WAY-200070

WAY-200070 is a potent and selective agonist of estrogen receptor β (ERβ; IC₅₀s = 2 and 187 nM for human full-length ERβ and ERα, respectively).¹ WAY-200070 (30 mg/kg, s.c. in mice) induces nuclear translocation of ERβ and increases c-fos activation and dopamine levels in the striatum four hours after administration.² At the same dose, it decreases depressive-like behavior in the tail suspension test. It has anxiolytic effects in mice using the four-plate and stress-induced hyperthermia tests and in zebrafish larvae using a light-dark choice behavior test.^2,3 In addition, WAY-200070 improves glucose and insulin sensitivity in mouse models of diabetes.⁴

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1. Malamas, M.S., Manas, E.S., McDevitt, R.E., et al. Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-β ligands. J. Med. Chem. 47(21), 5021-5040 (2004).

2. Hughes, Z.A., Liu, F., Platt, B.J., et al. WAY-200070, a selective agonist of estrogen receptor beta as a potential novel anxiolytic/antidepressant agent. Neuropharmacology 54(7), 1136-1142 (2008).

3. F., C., Chen, S., Liu, S., et al. Effects of lorazepam and WAY-200070 in larval zebrafish light/dark choice test. Neuropharmacology 95, 226-233 (2015).

4. Alonso-Magdalena, P., Ropero, A.B., García-Arévalo, M., et al. Antidiabetic actions of an estrogen receptor β selective agonist. Diabetes 62(6), 2015-2025 (2013).