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lurasidone

Name: lurasidone
Brand: Selleck Chemicals
SKU: S5714
Rating: 5 (2 reviews)

Synonyms: SM-13496

Catalog No.S5714 Purity: 99.96%

Lurasidone (SM-13496) is a second-generation antipsychotic agent that exhibits full antagonism at dopamine D2 and serotonin 5-HT2A receptors with binding affinities Ki = 1 nM and Ki = 0.5 nM, respectively. It also has high affinity for serotonin 5-HT7 receptors (Ki = 0.5 nM), partial agonist activity at 5-HT1A receptors (Ki = 6.4 nM) and lacks affinity for histamine H1 and muscarinic M1 receptors.

lurasidone Chemical Structure

CAS: 367514-87-2

Selleck's lurasidone has been cited by 2 publications

Purity & Quality Control

Batch: S571401 DMSO] 7 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.96%

99.96

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Biological Activity

Description

Targets

5-HT2A ^[1] (Cell-free assay)	5-HT7 receptor ^[1] (Cell-free assay)	D2 receptor ^[1] (Cell-free assay)	5-HT1A receptor ^[1] (Cell-free assay)
0.5 nM(Ki)	0.5 nM(Ki)	1 nM(Ki)	6.4 nM(Ki)

In vitro
In vitro	Lurasidone is a new atypical antipsychotic in the benzoisothiazoles class of chemicals. Like most second-generation antipsychotics it is a full antagonist at dopamine D2 and serotonin 5-HT2A receptors, and is a partial agonist at 5-HT1A receptors. It has much greater affinity for 5-HT7 subtype receptors than other atypical antipsychotics. Lurasidone also has high affinity for the 5-HT1A subtype, α2c-adrenergic receptors and low affinity for α1-adrenergic receptors. It has minimal affinity for 5-HT2C receptors and negligible affinity for histamine H1 and muscarinic receptors^[2].

In Vivo
In vivo	Lurasidone is rapidly absorbed, reaching peak concentrations within 1.5–3 hours (tmax) after single and multiple oral doses. Once absorbed, it extensively distributes in tissues and rapidly enters the CNS. Lurasidone has high binding to human plasma albumin and alpha-1-glycoprotein (≥99%)^[2]. Long-term treatment of schizophrenia with lurasidone has been shown to reduce the risk of relapse. The elimination half-life of lurasidone is about 20-40 h. Mean Cmax and area under the curve (AUC) for lurasidone were approximately threefold and twofold greater, respectively, in a comparison of administration with food v. fasting. Lurasidone absorption is independent of food fat content. Lurasidone is metabolised primarily via CYP3A4^[1]. In animal studies, lurasidone penetrated the placental barrier and distributed into the fetus, and was excreted in milk during lactation^[2].

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT03627195	Completed	Schizophrenia	Sumitomo Pharma America Inc.	June 7 2018	Phase 1
NCT02731612	Recruiting	Bipolar Disorder	Nazlin Walji\|University of British Columbia	May 8 2017	Phase 3
NCT02147379	Completed	Bipolar I Disorder	University of British Columbia	May 2014	Phase 3
NCT02174523	Completed	Schizophrenia	Sumitomo Pharma (Suzhou) Co. Ltd.\|Xuhui Central Hospital Shanghai	April 2014	Phase 1

References

Chemical lnformation & Solubility

Molecular Weight	492.68	Formula	C₂₈H₃₆N₄O₂S
CAS No.	367514-87-2	SDF	--
Smiles	C1CCC(C(C1)CN2CCN(CC2)C3=NSC4=CC=CC=C43)CN5C(=O)C6C7CCC(C7)C6C5=O
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 7 mg/mL ( (14.2 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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