Fast water-exchange Gd3+-(DO3A-like) complex functionalized with aza-15-crown-5 showing prolonged residence lifetime in vivo.
A bis-hydrated Gd3+ complex based on tris acetic acid-1,4,7,10-tetraazacyclododecane (DO3A) that was functionalized with aza-15-crown-5 demonstrated a nearly optimal water-exchanging rate (k(ex) = 3.1 x 10(7) s(-1)) and low acute cytotoxicity. Efficient magnetic resonance signal intensity enhancements and prolonged residence lifetime induced by this small molecular complex in vivo were demonstrated even with one-fifth of the standard dosage used in the clinic.
Li
Cong
C
Department of Chemistry and Open Laboratory of Chemical Biology of the Institute of Molecular Technology for Drug Discovery and Synthesis, The University of Hong Kong, Pokfulam Road, Hong Kong, PR China.
Li
Ying-Xia
YX
Law
Ga-Lai
GL
Man
Kwan
K
Wong
Wing-Tak
WT
Lei
Hao
H
D000818:Animals; D001372:Aza Compounds / Q000737:chemistry*; D002412:Cations / Q000737:chemistry; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D000080027:Cyclams; D005682:Gadolinium / Q000737:chemistry* / Q000494:pharmacology*; D006571:Heterocyclic Compounds / Q000737:chemistry*; D006801:Humans; D008279:Magnetic Resonance Imaging; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D051381:Rats; D013997:Time Factors; D014867:Water / Q000737:chemistry*
D001372:Aza Compounds; D002412:Cations; D000080027:Cyclams; D006571:Heterocyclic Compounds; D014867:Water; C038072:cyclen; D005682:Gadolinium