CAS:501684-93-1NS 1738

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

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18817579266

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18817579266

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实验数据

技术信息

CAS号

501684-93-1

储存条件

分子式

C14H9Cl2F3N2O2

运输

蓝冰

分子量

365.13

别名

溶解度

DMSO	510.0 mg/mL (1396.7 mM)
Water	insoluble

动物实验配方

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].