title: Basic design and synthesis of sulfonated contrast agents for magnetic resonance imaging based on gadolinium complexes.
abstract: Magnetic resonance angiography (MRA) is an imaging method to examine blood vessels based on the magnetic resonance imaging (MRI) technique. For this purpose, blood pool contrast agents have been developed to selectively increase the signal intensity of the intravascular lumen for improvement of the contrast-to-noise ratio in MR images. Here, we describe the design and the syntheses of six novel sulfonated contrast agents (KMR-Sulfo1 - 6), their chemical properties and their in vivo applications. In this study, we investigated the lipophilicity and the hydrophilicity of a gadolinium complex using a convenient two-step synthesis route, with the goal of prolonging the plasma half-life by binding mainly to human serum albumin. We confirmed that KMR-Sulfo5 fulfilled the requirements as a blood pool contrast agent: it showed a sufficient relaxivity r(1) of 5.9 mM(-1) s(-1), a long plasma half-life of 25.7 min and complete elimination from the body within 12 h after the administration.
authors.affiliation: Department of Applied Chemistry, Faculty of Science and Technology, Keio University, 3-14-1 Hiyoshi, Kohoku, Yokohama 223-8522, Japan.
authors.forename: Hiroki
authors.initials: H
authors.lastname: Hifumi
authors.forename: Akihiro
authors.initials: A
authors.lastname: Tanimoto
authors.forename: Aki
authors.initials: A
authors.lastname: Honda
authors.forename: Daniel
authors.initials: D
authors.lastname: Citterio
authors.forename: Koji
authors.initials: K
authors.lastname: Suzuki
mesh_terms: D000818:Animals; D003287:Contrast Media / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D005682:Gadolinium / Q000737:chemistry* / Q000493:pharmacokinetics; D006207:Half-Life; D008099:Liver / Q000098:blood supply; D018810:Magnetic Resonance Angiography; D008297:Male; D051381:Rats; D013457:Sulfur Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics
chemical_list: D003287:Contrast Media; D013457:Sulfur Compounds; D005682:Gadolinium