产品描述: | L-701324 is a potent, orally active NMDA receptor antagonist that antagonizes the activity of the NMDA receptor by blocking its glycine B binding site. L-701324 binds with high affinity to rat brain membranes (IC50=2 nM). L-701324 has antidepressant activity |
靶点: |
iGluR;NMDAR; iGluR |
体内研究: |
L-701324 (5-10 mg/kg; i.p.; once) exhibits antidepressant-like potential in the forced swim test (FST) and tail suspension test (TST) without affecting the locomotor activity of mice. L-701324 (5-10 mg/kg; i.p.; daily, for 2 weeks) produces strong antidepressant-like effects in the chronic unpredictable mild stress (CUMS) model of depression and prevents the CUMS-induced decreases in eurogenesis and the BDNF signaling cascade in the hippocampus. L-701324 (2.5-5 mg/kg; p.o.; once) inhibits NMDA receptor activity via a blockade of the NMDA/glycine-sensitive site at the NMDA receptor is accompanied by a reduction of anxiety-like behavior in both non-conditioned and conditioned conflict behavior situations |
参考文献: |
1. Liu L, et, al. Antidepressant-like activity of L-701324 in mice: A behavioral and neurobiological characterization. Behav Brain Res. 2021 Feb 5;399:113038. 2. Kotlinska J, et, al. A characterization of anxiolytic-like actions induced by the novel NMDA/glycine site antagonist, L-701,324. Psychopharmacology (Berl). 1998 Jan;135(2):175-81. 3. Hutson PH, et, al. L-701,324, a glycine/NMDA receptor antagonist, blocks the increase of cortical dopamine metabolism by stress and DMCM. Eur J Pharmacol. 1997 May 20;326(2-3):127-32. |
溶解性: |
DMSO : ≥ 34 mg/mL (93.46 mM) |
保存条件: |
2-8℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.749 ml |
13.744 ml |
27.488 ml |
5 mM |
0.55 ml |
2.749 ml |
5.498 ml |
10 mM |
0.275 ml |
1.374 ml |
2.749 ml |
50 mM |
0.055 ml |
0.275 ml |
0.55 ml |
|
注意: |
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