UBP 302

UBP 302用途

UBP 302,S 对映异构体,是一种有效且选择性的 GluK1 (GluR5)-subunit containing kainate receptor 拮抗剂 (表观 Kd=402 nM),对 GluK2 (GluR6) kainate receptors 亲和力很小。具有抗焦虑作用。

UBP 302名称

[ CAS 号 ]:
745055-91-8

[ 英文名 ]:
UBP 302

[英文别名 ]:

Tocris-2079
UBC
UBP-302
2f35

UBP 302生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> iGluR

信号通路 >> 跨膜转运 >> iGluR

[ 靶点 ]

Apparent Kd: 402 nM (GluK1)[2] IC50: 106 μM (AMPA receptors)[2]

[参考文献]

[1]. More JC, et al. Characterisation of UBP296: a novel, potent and selective kainate receptor antagonist. Neuropharmacology. 2004 Jul;47(1):46-64.

[2]. Dolman NP, et al. Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. J Med Chem. 2005 Dec 1;48(24):7867-81.

[3]. Apland JP, et al. The limitations of diazepam as a treatment for nerve agent-induced seizures and neuropathology in rats: comparison with UBP302. J Pharmacol Exp Ther. 2014 Nov;351(2):359-72.

UBP 302物理化学性质

[ 分子式 ]:
C₁₅H₁₅N₃O₆

[ 分子量 ]:
333.29600

[ 精确质量 ]:
333.09600

[ PSA ]:
144.62000

[ 储存条件 ]:
-20°C，密闭，干燥

UBP 302MSDS

详细MSDS(安全技术说明书)

UBP 302安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

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

UBP 302文献

The limitations of diazepam as a treatment for nerve agent-induced seizures and neuropathology in rats: comparison with UBP302.

J. Pharmacol. Exp. Ther. 351(2) , 359-72, (2014)

Exposure to nerve agents induces prolonged status epilepticus (SE), causing brain damage or death. Diazepam (DZP) is the current US Food and Drug Administration-approved drug for the cessation of nerv...

High-Throughput Screen of GluK1 Receptor Identifies Selective Inhibitors with a Variety of Kinetic Profiles Using Fluorescence and Electrophysiology Assays.

J. Biomol. Screen. 20 , 708-19, (2015)

GluK1, a kainate subtype of ionotropic glutamate receptors, exhibits an expression pattern in the CNS consistent with involvement in pain processing and migraine. Antagonists of GluK1 have been shown ...

A rat model of nerve agent exposure applicable to the pediatric population: The anticonvulsant efficacies of atropine and GluK1 antagonists.

Toxicol. Appl. Pharmacol. 284 , 204-16, (2015)

Inhibition of acetylcholinesterase (AChE) after nerve agent exposure induces status epilepticus (SE), which causes brain damage or death. The development of countermeasures appropriate for the pediatr...

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