PHA-543613

PHA-543613用途

PHA-543613是一种有效的口服活性脑渗透剂和选择性α7 nAChR激动剂,Ki为8.8 nM。PHA-543613显示α7-nAChR对α3β4、α1β1γδ、α4β2和5-HT3受体的选择性【1】。PHA-543613可用于阿尔茨海默病和精神分裂症的认知缺陷研究【2】。

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PHA-543613名称

[ CAS 号 ]:
478149-53-0

[ 英文名 ]:
PHA-543613

[英文别名 ]:

PHA-543613生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 胆碱受体

信号通路 >> 神经信号通路 >> 胆碱受体

研究领域 >> 神经疾病

[ 靶点 ]

Ki: 8.8 nM (α7 nAChR)[1]

[体内研究]

PHA-543613(0.3 mg/kg)成功逆转东莨菪碱诱导的大鼠短期记忆障碍[2]。

[参考文献]

[1]. Donn G Wishka, et al. Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship. J Med Chem. 2006 Jul 13;49(14):4425-36.

[2]. Nóra Bruszt, et al. Potentiation of cognitive enhancer effects of Alzheimer's disease medication memantine by alpha7 nicotinic acetylcholine receptor agonist PHA-543613 in the Morris water maze task. Psychopharmacology (Berl). 2021 Nov;238(11):3273-3281.

PHA-543613物理化学性质

[ 分子式 ]:
C₁₅H₁₇N₃O₂

[ 分子量 ]:
271.31

[ 精确质量 ]:
307.10900

[ PSA ]:
58.37000

[ LogP ]:
2.78260

[ 储存条件 ]:
室温，密封，干燥

PHA-543613MSDS

PHA-543613安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

PHA-543613合成路线

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PHA-543613文献

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J. Neuroinflammation 5 , 32, (2008)

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