303757-49-5Relevant academic research and scientific papers
Bone selective effect of an estradiol conjugate with a novel tetracycline-derived bone-targeting agent
Neale, Jason R.,Richter, Natali B.,Merten, Kevyn E.,Grant Taylor,Singh, Sujan,Waite, Leonard C.,Emery, Nicole K.,Smith, Ned B.,Cai, Jian,Pierce Jr., William M.
supporting information; experimental part, p. 680 - 683 (2009/09/06)
In this study a novel bone-targeting agent containing elements of the tricarbonylmethane system of ring A of tetracycline was developed and was shown to bind to the mineral constituent of bone, hydroxyapatite. Conjugation of this bone-targeting agent to estradiol resulted in a bone-targeted estrogen (BTE2-A1) with an enhanced ability to bind to hydroxyapatite. In an ovariectomized rat model of osteoporosis a partial separation of the skeletal effects of estradiol from the uterine effects was observed following subcutaneous administration of BTE2-A1. This novel bone-targeting estradiol delivery system has the potential to improve the safety profile of estradiol in the treatment of osteoporosis.
