Water-soluble contrast agents targeted at the estrogen receptor for molecular magnetic resonance imaging

Novel estrogen-conjugated pyridine-containing Gd(III) and Eu(Ill) contrast agents (EPTA-Gd/Eu) were designed and effectively synthesized. Convenient to administration and MRI experiments, both EPTA-Gd and EPTA-Eu are soluble in water. The EPTA-Gd selectively binds with a micromolar affinity to the estrogen receptor and induces proliferation of human breast cancer cells. The EPTA-Gd is not lethal and does not cause any adverse effects when administrated intravenously. It enhances T-1 and T-2 nuclear relaxation rates of water and serves as a selective contrast agent for localizing the estrogen receptor by MRI.