The invention discloses a highly
inert Gd-
DOTA-based contrast agent with a hydrophobic
side chain as well as a preparation method and application of the highly
inert Gd-
DOTA-based contrast agent, and two novel Gd-
DOTA-based contrast agents Gd-L1 and Gd-L2 are successfully developed by respectively connecting hydrophobic 3-phenyl
propylamine and 3, 3-diphenyl
propylamine to Gd-DOTABA. The two novel Gd-DOTA-based contrast agents remarkably improve the chemical inertness of the complex, the dissociation half-life period of the complex in a 1 M HCl solution at 37 DEG C is about 5 times that of Gd-DOTA, and a powerful guarantee is provided for
clinical safety; the MRI (
Magnetic Resonance Imaging) performance of the liver in a mouse shows that Gd-L1 is equivalent to commercially available Gd-BOPTA and is suitable for imaging of a liver and
gall system; after the Gd-L2 is combined with the
human serum albumin, the
longitudinal relaxation rate is obviously increased (r1 = 14.8 mM <-1 > s <-1 >, 1.4 T, 37 DEG C), the blood
elimination half-life period in a rabbit model is about 18 minutes, and the Gd-L2 is suitable for vascular MRI (
Magnetic Resonance Imaging). The two contrast agents avoid the
spleen residual problem, the organ accumulation possibility is reduced, and a
safer and more efficient MRI diagnostic tool is provided for clinic.