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Non-Indoles. Baicalein.

(Note: all prices are listed in CAD.)

Baicalein, aka 3,4,5-trihydroxyflavone, is a naturally-occurring phenolic flavone isolated from the plant Scutellaria baicalensis. It is similar in pharmacophore to other flavones such as apigenin, K36, and baicalin (the latter of which is a less bioavailable prodrug for baicalein). Various flavone derivatives appear to display similar in vitro binding affinity to benzodiazepenes at the BZD-specific GABAnergic binding sites[1]. This results in the increase of ionic current caused by chloride flow from the ligand gated channels. Animal studies have confirmed its action as a positive allosteric modulator of the GABAnergic site and it has shown to substitute for benzodiazepenes in rat discrimination studies[2]. Baicalein is also shown to have neuroprotective effects against beta-amyloid proteins in vitro [3], anticarcinogenic effects in vitro [4], and is a known potent inhibitor of viral mRNA transcriptases, including those for HIV [5].

This compound is NOT intended for human consumption, and is for laboratory reagent or forensic/analytical purposes ONLY. The intent of its sale is agrochemical and other agricultural research.

[1] – Marder, M., Estiú, G., Blanch, L. B., Viola, H., Wasowski, C., Medina, J. H., & Paladini, A. C. (2001). Molecular modeling and QSAR analysis of the interaction of flavone derivatives with the benzodiazepine binding site of the GABA A receptor complex. Bioorganic & Medicinal Chemistry, 9(2), 323-335. doi:10.1016/s0968-0896(00)00250-9
[2] – Wolfman, C. (1998). Pharmacological Characterization of 6-Bromo-3′-nitroflavone, a Synthetic Flavonoid with High Affinity for the Benzodiazepine Receptors. Pharmacology Biochemistry and Behavior, 61(3), 239-246. doi:10.1016/s0091-3057(98)00088-4
[3] – Choi, R. C., Zhu, J. T., Yung, A. W., Lee, P. S., Xu, S. L., Guo, A. J., . . . Tsim, K. W. (2013). Synergistic Action of Flavonoids, Baicalein, and Daidzein in Estrogenic and Neuroprotective Effects: A Development of Potential Health Products and Therapeutic Drugs against Alzheimer’s Disease. Evidence-Based Complementary and Alternative Medicine, 2013, 1-10. doi:10.1155/2013/635694
[4] – Li-Weber, M. (2009). New therapeutic aspects of flavones: The anticancer properties of Scutellaria and its main active constituents Wogonin, Baicalein and Baicalin. Cancer Treatment Reviews, 35(1), 57-68. doi:10.1016/j.ctrv.2008.09.005
[5] – Matthée, G., Wright, A. D., & König, G. M. (1999). HIV Reverse Transcriptase Inhibitors of Natural Origin. Planta Medica, 65(6), 493-506. doi:10.1055/s-1999-14004