Title of article :
Synthesis and pharmacology of a novel pyrrolo[2,1,5-cd]indolizine (NNC 45-0095), a high affinity non-steroidal agonist for the estrogen receptor
Author/Authors :
A. S. J?rgensen، نويسنده , , Joyce P. Jacobsen، نويسنده , , L. B. Christiansen، نويسنده , , P. S. Bury، نويسنده , , A. Kanstrup، نويسنده , , S. M. Thorpe، نويسنده , , Roderick S. Bain، نويسنده , , L. N?rum، نويسنده , , K. Wassermann، نويسنده ,
Abstract :
1-Ethyl-2-(4-hydroxyphenyl)pyrrolo[2,1,5-cd]indolizine (NNC 45-0095) is a novel compound which represents the parent pharmacophore structure of a series of pyrrolo[2,1,5-cd]indolizine derivatives with mixed estrogen agonist/antagonist properties. NNC 45-0095 binds with high affinity to the estrogen receptor (IC50=9.5 nM) and exhibits full protection of bone loss in the ovariectomized mouse model for post-menopausal osteoporosis.
