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

Lurasidone (Synonyms: SM-13496)

Cat. No.: HY-B0032A Purity: 99.33%
Handling Instructions

Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) 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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  • Biological Activity

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Description

Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) 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 (SM-13496) is an antagonist of dopamine D2 and 5-HT7 with IC50s of 1.68±0.09 and 0.495±0.090 nM, respectively. Lurasidone (SM-13496) 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 (SM-13496) demonstrates affinity for dopamine D2 and 5-HT2A receptors higher than other tested antipsychotics. Lurasidone (SM-13496) 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 (SM-13496) 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 (SM-13496) (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 (SM-13496) (1 to 10 mg/kg) dose-dependently inhibits conditioned avoidance response (CAR) in rats, and the ED50 values are 6.3 mg/kg. Lurasidone (SM-13496) 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 (SM-13496) (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
References
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 (SM-13496) 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

4°C, protect from light

*The compound is unstable in solutions, freshly prepared is recommended.

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