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CAS No.: 23210-58-4

酒石酸艾芬地尔 Catalog No. CSN11186

Synonyms: Ifenprodil (hemitartrate);NP-120;Ifenprodil Hemitartrate

Ifenprodil Tartrate is a high affinity and atypical noncompetitive NMDA receptor antagonist with IC50 of 0.3 μM.

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生物活性

描述Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM). The rate of onset of inhibition by low concentrations of ifenprodil acting at NR1A/NR2B receptors was considerably slower than the onset of inhibition seen with high concentrations of ifenprodil acting at NR1A/NR2A receptors. The degree of inhibition seen with 100 microM ifenprodil at NR1A/NR2A receptors was not altered by changes in the concentration of extracellular glycine. However, the inhibitory effect of 1 microM ifenprodil at NR1A/NR2B receptors was reduced by increasing the concentration of glycine^[3]. Moreover, ifenprodil decreased NMDA receptor equilibrium open probability by raising an energetic barrier to activation and also by biasing the receptor toward low open probability gating modes^[4]. A single injection of ifenprodil (3 mg/kg, intraperitoneally (i.p.)) was sufficient to provoke rapid antidepressant-like effects in chronic unpredictable mild stress (CUMS) rats. Moreover, ifenprodil activated mTOR signaling and reversed the CUMS-induced elevation of interleukin-1β (IL-1β), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α) in the hippocampus after acute administration^[5]. In the basolateral amygdala, ifenprodil dose dependently blocks excitatory transmission to principal neurons by a presynaptic mechanism. Ifenprodil reduces synaptic transmission in the basolateral amygdala by partially blocking P-type voltage-dependent calcium channels^[6].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01896388	Posttraumatic Stress Disorders	Phase 1 Phase 2	Recruiting	-	Japan ... more >> Department of Psychiatry, Chiba University School of Medicine Chiba, Chuo-ku, Japan 260-8670 Recruiting Chiba, Chuo-ku, Japan, 260-8670 Contact: Tsuyoshi Sasaki, MD +81-43-222-7171 sasaki@faculty.chiba-u.jp Contact: Kenji Hashimoto, PhD +81-43-222-7171 hashimoto@faculty.chiba-u.jp Principal Investigator: Masaomi Iyo, MD,PhD Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.2485 mL
- 6.2424 mL
- 12.4848 mL
- 5 mM
- 0.2497 mL
- 1.2485 mL
- 2.4970 mL
- 10 mM
- 0.1248 mL
- 0.6242 mL
- 1.2485 mL

技术信息

CAS号

23210-58-4

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C46H60N2O10

运输

蓝冰

分子量

800.98

别名

Ifenprodil (hemitartrate);NP-120;Ifenprodil Hemitartrate;Ifenprodil;RC 61-91;酒石酸艾芬地尔;艾芬地尔酒石酸盐

溶解度

DMSO	300.0 mg/mL (374.5 mM)
Water	insoluble

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