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TCN 201

TCN 201用途

TCN 201 是一种有效的,选择性和非竞争性的 GluN1/GluN2A NMDAR 拮抗剂。 TCN 201的拮抗作用取决于 GluN1 激动剂的浓度。TCN201 可以对含有天然 GluN2A 的 NMDAR 群体进行药理学鉴定。

TCN 201名称

[ CAS 号 ]:
852918-02-6

[ 中文名 ]:
4-[[[(3-氯-4-氟苯基)磺酰基]氨基]甲基]苯甲酸 2-苯甲酰基酰肼

[ 英文名 ]:
TCN 201

[英文别名 ]:

tcn 201
qcr-22

TCN 201生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> iGluR

研究领域 >> 神经疾病

信号通路 >> 跨膜转运 >> iGluR

[ 靶点 ]

NMDAR[1]

[体外研究]

tcn201(10μM)对卵母细胞中GluN1/GluN2B NMDAR介导的电流仅产生轻微的抑制作用[1]。tcn201(10-30μM)对NMDAR介导的反应的拮抗作用是亚型和甘氨酸依赖的,在卵母细胞中比tcn213更有效[1]。tcn201(0.1-100μM)在卵母细胞中不能完全阻断NMDAR介导的反应[1]。tcn201(10μM)对NMDAR介导电流的拮抗作用与其ifenprodil敏感性呈负相关[1]。tcn201(1-9μM)抑制鸡视网膜皮质扩散抑制(CSD)[2]。

[体内研究]

TCN-201(10mg/kg；i.p.)对大鼠CSD-g血氧水平依赖性(BOLD)反应无效[3]。

[参考文献]

[1]. Edman S, et, al. TCN 201 selectively blocks GluN2A-containing NMDARs in a GluN1 co-agonist dependent but non-competitive manner. Neuropharmacology. 2012 Sep; 63(3): 441-9.

[2]. Bu F, et, al. NR2A contributes to genesis and propagation of cortical spreading depression in rats. Sci Rep. 2016 Mar 22;6:23576.

[3]. Shatillo A, et, al. Involvement of NMDA receptor subtypes in cortical spreading depression in rats assessed by fMRI. Neuropharmacology. 2015 Jun; 93:164-70.

TCN 201物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 分子式 ]:
C₂₁H₁₇ClFN₃O₄S

[ 分子量 ]:
461.894

[ 精确质量 ]:
461.061218

[ PSA ]:
116.24000

[ LogP ]:
4.13

[ 折射率 ]:
1.625

[ 储存条件 ]:
2-8°C

TCN 201安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
22-36/37/38

[ 安全声明 (欧洲) ]:
26-36/37/39

[ 危险品运输编码 ]:
NONH for all modes of transport

TCN 201文献

Sensitivity of N-methyl-D-aspartate receptor-mediated excitatory postsynaptic potentials and synaptic plasticity to TCN 201 and TCN 213 in rat hippocampal slices.

J. Pharmacol. Exp. Ther. 352(2) , 267-73, (2014)

Whereas ifenprodil has been used as a selective GluN1/GluN2B (NR1/NR2B, B-type) receptor antagonist to distinguish between GluN2B (NR2B) and GluN2A (NR2A)-containing N-methyl-d-aspartate receptors (NM...

PAR1-activated astrocytes in the nucleus of the solitary tract stimulate adjacent neurons via NMDA receptors.

J. Neurosci. 35(2) , 776-85, (2015)

Severe autonomic dysfunction, including the loss of control of the cardiovascular, respiratory, and gastrointestinal systems, is a common comorbidity of stroke and other bleeding head injuries. Previo...

Extrasynaptic glutamate release through cystine/glutamate antiporter contributes to ischemic damage.

J. Clin. Invest. 124(8) , 3645-55, (2014)

During brain ischemia, an excessive release of glutamate triggers neuronal death through the overactivation of NMDA receptors (NMDARs); however, the underlying pathways that alter glutamate homeostasi...

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