Home Neuronal Signaling Dopamine Receptor antagonist - 5-HT Receptor antagonist lurasidone

research use only

lurasidone Dopamine Receptor antagonist

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

Purity & Quality Control

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

Related Products

Signaling Pathway

Dopamine Receptor Signaling Pathways

Dopamine Receptor Signaling Pathway

Mechanism of Action

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. 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[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. This compound has high binding to human plasma albumin and alpha-1-glycoprotein (≥99%)[2]. 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[1]. In animal studies, this compound 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
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
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4706192/
  • https://pubmed.ncbi.nlm.nih.gov/22570547/

Chemical Information

Molecular Weight 492.68 Formula

C28H36N4O2S
CAS No. 367514-87-2 SDF --
Synonyms SM-13496
Smiles C1CCC(C(C1)CN2CCN(CC2)C3=NSC4=CC=CC=C43)CN5C(=O)C6C7CCC(C7)C6C5=O

Storage and Stability

Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.