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PNU-120596

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Chemical Structure| 501925-31-1 同义名 : NSC 216666
CAS号 : 501925-31-1
货号 : A116736
分子式 : C13H14ClN3O4
纯度 : 99+%
分子量 : 311.721
MDL号 : MFCD00095313
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(160.4 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
动物实验配方：

1% DMSO+30% polyethylene glycol+1% Tween 80+water 10 mg/mL

生物活性
靶点

  • nAChR

    α7 nAChR, EC50:216 nM
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.21mL

0.64mL

0.32mL

16.04mL

3.21mL

1.60mL

32.08mL

6.42mL

3.21mL
参考文献

[1]Ng HJ, Whittemore ER, et al. Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators. Proc Natl Acad Sci U S A. 2007 May 8;104(19):8059-64.

[2]Hurst RS, Hajos M, et al. A novel positive allosteric modulator of the alpha7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J Neurosci. 2005 Apr 27;25(17):4396-405.

[3]Hurst RS, Hajós M, Raggenbass M, et al. A novel positive allosteric modulator of the alpha7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J Neurosci. 2005;25(17):4396‐4405

[4]Kalappa BI, Uteshev VV. The dual effect of PNU-120596 on α7 nicotinic acetylcholine receptor channels. Eur J Pharmacol. 2013;718(1-3):226-234

[5]Alzarea S, Rahman S. Effects of alpha-7 nicotinic allosteric modulator PNU 120596 on depressive-like behavior after lipopolysaccharide administration in mice. Prog Neuropsychopharmacol Biol Psychiatry. 2018;86:218-228