Discovery and Preclinical Characterization of (+)-3-[4-(1- Piperidinoethoxy)phenyl]spiro[indene- 1,1‘-indane]-5,5‘-diol Hydrochloride:  A Promising Nonsteroidal Estrogen Receptor Agonist for Hot Flush

Abstract

In our studies of the development of a novel class of selective estrogen receptor modulators, (+)-3-[4-(1-piperidinoethoxy)phenyl]spiro[indene-1,1'-indane]-5,5'-diol hydrochloride (1) was found to be an estrogen receptor ligand with beneficial effects in rat models for human hot flush. Moreover, 1 was found to have beneficial effects on lipid and bone metabolism while maintaining marginal effects on the uterus and breasts. These findings suggest that 1 would provide a new treatment for hot flush.