中文名: | PNU 120596;1-(5-氯-2,4-二甲氧基苯基)-3-(5-甲基异恶唑-3-基)脲 |
中文别名: | N-(5-氯-2,4-二甲氧基苯基)-N‘-(5-甲基-3-异噁唑基)脲;PNU 120596; PNU120596; NSC 216666;PNU 120596; PNU120596; NSC 216666 |
英文名称: | PNU-120596 |
英文别名: | N-(5-Chloro-2,4-dimethoxyphenyl)-N′-(5-methyl-3-isoxazolyl)-urea |
CAS No.: | 501925-31-1 |
分子式: | C13H14ClN3O4 |
分子量: | 311.72 |
性状: | 属性溶解性Soluble in DMSO (62 mg/ml), methanol (1 mg/ml), acetonitrile (0.5 mg/ml), ethanol (1 mg/ml), and water (<1 mg/ml).存贮条件储存温度-20°C描述产品介绍PNU-120596是一种有效的α7 nAChR变构调节剂,EC50为216 nM。用途A type II positive allosteric modulator.生化机理PNU 120596 is a type II positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptor (AChR) located on the somatodendritic membrane of hippocampal interneurons. This modulator increases the frequency of acetylcholine-evoked GABAergic postsynaptic currents in pyramidal neurons, which can be suppressed by TTX. In addition, studies show that PNU 120596 increases the average time the channel of AChR is open, but does not have any effect on the selectivity of ions flowing through the channel. Furthermore, PNU 120596 has little effect on α4β2, α3β4 and α9α10 receptors. Alternate studies indicate that PNU 120596 increases the effects of choline on native α7-containing AChRs activating these receptors, thus producing single ion channel openings which result in an influx of calcium ions, that can be inhibited with the addition of methyllycaconitine |
储存: | 储存温度-20°C |
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用途: | A type II positive allosteric modulator. |