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CAS No.: 501684-93-1

NS 1738 Catalog No. CSN23663

Synonyms: NSC 213859

NS 1738 is an allosteric modulator of α7 nicotinic acetylcholine receptor with cognitive-enhancing properties in vivo.

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技术信息

生物活性

描述NS 1738 is a novel positive allosteric modulator of the α7 nAChR, with respect to positive modulation of α7 nAChR (EC50 = 3.4 μM in oocyte experiments). NS 1738 acts by increasing the peak amplitude of acetylcholine (ACh)-evoked currents at all concentrations; thus, it increased the maximal efficacy of ACh. Under similar experimental conditions, NS 1738 shows comparable efficacy and potency at the rat α7 nAChR (EC50 = 3.9 μM). Moreover, NS1738 improved performance in the rat social recognition test to the same extent as (-)-nicotine, demonstrating that NS1738 is capable of producing cognitive enhancement in vivo^[1]. NS-1738 could bind to three allosteric sites of α7-AChBP, namely, the top pocket, the vestibule pocket and the agonist sub-pocket. NS-1738 has moderate binding affinities (-6.76 to -9.15 kcal/mol) at each allosteric site^[2]. The increase of the NMDA-evoked (N-methyl-D-aspartate-evoked) firing rate exerted by NS-1738 was superadditive over the sum of the single effects of NMDA and NS-1738. However, NS-1738 counteracted inhibitory effects of PHA-543613 in 5 out of 6 neurons, resulting in a synergistic potentiation of their firing responses to NMDA^[3].
参考文献

[1] Timmermann DB, Grønlien JH, Kohlhaas KL, et al. An allosteric modulator of the alpha7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo [published correction appears in J Pharmacol Exp Ther. 2009 Dec;331(3):1146. Chrsitensen, Jeppe K [corrected to Christensen, Jeppe K]]. J Pharmacol Exp Ther. 2007;323(1):294-307
[2] Kuang G, Wang X, Halldin C, et al. Theoretical study of the binding profile of an allosteric modulator NS-1738 with a chimera structure of the α7 nicotinic acetylcholine receptor. Phys Chem Chem Phys. 2016;18(40):28003-28009
[3] Bali ZK, Nagy LV, Budai D, Hernádi I. Facilitation and inhibition of firing activity and N-methyl-D-aspartate-evoked responses of CA1 hippocampal pyramidal cells by alpha7 nicotinic acetylcholine receptor selective compounds in vivo. Sci Rep. 2019;9(1):9324. Published 2019 Jun 27

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
- 2.7388 mL
- 13.6938 mL
- 27.3875 mL
- 5 mM
- 0.5478 mL
- 2.7388 mL
- 5.4775 mL
- 10 mM
- 0.2739 mL
- 1.3694 mL
- 2.7388 mL

技术信息

CAS号

501684-93-1

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H9Cl2F3N2O2

运输

蓝冰

分子量

365.13

别名

NSC 213859

溶解度

DMSO	510.0 mg/mL (1396.7 mM)
Water	insoluble

动物实验配方

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