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Ifenprodil tartrate

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Chemical Structure| 23210-58-4 同义名 : Ifenprodil (hemitartrate);NP-120
CAS号 : 23210-58-4
货号 : A114148
分子式 : C46H60N2O10
纯度 : 98%
分子量 : 800.976
MDL号 : N/A
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 300 mg/mL(374.54 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 5 mg/mL(6.24 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • NMDA receptor

    NMDA Receptor, IC50:0.3 μM
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 ... 展开 >> 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 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.25mL

0.25mL

0.12mL

6.24mL

1.25mL

0.62mL

12.48mL

2.50mL

1.25mL
参考文献

[1]Kew JN, Richards JG, et al. Developmental changes in NMDA receptor glycine affinity and ifenprodil sensitivity reveal three distinct populations of NMDA receptors in individual rat cortical neurons. J Neurosci. 1998 Mar 15;18(6):1935-43.

[2]Williams K. Ifenprodil discriminates subtypes of the N-methyl-D-aspartate receptor: selectivity and mechanisms at recombinant heteromeric receptors. Mol Pharmacol. 1993 Oct;44(4):851-9.

[3]Williams K. Ifenprodil discriminates subtypes of the N-methyl-D-aspartate receptor: selectivity and mechanisms at recombinant heteromeric receptors. Mol Pharmacol. 1993 Oct;44(4):851-9

[4]Amico-Ruvio SA, Paganelli MA, Myers JM, Popescu GK. Ifenprodil effects on GluN2B-containing glutamate receptors. Mol Pharmacol. 2012 Dec;82(6):1074-81

[5]Yao Y, Ju P, Liu H, Wu X, Niu Z, Zhu Y, Zhang C, Fang Y. Ifenprodil rapidly ameliorates depressive-like behaviors, activates mTOR signaling and modulates proinflammatory cytokines in the hippocampus of CUMS rats. Psychopharmacology (Berl). 2020 May;237(5):1421-1433

[6]Delaney AJ, Power JM, Sah P. Ifenprodil reduces excitatory synaptic transmission by blocking presynaptic P/Q type calcium channels. J Neurophysiol. 2012 Mar;107(6):1571-5