Abstract |
I-131-labeled alpha-amino-(4-hydroxybenzylidene)-diphosphonate ( BDP3) was examined in Sprague-Dawley rats for its bone affinity and other biokinetical characteristics. Iodine-131 BDP3 exhibited high bone affinity, with rapid blood clearance and renal excretion. Total-body retention measurements revealed an effective half-life of the activity of t1/2 = 169 hr. Similar kinetics were found in rat femurs, with t1/2 = 158 hr. Rats bearing osteosarcomas showed an enhanced uptake with a slower clearance (t1/2 = 177 hr). The amount of I-131 BDP3 excreted in urine agreed with the total body retention values. Fifty percent was excreted in the urine, as unchanged I-131 BDP3, by 24 hr after application. Almost no activity was found in the feces of the rats. LD50 measurements in rats amounted to 64 mg/kg. Because of these biokinetical characteristics and the simple labeling procedure, I-131 BDP3 is suggested as a radiopharmaceutical for the palliative treatment of pain that often accompanies disseminated bone metastases.
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Authors | M Eisenhut |
Journal | Journal of nuclear medicine : official publication, Society of Nuclear Medicine
(J Nucl Med)
Vol. 25
Issue 12
Pg. 1356-61
(Dec 1984)
ISSN: 0161-5505 [Print] United States |
PMID | 6209369
(Publication Type: Journal Article)
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Chemical References |
- Benzylidene Compounds
- Diphosphonates
- Iodine Radioisotopes
- alpha-amino-(4-hydroxybenzylidene)diphosphonate
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Topics |
- Animals
- Benzylidene Compounds
(metabolism)
- Bone Neoplasms
(radiotherapy, secondary)
- Diphosphonates
(metabolism)
- Iodine Radioisotopes
(therapeutic use)
- Male
- Osteosarcoma
(radiotherapy, secondary)
- Palliative Care
- Rats
- Rats, Inbred Strains
- Tissue Distribution
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