Soluble in DMSO. Storage: Typically at -20°C. Ordopidine is a dopamine D2 receptor antagonist and dopaminergic stabilizer.
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| Toxicity/Toxicokinetics |
No comprehensive toxicology data are publicly available for Ordopidine. The compound is intended for research use only and has not undergone full preclinical toxicology evaluation required for clinical development. As a dopamine D2 receptor antagonist, potential adverse effects may include extrapyramidal symptoms, sedation, and hyperprolactinemia. Standard toxicity studies would include acute toxicity assessment in rodents, repeated dose toxicity studies (14-day and 28-day), and genotoxicity screening (Ames test, micronucleus assay). The compound is for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
ACR325 was developed specifically for the treatment of Parkinson's disease and psychosis, including bipolar disorder, for which existing therapies have limited efficacy and significant side effects. ACR325 is a dopaminergic stabilizer that has shown promising efficacy in motor function and psychotic disease models.
Drug Indications Investigations are underway for the treatment of mood disorders, bipolar disorder, and psychosis. Mechanism of Action ACR325 is a dopaminergic stabilizer. This compound significantly increases dopamine and norepinephrine levels in the forebrain while inhibiting excessive dopamine activity in other brain regions without adversely affecting motor function. Ordopidine is also known as ACR325 and ACR-325. Its IUPAC name is 1-ethyl-4-(2-fluoro-3-(methylsulfonyl)phenyl)piperidine. Ordopidine is a small molecule dopaminergic stabilizer developed for the potential treatment of Parkinson's disease and psychosis. It is a dopamine D2 receptor antagonist. The compound can inhibit hyperactivity caused by psychostimulants and stimulate behavior in states of hypoactivity. In May 2016, Phase-I clinical trials in Parkinson's disease in Germany was discontinued. The compound reached Phase II clinical trials. No regulatory approvals have been reported. Ordopidine is for research use only. |
| Molecular Formula |
C14H20FNO2S
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| Molecular Weight |
285.3774
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| Exact Mass |
285.12
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| CAS # |
871351-60-9
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| PubChem CID |
11701939
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.447
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
19
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| Complexity |
385
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(N1CCC(C2=CC=CC(S(C)(=O)=O)=C2F)CC1)C
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| InChi Key |
UKUPJASJNQDHPH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H20FNO2S/c1-3-16-9-7-11(8-10-16)12-5-4-6-13(14(12)15)19(2,17)18/h4-6,11H,3,7-10H2,1-2H3
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| Chemical Name |
1-ethyl-4-(2-fluoro-3-methylsulfonylphenyl)piperidine
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| Synonyms |
ACR 325; ACR-325; ACR325
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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 | 3.5041 mL | 17.5205 mL | 35.0410 mL | |
| 5 mM | 0.7008 mL | 3.5041 mL | 7.0082 mL | |
| 10 mM | 0.3504 mL | 1.7520 mL | 3.5041 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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