Bemesetron

SKU: orb1308577

Description

Bemesetron (MDL 72222) is a potent and selective 5-HT3 receptor antagonist with an IC50 of 0.33 nM. Its neuroprotective properties have been investigated in research models for conditions like chemotherapy-induced nausea and central nervous system ischemia, supporting its use in both in vitro and in vivo neurological studies.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 40796-97-2
• MW: 314.21
• Purity: 99.77% (May vary between batches)
• Formula: C₁₅H₁₇Cl₂NO₂
• SMILES: CN1[C@@H]2CC[C@@H]1CC(C2)OC(=O)c1cc(Cl)cc(Cl)c1
• Target: 5-HT Receptor
• Solubility: DMSO:2 mg/mL (6.37 mM)

Bioactivity

• Target IC50:
  5-HT3 receptor:0.33 nM
• In Vivo:
  In male adult albino mice, Bemesetron (1 mg/kg; i.p.) causes a significant reduction of catalepsy, while Bemesetron (10 mg/kg; i.p.) significantly potentiates the phenomenon. The maximum inhibition of catalepsy (about 75%) occurs at 120 min, and the maximum potentiation (about 4.5-times the control value) occurs at 60 min after Haloperidol.
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• In Vitro:
  In primary cortical neuronal cells, Bemesetron (1 μM) significantly blocks the H2O2-induced increase of caspase-3 immunoreactivity. Bemesetron (0.01, 0.1 and 1 μM) and Y25130 (0.05, 0.5 and 5 μM) concentration-dependently reduce the H2O2-induced decrease showing inhibition of 74.9 and 79.0% with 1 μM and 5 μM, respectively.
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Storage & Handling

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

Alternative Names

Bemesetron, 3-TROPANYL-3,5-DICHLOROBENZOATE, 5-HT3 Receptor, 5HTReceptor, 5-HT3, 5HT Receptor, MDL 72222, MDL72222, MDL-72222, TROPANYL 3,5-DICHLOROBENZOATE

Compound Identifiers

PubChem CID

6350580