Original contribution
Dissociation of gadolinium chelates in mice: Relationship to chemical characteristics

https://doi.org/10.1016/0730-725X(92)90016-SGet rights and content

Abstract

Tissue distributions of seven 153Gd-labeled Gd chelates were determined at five residence intervals (5 min to 14 days) following intravenous administration of 0.4 mmol/kg to mice. Relationships were sought among physicochemical parameters: thermodynamic and conditional (pH 7.4) equilibrium stability constants (log K and log K′), acid dissociation rate constants (kobs), lipophilicity (log P), overall charge, and size (molecular weight). Size and lipophilicity did not correlate with tissue distributions. There were possible correlations between anionic charge and rapid, early renal excretion and between stability constants and long-term residual Gd deposition. Strong correlations (r > 0.99) were found between acid dissociation rates and long-term deposition of Gd in the whole body, liver, and femur. This is attributed to dissociation of Gd from the chelates in vivo. Acid dissociation rates may be useful in predicting dissociation of Gd from chelates in vivo.

References (29)

  • M.F. Tweedle et al.

    Comparative chemical structure and pharmacokinetics of MRI contrast agents

    Invest. Radiol.

    (1988)
  • D.D. Dischino et al.

    Synthesis of nonionic gadolinium chelates useful as contrast agents for magnetic resonance imaging. 1,4,7-Tris(carboxymethyl)-10-substituted-1,4,7,10-tetraazacyclododecanes and their corresponding gadolinium chelates

    Inorg. Chem.

    (1991)
  • J.F. Desreux

    Nuclear magnetic resonance spectroscopy of lanthanide complexes with tetraacetic tetraaza macrocycles. Unusual conformation properties

    Inorg. Chem.

    (1980)
  • Kumar, K.; Sukumaran, K.U.; Chang, C.A.; Tweedle, M.F.; Eckelman, W.C. True-tracer radiolabeling of gadolinium chelates...
  • Cited by (0)

    View full text