Itasetron

SKU: orb1703344

Description

Itasetron (U 98079A) is a selective 5-HT3 receptor antagonist. It is utilized in research to investigate age-related memory impairment and chemotherapy-induced emesis in rodent models, supporting studies in neuropharmacology and oncology.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 123258-84-4
• MW: 300.36
• Purity: 99.68% (May vary between batches)
• Formula: C₁₆H₂₀N₄O₂
• SMILES: C(N[C@H]1C[C@@]2(N(C)[C@](C1)(CC2)[H])[H])(=O)N3C=4C(NC3=O)=CC=CC4
• Target: 5-HT Receptor
• Solubility: DMSO:45 mg/mL (149.82 mM)

Bioactivity

• In Vivo:
  Itasetron orally is rapidly absorbed (about 90 min), is highly bioavailable (greater than 90%), and has a long half-life (about 12 h). Itasetron (0.5, 1, 2, 4, and 8 mg; twice daily) in comparison with 8 mg b.i.d. ondansetron. Assessments were made in patients (n = 104) with histologically confirmed cancer (excluding head and neck tumors) and about to receive their first course of moderately emetogenic chemotherapy. Itasetron demonstrated comparable efficacy to ondansetron; no statistically significant between-group differences were observed in the primary (complete response rate) or secondary (nausea and delayed emesis) efficacy criteria. The tolerability of Itasetron was assessed as 'very good' or 'rather good' by 81% of patients and 89% of physicians. In conclusion, Itasetron is effective and well tolerated in patients receiving moderately emetogenic chemotherapy. Oral doses of 1 mg b.i.d. or above will be used in further clinical studies.
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Storage & Handling

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

Alternative Names

DAU 6215CL, DAU6215CL, 5-HT3, 5HT Receptor, 5HTReceptor, Itasetron, UNII-00S0D0OEKR, U-98079A, U 98079A

Compound Identifiers

PubChem CID

6918106