Lurasidone hydrochloride

SKU: orb1307576

Description

Lurasidone HCl is an atypical antipsychotic and thiazole derivative with a multi-receptor profile, acting as an antagonist at dopamine D2, serotonin 5-HT2/5-HT7, and adrenergic α2 receptors, and a partial agonist at 5-HT1A receptors. It is widely used in preclinical research for studying schizophrenia and bipolar disorder mechanisms, employing both in vitro binding assays and in vivo behavioral models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 367514-88-3
• MW: 529.14
• Purity: >99.99% (May vary between batches)
• Formula: C₂₈H₃₆N₄O₂S·HCl
• SMILES: Cl.O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1C[C@@H]1CCCC[C@H]1CN1CCN(CC1)c1nsc2ccccc12
• Target: Norepinephrine,Dopamine Receptor,5-HT Receptor
• Solubility: DMSO:5.3 mg/mL (10.02 mM)

Bioactivity

• Target IC50:
  5-HT1A:6.75 nM|D2 receptor:1.68 nM|Noradrenaline α2C:10.8 nM|5-HT7:0.495 nM|5-HT2A:2.03 nM
• 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. Lurasidone (30 mg/kg, p.o.) significantly and dose-dependently reverses the MK-801-induced impairment of the passive-avoidance response of rats. 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. 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SM 13496, SM13496, SM-13496 (Hydrochloride), SM-13496 Hydrochloride, Norepinephrine α2C, Lurasidone, Lurasidone HCl, D2, DopamineReceptor, Dopamine, Dopamine Receptor, 5-HT2A, 5-HT Receptor, 5-HT1A, 5HT Receptor, 5HTReceptor, 5-HT7

Compound Identifiers

PubChem CID

11237860