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CAS No.: 501925-31-1

PNU-120596 Catalog No. CSN11494

Synonyms: NSC 216666

PNU-120596 is a a type II positive allosteric modulator of α7 nAChRs with an EC50 of 0.2 μM.

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技术信息

生物活性

描述PNU-120596 (NSC 216666 ) is a potent and selective positive allosteric α7 nAChR modulator with an EC50 of 0.2 μM. PNU-120596 increased agonist-evoked calcium flux mediated by an engineered variant of the human alpha7 nAChR. PNU-120596 increased peak agonist-evoked currents mediated by wild-type receptors and also demonstrated a pronounced prolongation of the evoked response in the continued presence of agonist. PNU-120596 increased the channel mean open time of alpha7 nAChRs but had no effect on ion selectivity and relatively little, if any, effect on unitary conductance. When applied to acute hippocampal slices, PNU-120596 increased the frequency of ACh-evoked GABAergic postsynaptic currents measured in pyramidal neurons^[3]. PNU-120596 enhanced voltage-dependent inhibition of α(7) responses by bicuculline and choline. In the presence of PNU-120596, α(7) channels favored a burst-like kinetic modality in the presence, but not absence of bicuculline and bursts of α(7) openings were voltage-dependent^[4]. The PNU 120596 (1 or 4 mg/kg, i.p.) dose-dependently prevented LPS-induced (lipopolysaccharide) depressive-like behavior during FST, TST, FST (forced swim test), TST (tail suspension test) and sucrose preference test. Similarly, the PNU 120596 (4 mg/kg, i.p.) significantly reduced LPS-induced increased expression of Iba-1 in the hippocampus or prefrontal cortex^[5].
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
- 3.2080 mL
- 16.0400 mL
- 32.0800 mL
- 5 mM
- 0.6416 mL
- 3.2080 mL
- 6.4160 mL
- 10 mM
- 0.3208 mL
- 1.6040 mL
- 3.2080 mL

技术信息

CAS号

501925-31-1

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H14ClN3O4

运输

蓝冰

分子量

311.72

别名

NSC 216666

溶解度

DMSO	200.0 mg/mL (641.6 mM)
Water	insoluble

动物实验配方

1% DMSO+30% polyethylene glycol+1% Tween 80+water

10 mg/mL

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