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CX546

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Chemical Structure| 215923-54-9 同义名 : -
CAS号 : 215923-54-9
货号 : A118774
分子式 : C14H17NO3
纯度 : 99%+
分子量 : 247.29
MDL号 : MFCD01860868
存储条件:

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(424.6 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 2 mg/mL(8.09 mM),配合低频超声助溶

无水乙醇: 100 mg/mL(404.38 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

动物实验配方:
生物活性
描述 CX546 is a selective positive AMPAR modulator; the prototypical ampakine agent. Intraperitoneal injections of CX546 increased hippocampal BDNF (brain-derived neurotrophic factor) mRNA levels in aged rats and middle-aged mice[3]. Administration of the positive modulator of alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid receptors (AMPAR), CX546, during the conditioning phase only, improved the disrupted LI in mGluR5 knockout mice and facilitated LI in control C57BL/6J mice, given extended number of conditioning trails. PPI (Prepulse inhibition) deficit of mGluR5(-/-) mice was effectively reversed by CX546, whereas aniracetam had a less pronounced effect[4]. In binding tests, CX546 caused an approximately 2-fold increase in the affinity for radiolabeled agonists, whereas CX516 was ineffective[5]. CX546 reduced the degree of desensitization more potently than CX516 or IDRA 21, but not as efficiently as cyclothiazide. CX546 increased agonist affinity threefold on nondesensitizing AMPA receptors by slowing agonist unbinding. In the presence of CX546, the current induced by short pulses of glutamate from recombinant GluR2 receptors decayed with a time course that was approximately twentyfold faster than EPSCs[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.04mL

0.81mL

0.40mL

20.22mL

4.04mL

2.02mL

40.44mL

8.09mL

4.04mL

参考文献

[1]Lipina T, Weiss K, et al. The ampakine CX546 restores the prepulse inhibition and latent inhibition deficits in mGluR5-deficient mice. Neuropsychopharmacology. 2007 Apr;32(4):745-56.

[2]Nagarajan N, Quast C, et al. Mechanism and impact of allosteric AMPA receptor modulation by the ampakine CX546. Neuropharmacology. 2001 Nov;41(6):650-63.

[3]Lauterborn JC, Lynch G, Vanderklish P, Arai A, Gall CM. Positive modulation of AMPA receptors increases neurotrophin expression by hippocampal and cortical neurons. J Neurosci. 2000;20(1):8-21

[4]Lipina T, Weiss K, Roder J. The ampakine CX546 restores the prepulse inhibition and latent inhibition deficits in mGluR5-deficient mice. Neuropsychopharmacology.2007;32(4):745-756

[5]Arai AC, Xia YF, Rogers G, Lynch G, Kessler M. Benzamide-type AMPA receptor modulators form two subfamilies with distinct modes of action. J Pharmacol Exp Ther. 2002;303(3):1075-1085

[6]Nagarajan N, Quast C, Boxall AR, Shahid M, Rosenmund C. Mechanism and impact of allosteric AMPA receptor modulation by the ampakine CX546. Neuropharmacology.2001;41(6):650-663