ChemicalBook CAS数据库列表 3-(2,5-二氟苯基)-7-(1,1-二甲基乙基)-6-[(1-甲基-1H-1,2,4-,三唑-5-基)甲氧基]-1,2,4-4-三唑[4,3-B]哒嗪
3-(2,5-二氟苯基)-7-(1,1-二甲基乙基)-6-[(1-甲基-1H-1,2,4-,三唑-5-基)甲氧基]-1,2,4-4-三唑[4,3-B]哒嗪
![3-(2,5-二氟苯基)-7-(1,1-二甲基乙基)-6-[(1-甲基-1H-1,2,4-,三唑-5-基)甲氧基]-1,2,4-4-三唑[4,3-B]哒嗪,286456-42-6,结构式](https://www.chemicalbook.com/CAS/GIF/286456-42-6.gif)
- CAS号:286456-42-6
- 英文名:L-838417
- 中文名:3-(2,5-二氟苯基)-7-(1,1-二甲基乙基)-6-[(1-甲基-1H-1,2,4-,三唑-5-基)甲氧基]-1,2,4-4-三唑[4,3-B]哒嗪
- CBNumber:CB8506755
- 分子式:C19H19F2N7O
- 分子量:399.4
- MOL File:286456-42-6.mol
3-(2,5-二氟苯基)-7-(1,1-二甲基乙基)-6-[(1-甲基-1H-1,2,4-,三唑-5-基)甲氧基]-1,2,4-4-三唑[4,3-B]哒嗪化学性质
- 熔点 :196-198°C
- 密度 :1.40±0.1 g/cm3(Predicted)
- 储存条件 :Store at +4°C
- 溶解度 :DMSO: ≥20mg/mL
- 酸度系数(pKa) :2.13±0.10(Predicted)
- 形态 :powder
- 颜色 :white to off-white
安全信息
- WGK Germany :3
3-(2,5-二氟苯基)-7-(1,1-二甲基乙基)-6-[(1-甲基-1H-1,2,4-,三唑-5-基)甲氧基]-1,2,4-4-三唑[4,3-B]哒嗪性质、用途与生产工艺
- 生物活性 L-838417 是GABAA 受体 α2, α3 和 α5 亚型的选择性部分激动剂，是 α1 亚型的拮抗剂，其对 α1β3γ2、α2β3γ2、α3β3γ2、α4β3γ2、α5β3γ2 和 α6β3γ2 的Ki 值分别为 0.79 nM、0.67 nM、1.67 nM、267 nM、2.25 nM 和 2183 nM。
-
靶点
Ki: 0.79 nM (α1β3γ2), 0.67 nM (α2β3γ2), 1.67 nM (α3β3γ2), 267 nM (α4β3γ2), 2.25 nM (α5β3γ2) and 2183 nM (α6β3γ2).
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体内研究
L-838417 (1.0 mg/kg) produces anxiolytic effects in adult rat, as indexed by a transformation of social avoidance into preference and an increase in social investigation.
L-838417 (2.0 mg/kg) eliminates social avoidance, but has no anxiolytic effects on social investigation.
L-838417 (0.5 mg/kg) reverses the anxiogenic effects of prior stress regardless of age, but with doses ≥ 1 mg/kg decreases social investigation, an effect possibly due in part to locomotor-impairing effects of this compound.
Animal Model: Male and female adolescent and adult Sprague–Dawley rats. Dosage: 0, 0.5, 1.0, 2.0, or 4.0 mg/kg. Administration: IP. Result: Adolescents required a higher dose (2 mg/kg) to attenuate their social avoidance.
The lowest dose of 0.5 mg/kg was sufficient to reverse the anxiogenic effects of repeated restraint as reflected by a significant increase in the coefficient relative to vehicle-treated animals.
3-(2,5-二氟苯基)-7-(1,1-二甲基乙基)-6-[(1-甲基-1H-1,2,4-,三唑-5-基)甲氧基]-1,2,4-4-三唑[4,3-B]哒嗪上下游产品信息
上游原料
下游产品
3-(2,5-二氟苯基)-7-(1,1-二甲基乙基)-6-[(1-甲基-1H-1,2,4-,三唑-5-基)甲氧基]-1,2,4-4-三唑[4,3-B]哒嗪生产厂家
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- 国家：英国
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286456-42-6, 3-(2,5-二氟苯基)-7-(1,1-二甲基乙基)-6-[(1-甲基-1H-1,2,4-,三唑-5-基)甲氧基]-1,2,4-4-三唑[4,3-B]哒嗪相关搜索:
