1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Bemesetron

Bemesetron (Synonyms: MDL 72222)

Cat. No.: HY-B1541 Purity: >99.0%
Handling Instructions

Bemesetron (MDL 72222) is a selective 5-HT3 receptor antagonist with an IC50 of 0.33 nM. Neuroprotective effect.

For research use only. We do not sell to patients.

Bemesetron Chemical Structure

Bemesetron Chemical Structure

CAS No. : 40796-97-2

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Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Bemesetron (MDL 72222) is a selective 5-HT3 receptor antagonist with an IC50 of 0.33 nM[1]. Neuroprotective effect[2].

IC50 & Target[1]

5-HT3 Receptor

0.33 nM (IC50)

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[2].
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[2].
Bemesetron (1 μM, 15 hours) significantly blocks the H2O2-induced increase of caspase-3 immunoreactivity[2].

Cell Viability Assay[2]

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[2]

Cell Line: Primary cortical neuronal cells
Concentration: 1 μM
Incubation Time: 15 hours
Result: Blocked significantly the H2O2-induced increase of caspase-3 immunoreactivity.
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[3].

Animal Model: Male adult albino mice, weighing 26-36 g[3]
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.
Molecular Weight







O=C(O[[email protected]@H]1C[[email protected]@H](N2C)CC[[email protected]@H]2C1)C3=CC(Cl)=CC(Cl)=C3


Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (6.37 mM; Need ultrasonic)

Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1826 mL 15.9129 mL 31.8258 mL
5 mM 0.6365 mL 3.1826 mL 6.3652 mL
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.

Purity: >99.0%

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BemesetronMDL 72222MDL72222MDL-722225-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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