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Biodistribution, toxicity and radiation dosimetry studies of the serotonin transporter radioligand 4-[18F]-ADAM in rats and monkeys.
- Source :
-
European journal of nuclear medicine and molecular imaging [Eur J Nucl Med Mol Imaging] 2010 Mar; Vol. 37 (3), pp. 545-55. Date of Electronic Publication: 2009 Oct 10. - Publication Year :
- 2010
-
Abstract
- Purpose: 4-[(18)F]-ADAM is a potent serotonin transport imaging agent. We studied its toxicity in rats and radiation dosimetry in monkeys before human studies are undertaken.<br />Methods: Single and multiple-dosage toxicity studies were conducted in Sprague-Dawley rats. Male and female rats were injected intravenously with 4-F-ADAM as a single dose of 1,023.7 microg/kg (1,000 times the human dose) or as five consecutive daily doses of 102.37 microg/kg (100 times the human dose). PET/CT scans were performed in seven Formosa Rock monkeys (four males and three females) using a Siemens Biograph scanner. After injection of 4-[(18)F]-ADAM (182+/-8 MBq), a low dose CT scan and a series of eight whole-body PET scans were performed. Whole-body images were acquired in 3-D mode. Time-activity data of source organs were used to calculate the residence times and estimate the absorbed radiation dose using OLINDA/EXM software.<br />Results: In the rats neither the single dose nor the five daily doses of 4-F-ADAM produced overt adverse effects clinically. In the monkeys the radiation doses received by most organs ranged between 7.1 and 35.7 microGy/MBq, and the urinary bladder was considered to be the critical organ. The effective doses extrapolated to male and female adult humans were 17.4 and 21.8 microSv/MBq, respectively.<br />Conclusion: Toxicity studies in Sprague-Dawley rats and radiation dosimetry studies in Formosa Rock monkeys suggested that 4-[(18)F]-ADAM is safe for use in human PET imaging studies.
- Subjects :
- Adult
Animals
Benzylamines chemistry
Benzylamines metabolism
Female
Humans
Male
Radiation Dosage
Radioligand Assay
Radiometry
Rats
Tissue Distribution
Benzylamines pharmacokinetics
Benzylamines toxicity
Fluorine Radioisotopes chemistry
Haplorhini
Serotonin Plasma Membrane Transport Proteins metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1619-7089
- Volume :
- 37
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- European journal of nuclear medicine and molecular imaging
- Publication Type :
- Academic Journal
- Accession number :
- 19820930
- Full Text :
- https://doi.org/10.1007/s00259-009-1281-z