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Perospirone | CAS No: 150915-41-6 | GMP-certified suppliers
A medication that treats schizophrenia and acute bipolar mania by modulating central nervous system pathways to alleviate psychotic and mood symptoms.
Therapeutic categories
Primary indications
- For the treatment of schizophrenia and acute cases of bipolar mania
Product Snapshot
- Perospirone is an oral small molecule formulation
- It is primarily indicated for the treatment of schizophrenia and acute bipolar mania
- The compound currently holds experimental status without formal approval in key regulatory markets
Clinical Overview
Pharmacodynamically, perospirone exhibits high-affinity antagonism at serotonin 5-HT2A receptors and dopamine D2 receptors. It functions as a serotonin 5-HT2 receptor inverse agonist and a dopamine D2 receptor antagonist, mechanisms central to its clinical efficacy. Additionally, it acts as a partial agonist at 5-HT1A receptors, which serve as autoreceptors modulating serotonin uptake and release. Perospirone also antagonizes dopamine D4 and α1-adrenergic receptors, and behaves as an inverse agonist at histamine H1 receptors, effects potentially related to its sedative and hypotensive properties. Interaction with dopamine D1 receptors occurs at low affinity and is of negligible clinical relevance.
The mechanism of action involves antagonism of D2 receptors within the mesolimbic dopamine pathway, reducing dopaminergic overactivity that contributes to the positive symptoms of schizophrenia such as hallucinations and delusions. Antagonism of 5-HT2A receptors in the nigrostriatal and mesocortical pathways is thought to mitigate negative symptoms and cognitive deficits by modulating dopamine and glutamate neurotransmission. The partial agonism at 5-HT1A receptors further regulates serotonin release, balancing neurotransmitter dynamics implicated in psychosis.
In terms of absorption, distribution, metabolism, and excretion (ADME), perospirone is typically administered as the hydrated hydrochloride salt, enhancing its stability and solubility. It undergoes hepatic metabolism involving cytochrome P450 enzymes, particularly CYP2C8, CYP2D6, CYP3A, and CYP3A4 isoforms, implicating potential drug-drug interactions. Its pharmacokinetic profile supports central nervous system penetration critical for antipsychotic efficacy.
Safety and toxicity considerations include a generally lower incidence of extrapyramidal symptoms relative to first-generation antipsychotics, although monitoring for sedation, hypotension, and metabolic changes is warranted. Neuroleptic malignant syndrome and tardive dyskinesia remain possible risks inherent to dopamine antagonist therapy. As with other antipsychotics, renal and hepatic function monitoring is recommended during treatment.
Perospirone is classified as an experimental agent in some regulatory jurisdictions and is primarily marketed and used clinically within Japan. Branding is mainly associated with its originating company, Dainippon Sumitomo Pharma.
For API procurement, attention to the authenticated hydrated hydrochloride salt form is essential to ensure physicochemical consistency and bioequivalence. Suppliers should provide comprehensive analytical characterization confirming identity, purity, and absence of significant impurities, consistent with pharmacopeial standards and regulatory expectations. Stability under relevant storage conditions and controlled handling to prevent degradation are critical for maintaining API quality.
Identification & chemistry
| Generic name | Perospirone |
|---|---|
| Molecule type | Small molecule |
| CAS | 150915-41-6 |
| UNII | N303OK87DT |
| DrugBank ID | DB08922 |
Pharmacology
| Summary | Perospirone exerts antipsychotic effects primarily through dopamine D2 receptor antagonism in the mesolimbic pathway, mitigating positive symptoms of schizophrenia. It also acts as an inverse agonist at serotonin 5-HT2A receptors and a partial agonist at 5-HT1A receptors, modulating serotonergic neurotransmission to address negative symptoms and cognitive impairments. Additional receptor interactions include antagonism at dopamine D4, α1-adrenergic, and histamine H1 receptors, contributing to its broader pharmacodynamic profile. |
|---|---|
| Mechanism of action | Antagonism at D2 receptors is believed to relieve the positive symptoms of schizophrenia such as delusions, hallucinations, and thought disorders. Perospirone targets the mesolimbic patway to reverse the overactivity of the dopaminergic signalling via D2 receptors . 5-HT2A antagonism is thought to allevaite the negative symptoms and cognitive impairments of schizophrenia. These receptors are Gi/Go coupled receptors that lead to decreased neurotransmitter release and neuronal inhibition when activated, thus play a role in dopamine release regulation. Perospirone targets these receptors in the nigrostriatal pathway to reduce dopamine release and function. In contrast, 5-HT2A receptor antagonism may improve the negative symptoms by enhancing dopamine and glutamate release in the mesocortical pathway . 5-HT1A receptor activation further inhibits the release of 5-HT into the synaptic cleft. |
| Pharmacodynamics | Perospirone is a serotonin 5-HT2 receptor inverse agonist and dopamine D2 receptor antagonist based on receptor binding experiments [A19680, A19681] that binds to both receptors with high affinity. Perospirone is also a partial agonist at 5-HT1A receptors which are autoreceptors that stimulate the uptake of 5-HT and inhibit 5-HT release . It also interacts with D4 receptors and α₁-adrenergic receptors as an antagonist, as well as histamine H1 receptor an inverse agonist. Binding to these receptors may explain sedative and hypotensive actions. Perospirone binds to D1 receptors with low affinity and minimal clinical significance [ A19681]. |
Targets
| Target | Organism | Actions |
|---|---|---|
| 5-hydroxytryptamine receptor 2A | Humans | inverse agonist |
| Dopamine D2 receptor | Humans | antagonist |
| 5-hydroxytryptamine receptor 1A | Humans | partial agonist |
ADME / PK
| Absorption | Perospirone is rapidly absorbed following oral administration with the time to reach peak plasma concentration of 0.8 to 1.5 hours. A single oral dose of 8mg perospirone results in peak plasma concentration of 5.7 ug/L . Perospirone is not reported to be accumulated after repeated dosing. |
|---|---|
| Half-life | The elimination half life is approximately 1.9 hours following oral ingestion of 8mg perospirone . |
| Protein binding | Plasma protein binding ratio is 92% with extensive binding to serum albumin and α1-acid glycoprotein . |
| Metabolism | Perospirone undergoes rapid and extensive first-pass metabolism in the liver; the metabolic pathways involve hydroxylation, N-dealkylation, and S-oxidation, which are catalyzed by CYP1A1, 2C8, 2D6, and 3A4. CYP3A4 is reported to have highest level of contribution in perospirone metabolism. Hydroxyperospirone is formed from hydroxylation of the the cyclohexane-1,2-dicarboximide moiety and retains pharmacological action by mediating antiserotonergic effects, although with lower affinity . |
| Route of elimination | Perospirone is mainly excreted via renal elimination. 0.4% of of total dose is excreted as unchanged drug following oral administration of 8mg perospirone . |
| Volume of distribution | The mean volume of distribution following oral administration of 32 mg/day of perospirone is 1733L, with values ranging from 356-5246 L. It is shown to cross the placenta and be secreted into milk in pregnant rats . |
| Clearance | Apparent clearance rate is approximately 425.5 ± 150.3 L/h in patients receiving a single oral dose of 8mg perospirone . |
Formulation & handling
- Perospirone is a small molecule compound suitable for oral formulation due to its low water solubility and moderate lipophilicity (LogP 3.74). Stability considerations should focus on protecting the solid form from moisture to maintain integrity during storage and handling. As an N-arylpiperazine derivative, Perospirone does not exhibit peptide or biologic sensitivity, allowing standard small molecule formulation techniques.
Regulatory status
Safety
| Toxicity | Frequently experienced adverse effects include extrapyramidal symptoms, insomnia, and drowsiness. More serious adverse effect include neuroleptic malignant syndrome . Oral LD50 value in rats is 870 mg/kg [MSDS]. |
|---|
- May cause extrapyramidal symptoms, insomnia, and drowsiness upon exposure
- Potential risk of neuroleptic malignant syndrome with systemic absorption
- Oral LD50 in rats is 870 mg/kg, indicating moderate acute toxicity
Perospirone is a type of Atypical antipsychotics
Atypical antipsychotics belong to the subcategory of pharmaceutical active pharmaceutical ingredients (APIs) used in the treatment of various mental disorders, particularly schizophrenia and bipolar disorder. These medications are designed to alleviate the symptoms of psychosis by targeting specific neuroreceptors in the brain.
Unlike traditional antipsychotics, atypical antipsychotics exhibit a different pharmacological profile, providing a more favorable side effect profile and improved efficacy. These medications primarily act on dopamine and serotonin receptors, regulating the neurotransmitter levels in the brain to restore the chemical balance.
The mechanism of action of atypical antipsychotics involves blocking dopamine receptors, particularly D2 receptors, as well as modulating serotonin receptors, notably 5-HT2A receptors. By inhibiting excessive dopamine transmission and enhancing serotonin activity, atypical antipsychotics help reduce hallucinations, delusions, and other psychotic symptoms.
Some commonly used atypical antipsychotics include risperidone, olanzapine, quetiapine, and aripiprazole. These APIs are typically formulated into oral tablets or capsules for convenient administration.
Despite their effectiveness, atypical antipsychotics may have potential side effects such as weight gain, metabolic abnormalities, sedation, and extrapyramidal symptoms. Therefore, close monitoring and individualized treatment plans are essential to ensure optimal therapeutic outcomes.
In conclusion, atypical antipsychotics are a crucial subcategory of APIs used in the treatment of mental disorders. Their distinct pharmacological profile and mechanism of action make them valuable in managing psychosis while minimizing adverse effects.
Perospirone (Atypical antipsychotics), classified under Antipsychotics
Antipsychotics belong to the pharmaceutical API (Active Pharmaceutical Ingredient) category used to treat psychiatric disorders such as schizophrenia, bipolar disorder, and other related conditions. These medications play a crucial role in managing symptoms associated with psychosis, including hallucinations, delusions, and disorganized thinking.
Antipsychotics work by modulating the levels of neurotransmitters in the brain, particularly dopamine and serotonin. They can be categorized into two classes: first-generation (typical) antipsychotics and second-generation (atypical) antipsychotics. Typical antipsychotics primarily target dopamine receptors, while atypical antipsychotics also affect serotonin receptors.
The pharmaceutical API category of antipsychotics includes various well-known drugs, such as haloperidol, chlorpromazine, risperidone, quetiapine, and olanzapine. These APIs are often formulated into different dosage forms, including tablets, capsules, injections, and oral suspensions, to provide flexibility in administration and patient-specific needs.
Antipsychotics offer relief from psychotic symptoms by stabilizing the imbalanced neurotransmitter activity in the brain. However, they may also have certain side effects, such as sedation, weight gain, extrapyramidal symptoms, and metabolic disturbances. It is essential for healthcare professionals to carefully monitor patients receiving antipsychotic treatment to optimize therapeutic benefits while minimizing adverse effects.
In summary, antipsychotics are a vital category of pharmaceutical APIs used to manage psychiatric disorders by modulating neurotransmitter activity in the brain. Their effectiveness in treating psychosis has made them a cornerstone of mental health treatment, providing much-needed relief to individuals suffering from these conditions.
Perospirone API manufacturers & distributors
Compare qualified Perospirone API suppliers worldwide. We currently have 1 companies offering Perospirone API, with manufacturing taking place in 1 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
When sending a request, specify which Perospirone API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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