1. Neuronal Signaling
  2. Serotonin Transporter Dopamine Transporter
  3. D-473

D-473 是一种口服有效、具有血脑屏障穿透能力的再摄取抑制剂,且偏好血清素。D-473 可抑制血清素、多巴胺和去甲肾上腺素转运体,显著提升大鼠脑区内这三种神经递质的细胞外水平。D-473 具有明确的类抗抑郁活性,不引发运动激活。D-473 被广泛用于重性抑郁症的相关研究。

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D-473

D-473 Chemical Structure

CAS No. : 1632000-05-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

D-473 is an orally active, blood-brain barrier penetrant and serotonin-preferring reuptake inhibitor. D-473 inhibits serotonin, dopamine and norepinephrine transporters, and significantly elevates the extracellular levels of these three neurotransmitters in rat brain regions. D-473 exhibits definite antidepressant-like activity without inducing motor activation. D-473 is widely used in studies related to major depressive disorder[1].

体外研究
(In Vitro)

D-473 抑制表达克隆人 hDAT、hSERT 和 hNET 的 HEK 293 细胞中的单胺摄取,对 hSERT 的效力最高 (Ki=9.18 nM),其次是 hNET (Ki=39.7 nM) 和 hDAT (Ki=70.4 nM)[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

D-473 (5-50 mg/kg;口服;单次给药;5 分钟游泳试验前 1 小时) 在大鼠强迫游泳试验中可剂量依赖性地显著缩短不动时间[1]
D-473 (25 mg/kg;口服;单次给药) 对大鼠的自发活动无显著影响[1]
D-473 (10 mg/kg;腹腔注射;单次给药) 可显著升高大鼠内侧前额叶皮层 (mPFC) 和背外侧纹状体 (DLS) 中的细胞外多巴胺、5-羟色胺和去甲肾上腺素水平,同时降低上述脑区中多巴胺代谢物的水平[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley rat with major depressive disorder (male, 200-225 g)[1]
Dosage: 5 mg/kg; 10 mg/kg; 25 mg/kg; 50 mg/kg
Administration: p.o.; single dose; 1 hour prior to 5-minute swim test
Result: Produced no significant reduction in immobility time at 5 mg/kg.
Reduced immobility time significantly compared to vehicle at 10 mg/kg.
Reduced immobility time significantly compared to vehicle at 25 mg/kg.
Reduced immobility time significantly compared to vehicle at 50 mg/kg.
分子量

439.49

Formula

C26H27F2NO3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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