TCN 201

更新时间：2024-01-08 21:55:29

TCN 201结构式	常用名	TCN 201	英文名	TCN 201
	CAS号	852918-02-6	分子量	461.894
	密度	1.4±0.1 g/cm3	沸点	N/A
	分子式	C₂₁H₁₇ClFN₃O₄S	熔点	N/A
	MSDS	美版	闪点	N/A
	符号	GHS07	信号词	Warning

TCN 201用途

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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。

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	N-[[4-(benzamidocarbamoyl)phenyl]methyl]-3-chloro-4-fluorobenzenesulfonamide
英文别名	更多

描述	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。
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.

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

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

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...

Benzoic acid, 4-[[[(3-chloro-4-fluorophenyl)sulfonyl]amino]methyl]-, 2-benzoylhydrazide

tcn 201

qcr-22

N-{4-[(2-Benzoylhydrazino)carbonyl]benzyl}-3-chloro-4-fluorobenzenesulfonamide