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CAS No.: 130798-51-5

MDL-29951 Catalog No. CSN13695

Synonyms: MDL-29,951

MDL-29951 is a glycine antagonist of NMDA receptor activation (Ki=0.14 mM, [3H]glycine binding) in vitro and in vivo.

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400-920-2911

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技术信息

生物活性

描述The N-methyl-D-aspartate receptor (NMDAR) is involved in normal physiological and pathological states in the brain^[3]. The NMDA-preferring glutamate receptor subtype possesses, in addition to the recognition site for glutamate, a binding site for glycine. MDL-29951 is a novel glycine antagonist of NMDA receptor activation with a K_i value of 0.14 μM. It is approximately 2000-fold selective for the glycine binding site over the glutamate recognition sites. MDL-29951 completely inhibited the use-dependent binding of [³H]N-[1-(2-thienyl) cyclohexyl]-piperidine and was noncompetitive, glycine-reversible inhibitor of both NMDA-induced biochemical and electrophysiological responses in brain slice preparations^[4]. In addition, MDL-29951 was found to inhibit the human F16Bpase (Fructose-1,6-bisphosphatase; one of the rate limiting enzymes of hepatic gluconeogenesis) with an IC₅₀ of 2.5 μM^[5]. Moreover, MDL-29951 diminished myelination in primary oligodendrocytes isolated from heterozygous mice^[6]. MDL-29951 was potent anticonvulsants after their i.c.v. administration to audiogenic seizure-susceptible DBA/2J mice^[4].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.3101 mL
- 16.5503 mL
- 33.1005 mL
- 5 mM
- 0.6620 mL
- 3.3101 mL
- 6.6201 mL
- 10 mM
- 0.3310 mL
- 1.6550 mL
- 3.3101 mL

技术信息

CAS号

130798-51-5

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H9Cl2NO4

运输

蓝冰

分子量

302.11

别名

MDL-29,951

溶解度

DMSO	50.0 mg/mL (165.5 mM)

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