| 产品介绍 |
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。
|
|---|
| 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.
|
|---|
| 体外研究 | |
|---|
| 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.
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Male C57BL/6 J mice in the chronic unpredictable mild stress (CUMS) (7 weeks of age) |
| 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.
|
| Animal Model: |
Male C57BL/6 J mice in the forced swim test (FST) and tail suspension test (TST) (7 weeks of age) |
| Dosage: |
5 and 10 mg/kg |
| Administration: |
Intraperitoneal injection; once |
| Result: |
Reduced the immobility of C57BL/6 J mice in the FST and TST.
|
| Animal Model: |
Male Sprague-Dawley rats (280-300 g) |
| Dosage: |
2.5 and 5 mg/kg |
| Administration: |
Oral administration; once |
| Result: |
Increased in the percentage of time spent in the open arm in a dose-dependent.
Increased punished responding in the Vogel's conflict test in a dose-dependent fashion.
|
|
|---|
| 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.
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Male C57BL/6 J mice in the chronic unpredictable mild stress (CUMS) (7 weeks of age) |
| 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.
|
| Animal Model: |
Male C57BL/6 J mice in the forced swim test (FST) and tail suspension test (TST) (7 weeks of age) |
| Dosage: |
5 and 10 mg/kg |
| Administration: |
Intraperitoneal injection; once |
| Result: |
Reduced the immobility of C57BL/6 J mice in the FST and TST.
|
| Animal Model: |
Male Sprague-Dawley rats (280-300 g) |
| Dosage: |
2.5 and 5 mg/kg |
| Administration: |
Oral administration; once |
| Result: |
Increased in the percentage of time spent in the open arm in a dose-dependent.
Increased punished responding in the Vogel's conflict test in a dose-dependent fashion.
|
|
|---|
| 性状 | Solid |
|---|
| 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。
|
|---|
| 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 |
|
|---|
| 参考文献 |
-
. 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]
. 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]
. 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]
|
|---|
有竞争力的价格
极速物流
技术支持
现货库存
浙公网安备 33010802013016号
