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GPR30 is a membrane receptor reported to bind 17β-estradiol (E2) and mediate rapid non-genomic estrogen responses, hence also named G protein-coupled estrogen receptor (GPER). G-1 is a proposed GPR30-specific agonist that has been used to implicate the receptor in several pathophysiological events. However, controversy surrounds the role of GPR30 in G-1- and E2 responses. We investigated GPR30 activity in the absence and presence of G-1 and E2 in several eukaryotic systems ex vivo and in vitro in the absence and presence of the receptor
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