"目錄號(hào): HY-14595
Metabolic Enzyme/ProteaseNeuronal Signaling-
Biochanin A 是一種天然存在的脂肪酸酰胺水解酶 (FAAH) 抑制劑，抑制FAAH质况，作用于小鼠，大鼠舱呻，人 FAAH，IC50分別為 1.8芹务，1.4 和 2.4 μM概作。
相關(guān)產(chǎn)品
PF-04457845-BIA 10-2474-LY2183240-URB-597-PF-3845-JNJ-42165279-JZL195-FAAH-IN-2-FAAH inhibitor 1-
生物活性
Description
Biochanin A is a naturally occurring fatty acid amide hydrolase (FAAH) inhibitor, which inhibits FAAH withIC50s of 1.8, 1.4 and 2.4 μM for mouse, rat, and human FAAH, respectively.
IC50& Target
IC50: 1.8 μM (mouse FAAH), 1.4 μM (rat FAAH), 2.4 μM (human FAAH)[1]
In Vitro
Biochanin A inhibits the hydrolysis of 0.5 μM AEA by mouse, rat and human FAAH with IC50s of 1.8, 1.4 and 2.4 μM respectively. FAAH is inhibited by Biochanin A with a pIC50value of 6.21±0.02, corresponding to an IC50value of 0.62 μM. 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 μM [3H]AEA with assay conditions giving these higher utilization rates, the activity is still inhibited by Biochanin A, Genistein, Formononetin and Daidzein in the low micromolar range (IC50s of 6.0, 8.4, 12 and 30 μM, respectively)[1].
In Vivo
Biochanin A is tested at doses of 30, 100 and 300 μg. 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 μg i.pl.) and Biochanin A (100 μg 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 μg 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.)[1].
References
