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Tacrine hydrochloride

CAS No. : 1684-40-8

MCE 国际站：Tacrine hydrochloride

产品活性：Tacrine hydrochloride 是一种 AChE 和 BChE 的有效抑制剂，IC₅₀ 值分别为 31 nM 和 25.6 nM 。Tacrine hydrochloride 也是 NMDAR 的抑制剂， IC₅₀ 值为 26 μM。Tacrine hydrochloride 可用于研究阿尔茨海默氏症。

研究领域：Neuronal Signaling  |  Membrane Transporter/Ion Channel

作用靶点：Cholinesterase (ChE)  |  iGluR

In Vitro: Tacrine (12.5-37.5 nM) inhibits venom acetylcholinesterase as well as human serum butyrylcholinesterase in a concentration-dependent manner.
Tacrine reduces the neurotoxicity induced by the activation of the NMDARs in murine cortical neuronal cultures with an IC₅₀of ~500 μM.
Tacrine inhibits the NMDAR responses in a concentration-dependent manner with an IC₅₀ of ~190 μM at -60 mV.

In Vivo: Tacrine (20-40 μmol/kg; s.c.) disrupts retention of learning in 17- and 30-day old mice in passive avoidance, and while the low dose of tacrine treatment (5 μmol/kg; s.c.) improves retention in 17-day old mice.
Tacrine (0.1-0.4 mg/mL; i.p. for 7 d) inhibits the expression of AChE, but does not significantly improve the protection of the retina function and morphology in mice.

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