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Lurasidone

Catalog No. T21337   CAS 367514-87-2
Synonyms: SM-13496

Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7(IC50=1.68 and 0.495 nM, respectively).It also a partial agonist of 5-HT1A receptor(IC50 : 6.75 nM).

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Lurasidone Chemical Structure
Lurasidone, CAS 367514-87-2
Pack Size Availability Price/USD Quantity
5 mg In stock $ 39.00
10 mg In stock $ 53.00
25 mg In stock $ 78.00
50 mg In stock $ 98.00
100 mg In stock $ 148.00
200 mg In stock $ 217.00
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Purity: 99.5%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7(IC50=1.68 and 0.495 nM, respectively).It also a partial agonist of 5-HT1A receptor(IC50 : 6.75 nM).
Targets&IC50 5-HT 7 Receptor:0.495 nM (IC50), 5-HT 1A Receptor:6.75 nM (IC50), D 2 Receptor:1.68 nM (IC50)
In vitro Lurasidone is administered once daily within the range of 40-160 mg/day for schizophrenia and 20-120 mg/day for bipolar depression, and its pharmacokinetic profile requires administration with food.?In adult healthy subjects and patients, a 40 mg dose results in peak plasma concentrations in 1-3 h, a mean elimination half-life of 18 h (mostly eliminated in the feces), and apparent volume of distribution of 6173 L;?it is approximately 99 % bound to serum plasma proteins.?Lurasidone's pharmacokinetics are approximately dose proportional in healthy adults and clinical populations within the approved dosing range, and this was also found in a clinical study of children and adolescents.?Lurasidone is principally metabolized by cytochrome P450 (CYP) 3A4 with minor metabolites and should not be coadministered with strong CYP3A4 inducers or inhibitors.?Lurasidone does not significantly inhibit or induce CYP450 hepatic enzymes[2].
In vivo In addition to its principal antagonist activity at dopamine D2 and serotonin 5-HT2A receptors, lurasidone has distinctive 5-HT7 antagonistic activity, and displays partial agonism at 5-HT1A receptors, as well as modest antagonism at noradrenergic α2A and α2C receptors.?Lurasidone is devoid of antihistaminic and anticholinergic activities[1].
Synonyms SM-13496
Molecular Weight 492.68
Formula C28H36N4O2S
CAS No. 367514-87-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 17.83 mg/mL (36.19mM), sonification is recommended.

TargetMolReferences and Literature

1. Greenberg W M , Citrome L . Pharmacokinetics and Pharmacodynamics of Lurasidone Hydrochloride, a Second-Generation Antipsychotic: A Systematic Review of the Published Literature[J]. Clinical Pharmacokinetics, 2016. 2. Maurizio, Pompili, Claudio,et al. Lurasidone: efficacy and safety in the treatment of psychotic and mood disorders[J]. Expert Opinion on Drug Safety, 2017. 3. Danek P J, Wójcikowski J, Daniel W A. Asenapine and iloperidone decrease the expression of major cytochrome P450 enzymes CYP1A2 and CYP3A4 in human hepatocytes. A significance for drug-drug interactions during combined therapy[J]. Toxicology and Applied Pharmacology. 2020, 406: 115239.

TargetMolCitations

1. Danek P J, Wójcikowski J, Daniel W A. Asenapine and iloperidone decrease the expression of major cytochrome P450 enzymes CYP1A2 and CYP3A4 in human hepatocytes. A significance for drug-drug interactions during combined therapy. Toxicology and Applied Pharmacology. 2020, 406: 115239 2. Danek P J, Daniel W A.The Novel Atypical Antipsychotic Lurasidone Affects Cytochrome P450 Expression in the Liver and Peripheral Blood Lymphocytes.International Journal of Molecular Sciences.2023, 24(23): 16796.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Clinical Compound Library FDA-Approved Drug Library Clinical Compound Library NO PAINS Compound Library Neuronal Signaling Compound Library Anti-Alzheimer's Disease Compound Library GPCR Compound Library

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Keywords

Lurasidone 367514-87-2 GPCR/G Protein Neuroscience 5-HT Receptor Dopamine Receptor SM 13496 SM-13496 SM13496 inhibit Serotonin Receptor 5-hydroxytryptamine Receptor Inhibitor inhibitor

 

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