G-15

G protein-coupled estrogen receptor (GPER), or GPR30, specifically binds natural and man-made estrogens.{23445} It is thought to be involved in estrogen-sensitive cancers.{23445,23446} GPER knockout mice are fertile, although they exhibit thymic atrophy, impaired glucose tolerance, and altered bone growth.{23445} G-15 is a cell-permeable non-steroidal antagonist of GPER (Ki = 20 nM).{23444} It displays low affinity cross-reactivity with the classical estrogen receptor (ER), ER?, so that at doses greater than 1 µM it is capable of mediating limited ER-dependent transcriptional activity.{23443} G-15 antagonizes the anti-depressive effects of estrogen in vivo.{23444}