40796-97-2
40796-97-2 结构式
基本信息
3-托烷-3,5-二氯苯甲酸
MLD-72222
bemesetron
Benesetron
Bemesetron (MDL 72222)
tropyl3,5-dichlorobenzoate
MNJNPLVXBISNSX-WDNDVIMCSA-N
tropine 3,5-dichlorobenzoate
TROPANYL 3,5-DICHLOROBENZOATE
3-TROPANYL-3,5-DICHLOROBENZOATE
物理化学性质
常见问题列表
|
5-HT 3 Receptor 0.33 nM (IC 50 ) |
Blockade of 5-HT
3
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 H
2
O
2
-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 H
2
O
2
-induced elevation of [Ca
2+
]
c
.
Bemesetron (1 μM, 15 hours) significantly blocks the H
2
O
2
-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 H 2 O 2 -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 H 2 O 2 -induced increase of caspase-3 immunoreactivity. |
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. |