PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50≥60μM).
信号通路
Transmembrane Transporters; Neuronal Signaling
靶点
α7 nAChR agonist
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IC50
26nM(Ki)
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体外研究
Treatment with PNU-282987 resulted in an attenuation of neuroinflammation in the MPTP-lesioned SN. Furthermore, PNU-282987 attenuated MPTP-induced dopaminergic cell loss in the SN and reduced striatal dopamine depletion.
体内研究
Mice were subjected to 70% partial hepatic I/R for 60 min and pretreated with either vehicle or with PNU-282987, and blood and hepatic tissue samples were collected at 3, 6 and 12h following reperfusion. pretreatment with PNU-282987 decreased serum transaminase levels and ameliorated liver injury after hepatic I/R. Moreover, pretreatment with PNU-282987 suppressed NF-κB activation, cytokine production (tumor necrosis factor α, interleukin 1β), and HMGB1 expression in liver after hepatic I/R. Mice treated with 2.5 and 10mg/kg of PNU devoted less time to rearing into open arms. In the HB task, MC mice displayed higher exploratory activity reflected in more head-dips (HD) during the first minute than EE and SE, whereas EE displayed low exploration levels reflected in total HD (5 min).
临床实验
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特征
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相关实验数据(此数据来自于公开文献,联迈生物并不保证其有效性):
酶活性检测实验
方法
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细胞实验
细胞系
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浓度
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处理时间
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方法
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动物实验
动物模型
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配制
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剂量
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给药方式
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参考文献: 1. Bodnar AL, et al. J Med Chem. 2005 Feb 24, 48(4), 905-8. 2. Li F, et al. Shock. 2013 Feb, 39(2), 197-203. 3. Stuckenholz V, et al. J Parkinsons Dis. 2013, 3(2), 161-72. 4. Mesa-Gresa P, et al. Behav Processes. 2014 Mar, 103, 117-24. 包装清单: