1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
    Dopamine Receptor

Lurasidone (Synonyms: SM-13496)

Cat. No.: HY-B0032A
Handling Instructions

Lurasidone is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.

For research use only. We do not sell to patients.

Lurasidone Chemical Structure

Lurasidone Chemical Structure

CAS No. : 367514-87-2

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50 mg USD 120 Get quote
100 mg USD 180 Get quote

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Lurasidone is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.

IC50 & Target

IC50: 1.68 nM (dopamine D2), 0.495 nM (5-HT7), 6.75 nM (5-HT1A)[1]

In Vitro

Lurasidone is an antagonist of dopamine D2 and 5-HT7 with IC50s of 1.68±0.09 and 0.495±0.090 nM, respectively. Lurasidone is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75±0.97 nM. In vitro receptor binding experiments reveal that Lurasidone demonstrates affinity for dopamine D2 and 5-HT2A receptors higher than other tested antipsychotics. Lurasidone does not increase [35S]GTPγS binding to the membrane preparations for dopamine D2 receptors by itself, but it antagonizes dopamine-stimulated [35S]GTPγS binding in a concentration-dependent manner with a KB value of 2.8±1.1 nM[1].

In Vivo

Lurasidone dose-dependently increases the ratio of DOPAC/dopamine in frontal cortex and striatum, but it shows a preferential effect on the frontal cortex compare with the striatum, especially at higher doses. Lurasidone (ED50 values 2.3 to 5.0 mg/kg) shows a comparable potency with olanzapine (ED50 values 1.1 to 5.1 mg/kg), higher potency than clozapine (ED50 9.5 to 290 mg/kg), and slightly lower potency than haloperidol (ED50 values 0.44 to 1.7 mg/kg). Lurasidone (1 to 10 mg/kg) dose-dependently inhibits conditioned avoidance response (CAR) in rats, and the ED50 values are 6.3 mg/kg. Lurasidone dose-dependently inhibits tryptamine (TRY)-induced forepaw clonic seizure and p-chloroamphetamine (p-CAMP)-induced hyperthermia with ED50 values of 5.6 and 3.0 mg/kg, respectively. Lurasidone (0.3 to 30 mg/kg) dose-dependently and significantly increases the number of shocks received by rats in the conflict test with MED of 10 mg/kg (p<0.01)[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0297 mL 10.1486 mL 20.2972 mL
5 mM 0.4059 mL 2.0297 mL 4.0594 mL
10 mM 0.2030 mL 1.0149 mL 2.0297 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Stock solution of LUR at 1 mg/mL is prepared in methanol using LUR hydrochloride. Stock solutions of LUR tablets at 1 mg/mL are prepared in methanol[2].

References
Kinase Assay
[1]

[35S]GTPγS binding experiments for the human dopamine D2L or 5-HT1A receptors stably expressed in the membranes of recombinant Chinese hamster ovary (CHO) cells are performed. Shortly after dopamine (or serotonin) and/or Lurasidone are incubated for 20 min at room temperature with the cell membrane preparation containing [35S]GTPγS (0.05 nM for D2L or 0.2 nM for 5-HT1A), the membranes are filtered through glass filters and the radioactivity bound to each filter is measured with a liquid scintillation counter[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

SD rats are individually isolated in clear plastic cages and injected with methamphetamine (MAP) (1 mg/kg i.p.) 1 h after the administration of drugs or vehicle. In the test of persistence of the effect, Lurasidone is administered 1, 2, 4, and 8 h before the MAP injection. Locomotor activity is measured for 80 min from 10 min after MAP injection. Four or five groups of 6 to 13 rats are used to calculate the ED50 value that inhibits MAP-induced hyperactivity by 50% of the animals tested[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

492.68

Formula

C₂₈H₃₆N₄O₂S

CAS No.

367514-87-2

SMILES

O=C([[email protected]]1[[email protected]]2C[[email protected]](CC2)[[email protected]@H]31)N(C[[email protected]](CCCC4)[[email protected]@H]4CN5CCN(CC5)C6=NSC7=CC=CC=C67)C3=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Lurasidone
Cat. No.:
HY-B0032A
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Lurasidone

Cat. No.: HY-B0032A