L-701324 是一种口服有效的 NMDA 受体拮抗剂，通

L-701324

L-701324 是一种口服有效的 NMDA 受体拮抗剂，通过阻断其甘氨酸 B 结合位点来拮抗 NMDA 受体的活性。L-701324 与大鼠脑膜具有高亲和力 (IC₅₀=2 nM)。L-701324 具有抗抑郁活性。

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生物活性    
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[1][2][3].

体内研究
(In Vivo)    
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[1].
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[1].
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[2].


Animal Model:    Male C57BL/6 J mice in the chronic unpredictable mild stress (CUMS) (7 weeks of age) [1]
Dosage:    5 and 10 mg/kg
Administration:    Intraperitoneal injection; daily, for 2 weeks
Result:    Reduced the immobility of C57BL/6 J mice.
Increased the expression of BDNF, pTrkB and pCREB in the hippocampus.

分子量    
363.79

性状    
Solid

Formula    
C21H14ClNO3

CAS 号    
142326-59-8

运输条件    
Room temperature in continental US; may vary elsewhere.

储存方式    
Powder    -20°C    3 years
4°C    2 years
In solvent    -80°C    6 months
-20°C    1 month
溶解性数据    
In Vitro: 
DMSO : ≥ 34 mg/mL (93.46 mM)

* "≥" means soluble, but saturation unknown.

配制储备液    
浓度溶剂体积质量    1 mg    5 mg    10 mg
1 mM    2.7488 mL    13.7442 mL    27.4884 mL
5 mM    0.5498 mL    2.7488 mL    5.4977 mL
10 mM    0.2749 mL    1.3744 mL    2.7488 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
 

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.  [Content Brief] [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.  [Content Brief] [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.  [Content Brief]