Relaxometry, luminescence measurements, electrophoresis, and animal biodistribution of lanthanide(III) complexes of some polyaza macrocyclic acetates containing pyridine

Won D. Kim, Garry E. Kiefer, Frédéric Maton, Kenneth McMillan, Robert N. Muller, A. Dean Sherry

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Abstract

Four Gd3+ complexes [Gd(BP2A)+, Gd(PC2A)+, Gd(PCTA)0, and Gd(BPO4A)-] with polyazamacrocyclic ligands that contain a pyridine moiety were prepared and examined for possible use as MRI contrast enhancement agents. We estimated the number of inner sphere water molecules (qGd) for the Gd3+ complexes from the values of q found for the Tb3+ and/or Eu3+ complexes by luminescence lifetime measurements. We have estimated that qGd = 3.5, 3.3, 2.4, and 0.2 for Gd(BP2A)+, Gd(PC2A)+, Gd(PCTA)0, and Gd(BPO4A)-, respectively. The inner sphere relaxivities (r1,inner) of these tetraaza macrocyclic complexes were higher than that of Gd(DOTA)- [i.e. 6.79 for Gd(BP2A)+, 6.21 for Gd(PC2A)+, and 4.60 for Gd(PCTA)0 mM-1s-1 at 40 MHz and 25°C], but the normalized relaxivities per qGd (1.94, 1.88, and 1.92 mM-1 s-1, respectively) were comparable to that of Gd(DOTA)-. A quantitative treatment of the NMRD profiles based on Solomon-Bloembergen-Morgan theory, using the NMRD profile of Gd(BPO4A)- to correct for an outer sphere contribution, showed that the complexes exhibit charactenstics similar to that of Gd(DOTA)- but with shorter electronic relaxation times. Tissue biodistribution results using radioactive 153Sm and 159Gd complexes in rats indicate that the cationic [153Sm-(BP2A)+ and 153Sm(PC2A)+] complexes accumulate preferably in the bone tissue while the neutral [153Sm-(PCTA)0] and anionic [153Sm(BPO4A)-] complexes appear to have renal clearances similar to those of other low molecular weight contrast agents [i.e. Gd(DTPA)2- and Gd(DOTA)-].

Original languageEnglish (US)
Pages (from-to)2233-2243
Number of pages11
JournalInorganic Chemistry
Volume34
Issue number8
StatePublished - 1995

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Lanthanoid Series Elements
electrophoresis
Electrophoresis
animals
Luminescence
acetates
pyridines
Animals
Acetates
luminescence
clearances
low molecular weights
Tissue
profiles
Gadolinium DTPA
bones
rats
relaxation time
Magnetic resonance imaging
Relaxation time

ASJC Scopus subject areas

  • Inorganic Chemistry

Cite this

Relaxometry, luminescence measurements, electrophoresis, and animal biodistribution of lanthanide(III) complexes of some polyaza macrocyclic acetates containing pyridine. / Kim, Won D.; Kiefer, Garry E.; Maton, Frédéric; McMillan, Kenneth; Muller, Robert N.; Sherry, A. Dean.

In: Inorganic Chemistry, Vol. 34, No. 8, 1995, p. 2233-2243.

Research output: Contribution to journalArticle

Kim, Won D. ; Kiefer, Garry E. ; Maton, Frédéric ; McMillan, Kenneth ; Muller, Robert N. ; Sherry, A. Dean. / Relaxometry, luminescence measurements, electrophoresis, and animal biodistribution of lanthanide(III) complexes of some polyaza macrocyclic acetates containing pyridine. In: Inorganic Chemistry. 1995 ; Vol. 34, No. 8. pp. 2233-2243.
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T1 - Relaxometry, luminescence measurements, electrophoresis, and animal biodistribution of lanthanide(III) complexes of some polyaza macrocyclic acetates containing pyridine

AU - Kim, Won D.

AU - Kiefer, Garry E.

AU - Maton, Frédéric

AU - McMillan, Kenneth

AU - Muller, Robert N.

AU - Sherry, A. Dean

PY - 1995

Y1 - 1995

N2 - Four Gd3+ complexes [Gd(BP2A)+, Gd(PC2A)+, Gd(PCTA)0, and Gd(BPO4A)-] with polyazamacrocyclic ligands that contain a pyridine moiety were prepared and examined for possible use as MRI contrast enhancement agents. We estimated the number of inner sphere water molecules (qGd) for the Gd3+ complexes from the values of q found for the Tb3+ and/or Eu3+ complexes by luminescence lifetime measurements. We have estimated that qGd = 3.5, 3.3, 2.4, and 0.2 for Gd(BP2A)+, Gd(PC2A)+, Gd(PCTA)0, and Gd(BPO4A)-, respectively. The inner sphere relaxivities (r1,inner) of these tetraaza macrocyclic complexes were higher than that of Gd(DOTA)- [i.e. 6.79 for Gd(BP2A)+, 6.21 for Gd(PC2A)+, and 4.60 for Gd(PCTA)0 mM-1s-1 at 40 MHz and 25°C], but the normalized relaxivities per qGd (1.94, 1.88, and 1.92 mM-1 s-1, respectively) were comparable to that of Gd(DOTA)-. A quantitative treatment of the NMRD profiles based on Solomon-Bloembergen-Morgan theory, using the NMRD profile of Gd(BPO4A)- to correct for an outer sphere contribution, showed that the complexes exhibit charactenstics similar to that of Gd(DOTA)- but with shorter electronic relaxation times. Tissue biodistribution results using radioactive 153Sm and 159Gd complexes in rats indicate that the cationic [153Sm-(BP2A)+ and 153Sm(PC2A)+] complexes accumulate preferably in the bone tissue while the neutral [153Sm-(PCTA)0] and anionic [153Sm(BPO4A)-] complexes appear to have renal clearances similar to those of other low molecular weight contrast agents [i.e. Gd(DTPA)2- and Gd(DOTA)-].

AB - Four Gd3+ complexes [Gd(BP2A)+, Gd(PC2A)+, Gd(PCTA)0, and Gd(BPO4A)-] with polyazamacrocyclic ligands that contain a pyridine moiety were prepared and examined for possible use as MRI contrast enhancement agents. We estimated the number of inner sphere water molecules (qGd) for the Gd3+ complexes from the values of q found for the Tb3+ and/or Eu3+ complexes by luminescence lifetime measurements. We have estimated that qGd = 3.5, 3.3, 2.4, and 0.2 for Gd(BP2A)+, Gd(PC2A)+, Gd(PCTA)0, and Gd(BPO4A)-, respectively. The inner sphere relaxivities (r1,inner) of these tetraaza macrocyclic complexes were higher than that of Gd(DOTA)- [i.e. 6.79 for Gd(BP2A)+, 6.21 for Gd(PC2A)+, and 4.60 for Gd(PCTA)0 mM-1s-1 at 40 MHz and 25°C], but the normalized relaxivities per qGd (1.94, 1.88, and 1.92 mM-1 s-1, respectively) were comparable to that of Gd(DOTA)-. A quantitative treatment of the NMRD profiles based on Solomon-Bloembergen-Morgan theory, using the NMRD profile of Gd(BPO4A)- to correct for an outer sphere contribution, showed that the complexes exhibit charactenstics similar to that of Gd(DOTA)- but with shorter electronic relaxation times. Tissue biodistribution results using radioactive 153Sm and 159Gd complexes in rats indicate that the cationic [153Sm-(BP2A)+ and 153Sm(PC2A)+] complexes accumulate preferably in the bone tissue while the neutral [153Sm-(PCTA)0] and anionic [153Sm(BPO4A)-] complexes appear to have renal clearances similar to those of other low molecular weight contrast agents [i.e. Gd(DTPA)2- and Gd(DOTA)-].

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