Home Neuronal Signaling Dopamine Receptor antagonist Lurasidone HCl For research use only.

Lurasidone HCl

Synonyms: SM-13496

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 Chemical Structure

Lurasidone HCl Chemical Structure

CAS: 367514-88-3

Selleck's Lurasidone HCl has been cited by 1 publication

Purity & Quality Control

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

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Biological Activity

Description 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.
Targets
5-HT7 [1] D2 receptor [1] 5-HT2A [1] 5-HT1A [1] noradrenaline α2C [1]
0.495 nM 1.68 nM 2.03 nM 6.75 nM 10.8 nM
In vitro
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
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]
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

Chemical lnformation & Solubility

Molecular Weight 529.14 Formula

C28H36N4O2S.HCl
CAS No. 367514-88-3 SDF Download Lurasidone HCl SDF
Smiles C1CCC(C(C1)CN2CCN(CC2)C3=NSC4=CC=CC=C43)CN5C(=O)C6C7CCC(C7)C6C5=O.Cl
Storage (From the date of receipt)

In vitro
Batch:

4-Methylpyridine : 15 mg/mL

DMSO : 1 mg/mL ( (1.88 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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