WAY 200070

Description: WAY-200070 is a selective agonist of the estrogen receptor beta (ERRbeta) with an IC50 of 2.3 nM. Recent studies have reported that estrogen has antidepressant-like effects in animal models. As an ERRbeta agonist, WAY-200070 has antidepressant and anxiolytic activities as shown in multiple in vivo mouse models. Upon administration, WAY-200070 (30 mg/kg s.c.) caused the nuclear translocation of striatal ER beta receptors from the cytosol. WAY-200070 also increased c-fos activation 4h, but not 15 min after administration. Both nuclear translocation and c-fos induction effects of WAY-200070 demonstrate that WAY-200070 has bound to estrogen receptors and triggered downstream events. The absence of these effects in the ER beta KO mice confirms that WAY-200070 was targeting ER beta. Administration of WAY-200070 (30 mg/kg s.c.) produced a delayed approximately 50% increase in dopamine in the striatum of wild type mice.

References: Neuropharmacology. 2008 Jun; 54(7):1136-42.