Magnetic resonance imaging (MRI) contrast agents that target the brain


Patrick J. O'Connell,, James I. Bruce,, and Michael Mortimer, Department of Chemistry, The Open University, Walton Hall, Milton Keynes, MK7 6AA, United Kingdom
Currently available commercial contrast agents do not cross an intact blood brain barrier (BBB) and are therefore only clinically useful when the BBB is disrupted due to disease. The aim of this project is to synthesise a gadolinium complex that may cross an intact BBB and enable imaging of the brain before a diseased state (eg tumour) has reached an advanced stage and consequently difficult to treat. Once the core ligand has been synthesised, it can be linked to a molecule, R, which promotes transport across the BBB. This ligand can then be reacted with gadolinium chloride to produce a charge-neutral, heptadentate complex. The ability of the complex to enhance the MRI signal can be determined by performing water relaxivity measurements. Its ability to cross the BBB can be estimated by performing octanol-water partitioning measurements. This poster describes the synthesis of the above contrast agents and measurements performed on them.


New Reactions and Methodology, Materials, Total Synthesis, Process R&D
8:00 PM-10:00 PM, Sunday, 28 August 2005 Washington DC Convention Center -- Hall A, Poster

8:00 PM-10:00 PM, Monday, 29 August 2005 Washington DC Convention Center -- Hall A, Sci-Mix

Division of Organic Chemistry

The 230th ACS National Meeting, in Washington, DC, Aug 28-Sept 1, 2005