| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Perospirone targets dopamine D2 receptors, serotonin 5-HT2A receptors, and 5-HT1A receptors. The compound is an orally active antagonist of the 5-HT2A receptor with a Ki of 0.6 nM and dopamine D2 receptor with a Ki of 1.4 nM. It is also a partial agonist of the 5-HT1A receptor with a Ki of 2.9 nM. By blocking dopamine D2 receptors, perospirone reduces dopaminergic neurotransmission, which is thought to contribute to its antipsychotic effects. By antagonizing 5-HT2A receptors, the compound may improve negative symptoms and reduce extrapyramidal side effects compared to typical antipsychotics. The partial agonist activity at 5-HT1A receptors may contribute to its efficacy in treating anxiety and depression associated with schizophrenia. Perospirone's multi-receptor profile is characteristic of atypical antipsychotics.
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| ln Vitro |
In vitro, perospirone demonstrates potent antagonist activity at dopamine D2 and serotonin 5-HT2A receptors, and partial agonist activity at 5-HT1A receptors. The compound binds to 5-HT2A receptors with a Ki of 0.6 nM and dopamine D2 receptors with a Ki of 1.4 nM. It binds to 5-HT1A receptors with a Ki of 2.9 nM, acting as a partial agonist. In receptor binding assays, perospirone shows high affinity for these receptors. In functional assays, the compound antagonizes dopamine-induced and serotonin-induced responses in cells expressing these receptors. Perospirone's in vitro activity supports its use as an atypical antipsychotic.
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| ln Vivo |
In vivo, perospirone demonstrates efficacy in the treatment of schizophrenia. The compound was first launched in Japan in 2001 for the treatment of schizophrenia. Perospirone is an atypical antipsychotic utilized in the study/research of schizophrenia. Sixteen milligrams of perospirone caused over 70% dopamine D2 receptor occupancy near its peak level, then becoming about half after 22 hours. The time courses of receptor occupancy and plasma concentration were quite different. Perospirone's in vivo efficacy in treating schizophrenia and its favorable side effect profile compared to typical antipsychotics support its clinical use. The compound is a non-typical antipsychotic agent.
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| Enzyme Assay |
In vitro receptor binding assays for perospirone employ radioligand displacement techniques using membrane preparations from cells expressing dopamine D2, 5-HT2A, or 5-HT1A receptors. For D2 receptor binding, membranes from cells expressing the D2 receptor are used with radioligands such as [³H]-spiperone or [³H]-raclopride. For 5-HT2A receptor binding, [³H]-ketanserin is used. For 5-HT1A receptor binding, [³H]-8-OH-DPAT is used. The assay involves incubating perospirone at varying concentrations with the membrane preparation and the radioligand. Following incubation, bound and free radioligand are separated by rapid filtration, and radioactivity is measured. Non-specific binding is determined in the presence of a high concentration of an unlabeled competitor. Binding affinity (Ki) values are calculated from competition curves using nonlinear regression analysis.
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| Cell Assay |
In vitro cellular assays for perospirone employ cell lines expressing dopamine D2, 5-HT2A, or 5-HT1A receptors. Cells are cultured in appropriate media and treated with perospirone at various concentrations in the presence or absence of receptor agonists. For D2 receptor studies, readouts may include inhibition of forskolin-stimulated cAMP accumulation. For 5-HT2A receptor studies, readouts may include inhibition of agonist-induced calcium flux. For 5-HT1A receptor studies, readouts may include inhibition of forskolin-stimulated cAMP accumulation (agonist activity). The compound's effects on cell viability and proliferation can be assessed using standard cytotoxicity assays.
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| Animal Protocol |
In vivo animal experiments for perospirone employ models of schizophrenia and other behavioral disorders. For antipsychotic studies, animal models such as amphetamine-induced hyperactivity or apomorphine-induced climbing are used. Perospirone is administered orally or intraperitoneally, and behavior is quantified. For receptor occupancy studies, animals are administered perospirone, and receptor occupancy is measured by PET or ex vivo binding assays. For pharmacokinetic studies, blood samples are collected at various time points, and perospirone concentrations are measured by HPLC or mass spectrometry. Dosing regimens vary depending on the experimental objectives.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of perospirone have been characterized in humans. Perospirone is rapidly absorbed and rapidly eliminated. In healthy subjects, plasma concentrations of perospirone and its active metabolite ID-15036 peaked at 1 hour after administration, with half-lives of 2.2 and 1.9 hours, respectively. The elimination half-life of perospirone is approximately 1-3 hours, and it reaches its maximum plasma levels within 1-2 hours. Perospirone is metabolized to ID-15036 mainly by CYP3A4. The metabolism of perospirone was significantly inhibited by treatment with itraconazole but not by tandospirone, suggesting that CYP3A4 is significantly involved in its metabolism. Factors such as age, sex and comedications can influence perospirone pharmacokinetics.
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| Toxicity/Toxicokinetics |
The toxicity profile of perospirone is consistent with that of atypical antipsychotics. Common adverse effects include somnolence, akathisia, and extrapyramidal symptoms. Hyperprolactinemia may occur due to D2 receptor antagonism. Weight gain and metabolic disturbances may occur, although the risk may be lower than with some other atypical antipsychotics. The compound should be used with caution in patients with a history of cardiovascular disease, seizures, or hepatic impairment. Perospirone is approved for use in Japan for the treatment of schizophrenia. The compound's safety in pregnancy and lactation has not been established, and its use should be guided by clinical judgment.
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| References |
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| Additional Infomation |
See also: Perospirone (note moved to).
Perospirone HCl is an orally active atypical antipsychotic agent with dopamine D2 and serotonin 5-HT2A receptors antagonist, and 5-HT1A receptor agonist properties. It binds to 5-HT2A receptors with a Ki of 0.6 nM, dopamine D2 receptors with a Ki of 1.4 nM, and 5-HT1A receptors with a Ki of 2.9 nM. Perospirone is used for the treatment of schizophrenia and was first launched in Japan in 2001. In healthy subjects, plasma concentrations peaked at 1 hour after administration, with half-lives of 2.2 and 1.9 hours for perospirone and its metabolite ID-15036, respectively. Perospirone has a molecular weight of 463.04 and a molecular formula of C₂₃H₃₀N₄O₂S·HCl. It is also known as SM-9018. |
| Molecular Formula |
C23H30N4O2S.HCL
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| Molecular Weight |
463.03584
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| Exact Mass |
462.185
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| CAS # |
129273-38-7
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| Related CAS # |
Perospirone;150915-41-6
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| PubChem CID |
115367
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| Appearance |
White to off-white solid powder
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| Boiling Point |
667.4ºC at 760 mmHg
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| Melting Point |
95-970ºC
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| Flash Point |
357.4ºC
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| LogP |
4.116
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
31
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| Complexity |
615
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1CC[C@@H]2[C@H](C1)C(=O)N(CCCCN3CCN(CC3)C4=NSC5=CC=CC=C54)C2=O.Cl
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| InChi Key |
HIZFAPMOZFYELI-GNXQHMNLSA-N
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| InChi Code |
InChI=1S/C23H30N4O2S.ClH/c28-22-17-7-1-2-8-18(17)23(29)27(22)12-6-5-11-25-13-15-26(16-14-25)21-19-9-3-4-10-20(19)30-24-21;/h3-4,9-10,17-18H,1-2,5-8,11-16H2;1H/t17-,18+;
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| Chemical Name |
(3aR,7aS)-2-[4-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]butyl]-3a,4,5,6,7,7a-hexahydroisoindole-1,3-dione;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, avoid exposure to moisture. |
| 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) |
DMSO : ~125 mg/mL (~269.96 mM)
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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 | 2.1596 mL | 10.7982 mL | 21.5964 mL | |
| 5 mM | 0.4319 mL | 2.1596 mL | 4.3193 mL | |
| 10 mM | 0.2160 mL | 1.0798 mL | 2.1596 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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