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Lurasidone hydrochloride

Catalog No. T1735 CAS 367514-88-3

Synonyms: Lurasidone HCl, SM-13496 (Hydrochloride), SM-13496

Lurasidone hydrochloride (Lurasidone HCl) is a thiazole derivative and atypical antipsychotic agent that functions as a dopamine D2 receptor antagonist; serotonin 5-HT2 receptor antagonist, serotonin 5-HT7 receptor antagonist, an antagonist of the adrenergic α2A and α2C receptors, as well as a partial serotonin 5-HT1A receptor agonist. It is used in the treatment of schizophrenia and bipolar disorder.

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Lurasidone hydrochloride Chemical Structure

Lurasidone hydrochloride, CAS 367514-88-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 35.00
10 mg	In stock	$ 57.00
25 mg	In stock	$ 73.00
50 mg	In stock	$ 97.00
100 mg	In stock	$ 147.00
200 mg	In stock	$ 237.00
500 mg	In stock	$ 497.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 99.48%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Lurasidone hydrochloride (Lurasidone HCl) is a thiazole derivative and atypical antipsychotic agent that functions as a dopamine D2 receptor antagonist; serotonin 5-HT2 receptor antagonist, serotonin 5-HT7 receptor antagonist, an antagonist of the adrenergic α2A and α2C receptors, as well as a partial serotonin 5-HT1A receptor agonist. It is used in the treatment of schizophrenia and bipolar disorder.
Targets&IC50	5-HT1A:6.75 nM, D2 receptor:1.68 nM, Noradrenaline α2C:10.8 nM, 5-HT2A:2.03 nM, 5-HT7:0.495 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]

Synonyms	Lurasidone HCl, SM-13496 (Hydrochloride), SM-13496
Molecular Weight	529.14
Formula	C28H36N4O2S·HCl
CAS No.	367514-88-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5.29 mg/mL (10 mM), Sonification is recommended

References and Literature

1. Ishibashi T, et al. J Pharmacol Exp Ther, 2010, 334(1), 171-181. 2. Ishiyama T, et al. Eur J Pharmacol, 2007, 572(2-3), 160-170. 3. Enomoto T, et al. Behav Brain Res, 2008, 186(2), 197-207. 4. Fumagalli F, et al. Int J Neuropsychopharmacol, 2012, 15(2), 235-246. 5. Danek P J, Wójcikowski J, Daniel W A. The atypical neuroleptics iloperidone and lurasidone inhibit human cytochrome P450 enzymes in vitro. Evaluation of potential metabolic interactions[J]. Pharmacological reports: PR. 2020, 72(6): 1685-1694. 6. Marta Kot, Anna Haduch, Mariusz Papp, Władysława A. Daniel. The effect of chronic treatment with lurasidone on rat liver cytochrome P450 expression and activity in the chronic mild stress (CMS) model of depression [J]. Drug Metabolism and Disposition. 2017, 45(12): 1336-1344.

Citations

1. Danek P J, Daniel W A. The Atypical Antipsychotic Lurasidone Affects Brain but Not Liver Cytochrome P450 2D (CYP2D) Activity. A Comparison with Other Novel Neuroleptics and Significance for Drug Treatment of Schizophrenia. Cells. 2022, 11(21): 3513. 2. Kot M, Haduch A, Papp M, et al. The effect of chronic treatment with lurasidone on rat liver cytochrome P450 expression and activity in the chronic mild stress (CMS) model of depression. Drug Metabolism and Disposition. 2017, 45(12): 1336-1344 3. Danek P J, Wójcikowski J, Daniel W A. The atypical neuroleptics iloperidone and lurasidone inhibit human cytochrome P450 enzymes in vitro. Evaluation of potential metabolic interactions. Pharmacological Reports:PR. 2020, 72(6): 1685-1694

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Anti-Neurodegenerative Disease Compound Library GPCR Compound Library Drug Repurposing Compound Library EMA Approved Drug Library Bioactive Compound Library FDA-Approved & Pharmacopeia Drug Library

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Keywords

Lurasidone hydrochloride 367514-88-3 GPCR/G Protein Neuroscience 5-HT Receptor Norepinephrine Dopamine Receptor Lurasidone HCl Inhibitor 5-hydroxytryptamine Receptor SM-13496 (Hydrochloride) Lurasidone Lurasidone Hydrochloride SM 13496 inhibit SM-13496 Serotonin Receptor SM13496 inhibitor

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