EDHPA based contrast agents for MR imaging, apparatus and method

Drug – bio-affecting and body treating compositions – In vivo diagnosis or in vivo testing – Magnetic imaging agent

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128653, 128654, 514499, 514501, 514510, 514730, 514741, 514748, 514836, 534 10, 534 15, 534 16, 556 50, 556 61, 556116, 556148, A61K 4900

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047465077

ABSTRACT:
Ethylene Diamine Hydroxy Phenylacetic Acid (EDHPA) type chelators strongly bind paramagnetic metal ions to provide excellent contrast agents for magnetic resonance (MR) imaging. The magnetic dipole generated by unpaired electrons within the paramagnetic (PM) atom, causes a local reduction in the bulk magnetic field of the MR system. The resulting shortening of the T1 (spin lattice) relaxation time in the hydrogen protons within the area of interest, causes an intense "free induction signal" and a corresponding modulation in the collected scanning data. The tissue of organ of interest appears on the MR display as a high intensity of white area. Background tissue is displayed as darker or lower intensity greys. Each member chelator EDHPA' of the EDHPA family of chelators, is a phenolic analog of EDTA, with variations in the para position radical (PR) of the phenol ring. Each EDHPA' chelator is formed by twin amino acid molecules (phenylalanine etc), which provide twin chelation units having three coordination points each for binding the paramagnetic metal.

REFERENCES:
patent: 2795550 (1957-06-01), Harle et al.
patent: 4442305 (1984-04-01), Weitl et al.
patent: 4647447 (1987-03-01), Gries et al.
Pykett, I. L., Sci. Am., May 1982, pp. 78-88.

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