Bemesetron

SKU: orb1940730

Description

Bemesetron is a selective antagonist of 5-HT3 (IC50 = 0.33 nM) with neuroprotective effects.(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.(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.

Key Properties

• CAS Number: 40796-97-2
• MW: 314.21
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₇Cl₂NO₂
• SMILES: CN1[C@H]2CC[C@@H]1C[C@@H](C2)OC(=O)c1cc(Cl)cc(Cl)c1
• Target: 5-HT Receptor
• Solubility: In Vitro: DMSO : 2 mg/mL (6.37 mM)

Bioactivity

• In Vivo:
  Bemesetron (0.1, 1 and 10 mg/kg; i.p.) is used in male adult albino mice. The lowest dose do not cause any significant change in catalepsy. However, Bemesetron (1 mg/kg) causes a significant reduction of catalepsy (from 90 min after Haloperidol), while 10 mg/kg significantly potentiates the phenomenon (from 60 min after Haloperidol). 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. Animal model: Male adult albino mice, weighing 26-36 g. Dosage: 0.1-10 mg/kg. Administration: Intraperitoneally injected, 20 min (pretreatment) +180 min (treatment). Result: Reduced catalepsy significantly at a dose of 1 mg/kg, whilst 10 mg/kg potentiated the phenomenon and 0.1 mg/kg was found to be without effect.
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• In Vitro:
  Blockade of 5-HT3 receptor with Bemesetron (MDL7222) reduces hydrogen peroxide-induced neurotoxicity in cultured rat cortical cells. Bemesetron (0.01, 0.1 and 1 μM, 15 hours) and Y25130 (0.05, 0.5 and 5 μM) concentration-dependently reduce the H2O2-induced decrease of MTT reduction showing 74.9±2.4 and 79.0 ±2.5% with 1 μM and 5 μM, respectively, which are maximal effects. Pretreatment (20 minutes) with Bemesetron (1 μM), Y25130 (5 μM) or MK-801 (10 μM) significantly, but not completely, inhibits the H2O2-induced elevation of [Ca2+]c. Bemesetron (1 μM, 15 hours) significantly blocks the H2O2-induced increase of caspase-3 immunoreactivity. Cell Viability Assay Cell line: Primary cortical neuronal cells. Concentration: 0.01-1 μM Incubation time: 20 minutes (pretreatment); 15 hours (post-incubation). Result: Concentration-dependently reduced the H2O2-induced decrease of MTT reduction showing 74.9±2.4% with 1 μM, which was maximal effect. Western blot analysis. Cell line: Primary cortical neuronal cells. Concentration: 1 μM. Incubation time: 15 hours. Result: Blocked significantly the H2O2-induced increase of caspase-3 immunoreactivity.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MDL 72222 | 3-TROPANYL-3,5-DICHLOROBENZOATE | TROPANYL 3,5-DICHLOROBENZOATE

Quick Database Links

Gene Symbol

5-HT Receptor