Home Neuronal Signaling Dopamine Receptor antagonist - Norepinephrine antagonist Lurasidone HCl

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Lurasidone HCl Dopamine Receptor antagonist

Cat.No.S3044

Lurasidone (SM-13496) is an atypical antipsychotic, inhibits Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C with IC50 of 1.68 nM, 2.03 nM, 0.495 nM, 6.75 nM and 10.8 nM, respectively.
Lurasidone HCl Dopamine Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 529.14

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Quality Control

Batch: S304401 4-Methylpyridine]15 mg/mL]true]DMSO]1 mg/mL]false]Water]Insoluble]false Purity: 99.97%
99.97

Chemical Information, Storage & Stability

Molecular Weight 529.14 Formula

C28H36N4O2S.HCl

 Storage (From the date of receipt)
CAS No. 367514-88-3 Download SDF Storage of Stock Solutions

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

Solubility

In vitro
Batch:

4-Methylpyridine : 15 mg/mL

DMSO : 1 mg/mL (1.88 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

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Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
5-HT7 [1]
0.495 nM
D2 receptor [1]
1.68 nM
5-HT2A [1]
2.03 nM
5-HT1A [1]
6.75 nM
noradrenaline α2C [1]
10.8 nM
In vitro
Lurasidone antagonizes dopamine-stimulated [35S]GTPγS binding at human dopamine D2L receptor in a concentration-dependent manner with a KB value of 2.8 nM. Lurasidone antagonizes 5-HT-stimulated cAMP accumulation in the CHO/h5-HT7 cells with a KB value of 2.6 nM. Lurasidone partially stimulates [35S]GTPγS binding to the membrane preparation for human 5-HT1A receptors with a maximum effect of 33%. Lurasidone dose-dependently increases the ratio of DOPAC/dopamine in rat frontal cortex and striatum. [1]
In vivo
The inhibitory actions of Lurasidone on MAP-induced hyperactivity persists for more than 8 hours, and the ED50 values of the action at 1 hour, 2 hours, 4 hours, and 8 hours after the treatment are 2.3 mg/kg, 0.87 mg/kg, 1.6 mg/kg, and 5.0 mg/kg, respectively. Lurasidone (1 mg/kg–10 mg/kg) dose-dependently inhibits conditioned avoidance response in rats with ED50 of 6.3 mg/kg. Lurasidone dose-dependently inhibits TRY-induced forepaw clonic seizure and p-CAMP-induced hyperthermia in rats with ED50 of 5.6 mg/kg and 3.0 mg/kg, respectively. Lurasidone (0.3 mg/kg–30 mg/kg) dose-dependently and significantly increases the number of shocks received by rats in the Vogel's conflict test with MED of 10 mg/kg. Lurasidone (3 mg/kg, 2 weeks) significantly suppresses hyperactivity behavior in olfactory bulbectomy model rats. Lurasidone (700 mg/kg–1000 mg/kg) slightly prolongs the duration of loss of righting reflexes elicited by hexobarbital (anesthesia) in mice in a dose-dependent manner. [1] Lurasidone (30 mg/kg, p.o.) significantly and dose-dependently reverses the MK-801-induced impairment of the passive-avoidance response of rats. [2] Lurasidone (3 mg/kg p.o.) potently reverses MK-801-induced learning impairment in the Morris water maze test in rats. Lurasidone (3 mg/kg p.o.) potently reverses MK-801-induced reference memory impairment and moderately but not significantly attenuates MK-801-induced working memory impairment in the radial-arm maze test. [3] Lurasidone (10 mg/kg) treatment increases total BDNF mRNA levels in rat prefrontal cortex and, to less extent, in hippocampus. Lurasidone (10 mg/kg) significantly increases the levels of mature BDNF protein in rat prefrontal cortex, without affect the protein levels of the neurotrophin (both precursor and mature forms) in hippocampal extracts. [4]
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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