The New Polyamine Multi-carboxylation With The Material Class Of Magnetic Resonance Imaging Contrast Agent

Magnetic resonance imaging (MRI) is one of the most advanced techniques of medicinal imaging diagnosis. It possesses the excellence of non-radianU non-trauma, provides the image of every direction layer and higher contrast image of parenchyma. Under the adscititious magnetic field, it can produce different magnetic resonance signal due to the different capacity between the normal and affected tissue in critter vivo. Above 30% MRI investigations need to use contrast agents in clinical application. Because the MRI contrast agent can shorten the relaxation times of 1H nuclear spin, so that can changed the magnetic resonance signal of partial tissue, increased the susceptivity of MRI diagnosis, improved the definition of image. Some paramagnetic complexes which were routinely used as contrast agents are short of the high relaxation rate and organ-selectivity. In order to conquer these defectes, many agents were investigated to modify the DTPA(diethylene triaminepentaacetic acid) and DOTA (1,4,7,10-tetraazacyclodo-decane-N,N',N",N'''-tetra acetic acid). In this paper, we used the 4-amino-antipyrine (4-APP) and compounds contain pyrimidine group to modify the DTPA and EDTA, and attempt to obtain tissue-specific contrast agents with high relaxivities.1. Two novel ligands of DTPA-4-APP and EDTA-4-APP derivatives have been synthesized respectively by reaction of DTPA-dianhydride and EDTA-dianhydride with4-APP. Their complexes of gadolinum manganese and iron were prepared. The structures of two ligands and their complexes are analyzed by IR,1H NMR and elemental analysis. The NMR T1 relaxivitives(R1) of complexes have been investigated and the results showed that the Gd(III) complexes possesse the precondition to be contrast agents for magnetic resonance imaging.2. The spin-lattice relaxivity(T1) of a Gd(DTPA-4-APP) complex in bovine serumalbumin(BSA) solution has been investigated. The result indicated that the Gd(DTPA-4-APP) in BSA took on a higher relaxation rate by integrate non-covalently with BSA and formed two integrate species[Gd(DTPA-4-AAP)]-BSA,and [Gd(DTPA-4-AAP)]2-BSA.3. DTPA be modified by five compounds contain pyrimidine group,and their complexes of gadolinium were prepared. Spin-lattice relaxivities(T1) has been investigated.Gd(DTPA -2-amino-4,6-bimethyl-pyrimidine) and Gd(DTPA-4-amino-aminouracil) have higher relaxivities and possess the precondition to be the contrast agents for magnetic resonance imaging.