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Biochanin A

CAS No. : 491-80-5

MCE 站：Biochanin A

产品活性：Biochanin A 是一种天然存在的脂肪酸酰胺水解酶 (FAAH) 抑制剂，抑制FAAH，作用于小鼠，大鼠，人 FAAH，IC₅₀ 分别为 1.8，1.4 和 2.4 μM。

研究领域：Metabolic Enzyme/Protease  |  Neuronal Signaling  |  Autophagy

作用靶点：FAAH  |  Autophagy

In Vitro: Biochanin A inhibits the hydrolysis of 0.5 ?M AEA by mouse, rat and human FAAH with IC₅₀ s of 1.8, 1.4 and 2.4 ?M respectively. FAAH is inhibited by Biochanin A with a pIC₅₀ value of 6.21±0.02, corresponding to an IC₅₀ value of 0.62 ?M. Biochanin A produces significant inhibition of the URB597-sensitive tritium retention at high nanomolar-low micromolar concentrations. Experiments are run with human FAAH and 0.5 ?M [³H]AEA with assay conditions giving these higher utilization rates, the activity is still inhibited by Biochanin A, Genistein, Formotin and Daidzein in the low micromolar range (IC₅₀s of 6.0, 8.4, 12 and 30 ?M, respectively).

In Vivo: Biochanin A is tested at doses of 30, 100 and 300 ?g. The highest dose also reduced formalin-induced ERK phosphorylation in a manner antagonized by AM251. Thus, Biochanin A behaved like URB597 after local administration to the paw. In anaesthetized mice, URB597 (30 ?g i.pl.) and Biochanin A (100 ?g i.pl.) both inhibit the spinal phosphorylation of extracellular signal-regulated kinase produced by the intraplantar injection of formalin. The effects of both compounds are significantly reduced by the CB1 receptor antagonist/inverse agonist AM251 (30 ?g i.pl.). Biochanin A (15 mg/k i.v.) does not increase brain AEA concentrations, but produces a modest potentiation of the effects of 10 mg/kg i.v. AEA in the tetrad test. Biochanin A (15 mg/kg i.v.) is without effects on its own, but significantly potentiates the effects of AEA (10 mg/kg i.v.).

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