| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
PNU-96391 targets dopamine D2 receptors and 5-HT2A serotonin receptors. It acts as an antagonist at dopamine D2 receptors and a partial agonist at 5-HT2A receptors. Dopamine D2 receptors are involved in reward, motivation, and motor control, and are implicated in psychiatric disorders such as schizophrenia and addiction. 5-HT2A receptors are involved in mood, cognition, and perception.
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| ln Vitro |
PNU-96391 demonstrates antagonist activity at dopamine D2 receptors and partial agonist activity at 5-HT2A receptors in vitro. Its binding affinity for these receptors has been characterized in radioligand binding assays. The compound's functional effects have been evaluated in cell-based assays measuring receptor-mediated signaling. Its unique pharmacological profile (D2 antagonist/5-HT2A partial agonist) makes it a valuable research tool.
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| ln Vivo |
PNU-96391 has been studied in vivo for its effects on dopaminergic and serotonergic systems. As a dopamine D2 antagonist and 5-HT2A partial agonist, it may have effects on behavior, motor function, and cognition. It has been investigated for potential therapeutic applications in chronic diseases. Detailed in vivo efficacy data are limited in publicly available sources. The compound is primarily used as a research tool.
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| Enzyme Assay |
Dopamine D2 and 5-HT2A receptor binding assays are performed using membranes prepared from cells expressing recombinant receptors or from brain tissue. Radioligand binding studies use [3H]-raclopride (D2) or [3H]-ketanserin (5-HT2A) as labeled ligands. Membrane preparations are incubated with varying concentrations of PNU-96391 and a fixed concentration of radioligand in binding buffer for 60-120 minutes. Non-specific binding is determined using excess unlabeled ligand (e.g., haloperidol for D2, ketanserin for 5-HT2A). Bound radioactivity is measured by scintillation counting after filtration. IC50 and Ki values are calculated by non-linear regression.
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| Cell Assay |
Cellular D2 and 5-HT2A receptor activity is evaluated in cell lines expressing recombinant receptors (e.g., HEK-293 cells transfected with D2 or 5-HT2A). Cells are cultured in appropriate media and treated with PNU-96391 at various concentrations (0.1-100 μM). Functional assays measure receptor-mediated signaling: for D2 receptors, inhibition of cAMP accumulation; for 5-HT2A receptors, calcium mobilization (using Fluo-4 or Fura-2). The compound's antagonist activity at D2 and partial agonist activity at 5-HT2A are characterized. Cell viability is assessed using MTT or LDH assays.
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| Animal Protocol |
In vivo studies are conducted in rodent models of psychiatric or neurological disorders. PNU-96391 is administered orally or intraperitoneally at doses determined by preclinical studies. Behavioral assessments may include tests of locomotor activity, prepulse inhibition, and cognitive function. Brain tissue is collected for neurochemical analysis (dopamine and serotonin levels) and receptor occupancy studies. Sample sizes typically range from 8-12 animals per group. Detailed protocols are not publicly available.
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
PNU-96391 Known human metabolites include 3-(3-(methylsulfonyl)phenyl)piperidine. PNU-96391 has a molecular weight of 281.41 g/mol and a molecular formula of C15H23NO2S. Solubility: DMSO. Storage: typically at -20°C. Bioavailability, half-life, and tissue distribution data are not publicly available. The compound is a research tool for studying dopamine and serotonin receptor pharmacology. |
| Toxicity/Toxicokinetics |
Limited toxicology data are available for PNU-96391. As a dopamine D2 antagonist and 5-HT2A partial agonist, potential toxicities may include effects on the central nervous system, motor function, and cardiovascular system. Standard toxicology studies would include acute and subchronic toxicity in rodents, genotoxicity screening, and evaluation of effects on behavior and motor function. No clinical trials have been reported for this compound. The compound is intended for research use only.
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| References | |
| Additional Infomation |
PNU-96391 is also known as (-)-OSU6162, OSU-6162, and (-)-OSU. Its chemical name is Piperidine, 3-(3-(methylsulfonyl)phenyl)-1-propyl-, (S)-. It is a dopamine D2 antagonist and 5-HT2A partial agonist. It is used in research on chronic diseases. No clinical trials or regulatory approvals have been reported. The compound is for research use only.
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| Molecular Formula |
C15H23NO2S
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| Molecular Weight |
281.41
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| Exact Mass |
281.145
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| CAS # |
146798-66-5
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| PubChem CID |
9795741
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.093g/cm3
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| Boiling Point |
436.523ºC at 760 mmHg
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| Flash Point |
217.802ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.526
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| LogP |
3.698
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
19
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| Complexity |
374
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCCN1CCCC(C2C=CC=C(S(=O)(C)=O)C=2)C1
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| InChi Key |
GZVBVBMMNFIXGE-CQSZACIVSA-N
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| InChi Code |
InChI=1S/C15H23NO2S/c1-3-9-16-10-5-7-14(12-16)13-6-4-8-15(11-13)19(2,17)18/h4,6,8,11,14H,3,5,7,9-10,12H2,1-2H3/t14-/m1/s1
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| Chemical Name |
(3S)-3-(3-methylsulfonylphenyl)-1-propylpiperidine
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| Synonyms |
PNU96391; OSU-6162; PNU-96391
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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 | 3.5535 mL | 17.7677 mL | 35.5353 mL | |
| 5 mM | 0.7107 mL | 3.5535 mL | 7.1071 mL | |
| 10 mM | 0.3554 mL | 1.7768 mL | 3.5535 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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