Lurasidone

SKU: orb1306396

Description

Lurasidone (SM-13496) is a small molecule acting as a dopamine D2 and 5-HT7 receptor antagonist, with respective IC50 values of 1.68 nM and 0.495 nM, and as a 5-HT1A receptor partial agonist (IC50=6.75 nM). It is widely used in preclinical research for studying schizophrenia and mood disorders, employing both in vitro binding assays and in vivo behavioral models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 367514-87-2
• MW: 492.68
• Purity: 99.50% (May vary between batches)
• Formula: C₂₈H₃₆N₄O₂S
• SMILES: 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: 5-HT Receptor,Dopamine Receptor
• Solubility: DMSO:17.83 mg/mL (36.19 mM);10% DMSO+90% Corn Oil:1.5 mg/mL (3.04 mM)

Bioactivity

• Target IC50:
  5-HT1A receptor:6.75 nM (IC50)|D2 receptor:1.68 nM (IC50)|5-HT7 receptor:0.495 nM (IC50)
• In Vivo:
  In addition to its principal antagonist activity at dopamine D2 and serotonin 5-HT2A receptors, lurasidone has distinctive 5-HT7 antagonistic activity, and displays partial agonism at 5-HT1A receptors, as well as modest antagonism at noradrenergic α2A and α2C receptors. Lurasidone is devoid of antihistaminic and anticholinergic activities.
• In Vitro:
  Lurasidone is administered once daily within the range of 40-160 mg/day for schizophrenia and 20-120 mg/day for bipolar depression, and its pharmacokinetic profile requires administration with food. In adult healthy subjects and patients, a 40 mg dose results in peak plasma concentrations in 1-3 h, a mean elimination half-life of 18 h (mostly eliminated in the feces), and apparent volume of distribution of 6173 L; it is approximately 99 % bound to serum plasma proteins. Lurasidone's pharmacokinetics are approximately dose proportional in healthy adults and clinical populations within the approved dosing range, and this was also found in a clinical study of children and adolescents. Lurasidone is principally metabolized by cytochrome P450 (CYP) 3A4 with minor metabolites and should not be coadministered with strong CYP3A4 inducers or inhibitors. Lurasidone does not significantly inhibit or induce CYP450 hepatic enzymes.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

5-HT Receptor, 5-HT1A, 5HT Receptor, 5HTReceptor, 5-HT7, 5-hydroxytryptamine Receptor, D2, Dopamine, Dopamine Receptor, DopamineReceptor, inhibit, Lurasidone, Inhibitor, SM13496, SM-13496, SM 13496, Serotonin Receptor

Compound Identifiers

PubChem CID

213046