Abstract
The aim of this study was to investigate the in vitro and in vivo performance of a 67Ga complex with cis, cis-1, 3, 5-triaminocyclohexane-N, N′, N″-triacetic acid (tachta) as a potential ligand for use as a Ga(III) radiopharmaceutical for PET imaging. The radiolabeling procedure, electrophoretic properties, lipophilicity, acid stability, human serum stability and biodistribution in mice of 67Ga(tachta) were investigated. The 67Ga(tachta) complex forms at 10-3 M tachta concentration at 40°C in 100% yield; it is neutral, non-lipophilic, 90% stable at pH = 4 and 5 and 100% stable at pH = 6, for at least 8 d. Serum stability experiments demonstrated that at 5 hr 67Ga(tachta) exists in serum as a free complex. At 24 hr, 30% of 67Ga(tachta) is reversibly bound to transferrin-albumin fraction of serum, and that this percentage remains unchanged for a period of 4 d. Biodistribution in mice showed that 67Ga(tachta) rapidly clears via the kidneys from the body with less than 10% of injected activity left in the body at 3 hours and only 6% remaining after 24 hr. The complex also cleared rapidly from all of the major organs, with bone showing some slightly increased (1.15% ID/g) 24 hr accumulation, in comparison with the 3 hr time point. Based upon these data, 67Ga(tachta) may be considered as a candidate for developing new Ga(III) radiopharmaceuticals for PET.
Original language | English (US) |
---|---|
Pages (from-to) | 695-701 |
Number of pages | 7 |
Journal | Nuclear Medicine and Biology |
Volume | 28 |
Issue number | 6 |
DOIs | |
State | Published - 2001 |
Externally published | Yes |
Keywords
- Cis
- Cis-1, 3, 5-triaminocyclohexane-N
- Ga
- N′, N″-triacetic acid (tachta)
ASJC Scopus subject areas
- Molecular Medicine
- Radiology Nuclear Medicine and imaging
- Cancer Research