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lurasidone Dopamine Receptor antagonist

Cat.No.S5714

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. This compound 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 Dopamine Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 492.68

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 7 mg/mL (14.2 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 492.68 Formula

C28H36N4O2S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 367514-87-2 -- Storage of Stock Solutions

Synonyms SM-13496 Smiles C1CCC(C(C1)CN2CCN(CC2)C3=NSC4=CC=CC=C43)CN5C(=O)C6C7CCC(C7)C6C5=O

Mechanism of Action

Targets/IC50/Ki
5-HT2A
(Cell-free assay)
0.5 nM(Ki)
5-HT7 receptor
(Cell-free assay)
0.5 nM(Ki)
D2 receptor
(Cell-free assay)
1 nM(Ki)
5-HT1A receptor
(Cell-free assay)
6.4 nM(Ki)
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. This compound 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.
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. This compound has high binding to human plasma albumin and alpha-1-glycoprotein (≥99%). Long-term treatment of schizophrenia with this agent has been shown to reduce the risk of relapse. The elimination half-life of this chemical is about 20-40 h. Mean Cmax and area under the curve (AUC) for this drug were approximately threefold and twofold greater, respectively, in a comparison of administration with food v. fasting. Its absorption is independent of food fat content. It is metabolised primarily via CYP3A4. In animal studies, this compound penetrated the placental barrier and distributed into the fetus, and was excreted in milk during lactation.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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

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