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 |
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| Authors: | Jørgensen A S Jacobsen P Christiansen L B Bury P S Kanstrup A Thorpe S M Bain S Naerum L Wassermann K |
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| Institution: | 1. Department of Polymer Science & Engineering, Graduate School of Science and Engineering, Yamagata University, 4-3-16 Jonan, Yonezawa, Yamagata 992–8510, Japan;2. Research Center for Integrative Molecular Systems, Institute for Molecular Science, Myodaiji, Okazaki 444–8787, Japan;3. Division of Applied Chemistry, Graduate School of Engineering, Osaka University, 2–1 Yamadaoka, Suita, Osaka 565–0871, Japan |
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| Abstract: | 1-Ethyl-2-(4-hydroxyphenyl)pyrrolo2,1,5-cd]indolizine (NNC 45-0095) is a novel compound which represents the parent pharmacophore structure of a series of pyrrolo2,1,5-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. |
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