Eltoprazine hydrochloride (DU 28853 hydrochloride) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.IC50 value:Target: 5-HT1A/1B agonist; 5-HT2C antagonistin vitro: The binding of [3H]eltoprazine to whole tissue sections was saturable and revealed an apparent dissociation constant (Kd) of 11 nM. Specific [3H]eltoprazine binding was completely displaced by 5-HT; conversely, unlabelled eltoprazine reduced [3H]5-HT binding to the levels of non-specific binding. Eltoprazine evoked membrane changes that were similar to but much weaker than those induced by 5HT. Both the 5HT- and eltoprazine-evoked membrane hyperpolarizations were largely suppressed in the presence of spiperone.in vivo: eltoprazine is extremely effective in suppressing dyskinesia in experimental models, although this effect was accompanied by a partial worsening of the therapeutic effect of l-dopa. Interestingly, eltoprazine was found to (synergistically) potentiate the antidyskinetic effect of amantadine. The current data indicated that eltoprazine is highly effective in counteracting dyskinesia in preclinical models Rats were chronically treated with mianserin (10 mg/kg i.p.) or eltoprazine (1 mg/kg i.p.) and were tested in the elevated plus-maze test for anxiety. Mianserin and eltoprazine displayed opposite effects in the elevated plus-maze: mianserin induced anxiolytic-like effects, while eltoprazine showed anxiogenic-like ones. Form:Solid IC50& Target:5-HT 1A Receptor 5-HT 1B Receptor 5-HT 2C Receptor
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Eltoprazine hydrochloride
Dangerous GoodsCAS number:98206-09-8 molecular formula:C12H16N2O2
overview
compound introduction
Specs
| Chinese alias | 盐酸依托拉嗪 | ||
| English alias | AM1234 | MFCD00868056 | SCHEMBL177715 | 1-(1,4-benzodioxan-5-yl)-piperazine | PDSP1_000561 | 4-(2,3-dihydro-benzo[1,4]dioxin-5-yl)-piperazine | 4-(2,3-dihydrobenzo[1,4]dioxin-5-yl)piperazine | 4-(2,3-dihydrobenzo[1,4]dioxin-5-yl)-piperazine | Eltoprazinum | ||
| CAS number | 98206-09-8 | molecular formula | C12H16N2O2 |
| molecular weight | 220.27 g/mol | Exact mass | ≥99% |
| PSA | 33.700 Ų | logp | 1.100 |
numbering system
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physicochemical properties
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Safety information
pictogram:
GHS06 , GHS07
Signal word:
Danger
Hazard Statement:
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H301: 吞咽会中毒
Statement of Preventive Measures:
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染:用水充分清洗。 P321: 特殊处理(请参阅此标签上的...)。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P271: 仅在室外或通风良好的地方使用。 P270: 使用本产品时,请勿进食、饮水
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MSDS
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