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- 產(chǎn)品描述： PNU-120596 (NSC 216666) is a potent and selective α7 nAChR positive allosteric modulator (PMA) with an EC50 of 216 nM. PNU-120596 is inactive against α4β2, α3β4, and α9α10 nAChRs. PNU-120596 has the potential for psychiatric and neurological disorders research
- 靶點(diǎn)： EC50: 216 nM (α7 nAChR)
- 體外研究： PNU-120596 increases agonist-evoked calcium flux mediated by an engineered variant of the human α7 nAChR. Electrophysiology studies confirme that PNU-120596 increases peak agonist-evoked currents mediated by wild-type receptors and also demonstrates a pronounced prolongation of the evoked response in the continued presence of agonist. PNU-120596 increases the channel mean open time of α7 nAChRs.
When applied to acute hippocampal slices, PNU-120596 increases the frequency of ACh-evoked GABAergic postsynaptic currents measured in pyramidal neurons.
PNU-120596 enhances agonist-evoked gating of nicotinic receptors by eliciting conformational effects that are similar but nonidentical to the gating conformations promoted by ACh.
- 體內(nèi)研究： PNU-120596 (1 mg/kg; intravenous injection; once) treatment improves the auditory gating deficit caused by Amphetamine in rats, a model proposed to reflect a circuit level disturbance associated with schizophrenia.
When administered before carrageenan, NU-120596 (30 mg/kg; i.p.) significantly reduces mechanical hyperalgesia and weight-bearing deficits for up to 4 h in Sprague-Dawley rats. PNU-120596 attenuates the carrageenan-induced increase in levels of TNF-α and IL-6 within the hind paw oedema Animal Model: Male Sprague Dawley rats (250-300 g) treated with Amphetamine Dosage: 1 mg/kg Administration: Intravenous injection; once Result: Improved the auditory gating deficit caused by Amphetamine.
- 細(xì)胞實(shí)驗(yàn)： Cell lines: MCF7 和 Ishikawa 細(xì)胞 Concentrations: 1000 nM Incubation Time: 8天 Method: MCF7和Ishikawa細(xì)胞在10%三倍活性炭處理的包含血清的培養(yǎng)基中生長3天。然后細(xì)胞以2,000細(xì)胞/孔的密度接種在96孔組織培養(yǎng)板，并按照指示每48小時處理一次。使用CellTiter-Glo發(fā)光細(xì)胞活性試劑盒根據(jù)制造商方案次處理后，第8天，進(jìn)行細(xì)胞增殖試驗(yàn)
- 動物實(shí)驗(yàn)： Animal Models: 負(fù)荷 MCF-7 人乳腺腫瘤異種移植物的小鼠 Dosages: 8 mg/kg Administration: p.o.
- 參考文獻(xiàn)：
1. Hurst RS, 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.
2. Barron SC, et al. An allosteric modulator of alpha7 nicotinic receptors, N-(5-Chloro-2,4-dimethoxyphenyl)-N'-(5-methyl-3-isoxazolyl)-urea (PNU-120596), causes conformational changes in the extracellular ligａnd binding domain similar to those caused by acetylcholine. Mol Pharmacol, 2009 76(2), 253-263.
3. Munro G, et al. The α7 nicotinic ACh receptor agonist compound B and positive allosteric modulator PNU-120596 both alleviate inflammatory hyperalgesia and cytokine release in the rat. Br J Pharmacol, 2012, doi: 10.1111/j.1476-5381.2012.02003.x
- 溶解度： Soluble in DMSO
- 保存條件： -20℃
- 配置溶液濃度參考：
1mg 5mg 10mg 1 mM 3.208 ml 16.04 ml 32.08 ml 5 mM 0.642 ml 3.208 ml 6.416 ml 10 mM 0.321 ml 1.604 ml 3.208 ml 50 mM 0.064 ml 0.321 ml 0.642 ml
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