Stability of MRI paramagnetic contrast media: a proton relaxometric protocol for transmetallation assessment.

Abstract:

RATIONALE AND OBJECTIVES:The suitability of paramagnetic complexes as magnetic resonance contrast agents depends on various factors such as their relaxivity, stability, selectivity, and the inertness toward transmetallation by endogenous ions. The transmetallation of a series of 18 gadolinium complexes by the Zn2+ ion was studied in vitro by proton relaxometry. METHODS:Transmetallation was analyzed through the evolution of the paramagnetic longitudinal relaxation rate of water protons at 37 degrees C in pH = 7 phosphate buffer solutions containing 2.5 mmol/L of the gadolinium complexes and 2.5 mmol/L zinc chloride. The measurements were performed at 0.47 T over a period of at least 3 days. RESULTS:The results confirm the high stability of macrocyclic systems and a high sensitivity of Gd-diethylenetriamine-pentaacetic acid (DTPA) derivatives to transmetallation by Zn2+ ions. The decreasing order of stability with respect to metal exchange is as follows: Gd-macrocyclics > Gd-C-functionalized DTPA > Gd-DTPA > primary and secondary Gd-DTPA bisamides. The ternary bisamide analyzed in this study [Gd-DTPA-1,11-bisbismethylamino-1,11-dioxo-3,6,9-triaza-3,6,9-tris(carboxymethyl)undecane] is more stable than the parent compound Gd-DTPA. CONCLUSIONS:A simple relaxometric protocol has been successfully developed to study the in vitro transmetallation process of gadolinium complexes. The importance of the functionalization and substitution of the DTPA-like complexes is clearly shown.

journal_name

Invest Radiol

journal_title

Investigative radiology

authors

Laurent S,Elst LV,Copoix F,Muller RN

doi

10.1097/00004424-200102000-00008

keywords:

subject

Has Abstract

pub_date

2001-02-01 00:00:00

pages

115-22

issue

2

eissn

0020-9996

issn

1536-0210

journal_volume

36

pub_type

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