Document Detail

MedLine Citation:
PMID:  11518651     Owner:  NLM     Status:  MEDLINE    
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 degrees 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.
E Dadachova; C Park; N Eberly; D Ma; C H Paik; M W Brechbiel
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Nuclear medicine and biology     Volume:  28     ISSN:  0969-8051     ISO Abbreviation:  Nucl. Med. Biol.     Publication Date:  2001 Aug 
Date Detail:
Created Date:  2001-08-23     Completed Date:  2001-12-07     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  9304420     Medline TA:  Nucl Med Biol     Country:  England    
Other Details:
Languages:  eng     Pagination:  695-701     Citation Subset:  IM    
Radioimmune and Inorganic Chemistry Section, Radiation Oncology Branch, National Cancer Institute, NIH, Bethesda, MD 20892, USA.
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MeSH Terms
Cyclohexanes / blood,  chemical synthesis,  pharmacokinetics*
Drug Stability
Gallium Radioisotopes / pharmacokinetics
Hydrogen-Ion Concentration
Metabolic Clearance Rate
Mice, Inbred BALB C
Radioligand Assay
Radiopharmaceuticals / blood,  chemical synthesis*,  pharmacokinetics
Tissue Distribution
Tomography, Emission-Computed
Reg. No./Substance:
0/Cyclohexanes; 0/Gallium Radioisotopes; 0/H3tachta; 0/Radiopharmaceuticals

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