| Autor: |
C J, Mathias, S, Wang, D J, Waters, J J, Turek, P S, Low, M A, Green |
| Rok vydání: |
1998 |
| Předmět: |
|
| Zdroj: |
Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 39(9) |
| ISSN: |
0161-5505 |
| Popis: |
Indium-111-labeled diethylenetriamine pentaacetic acid (DTPA)-folate was evaluated as a radiopharmaceutical for targeting tumor-associated folate receptors.Athymic mice were subcutaneously inoculated with approximately 1.8 x 10(6) folate receptor-positive KB (human nasopharyngeal carcinoma) cells, yielding 0.2- to 0.6-g tumors in 15 days, at which time (111)In-DTPA-folate, (111)In-DTPA or (111)In-citrate was administered by intravenous injection.The (111)In-DTPA-folate conjugate afforded marked tumor-specific (111)In deposition in vivo using this mouse model. The involvement of the folate receptor in mediating tumor uptake of (111)In-DTPA-folate was demonstrated by the blocking of tumor uptake by coadministration of free folic acid (intravenous). The (111)In-DTPA-folate also shows folate receptor-mediated uptake and retention in the kidneys, presumably reflecting radiotracer binding to folate receptors of the proximal tubules. In control experiments, the (111)In-citrate radiopharmaceutical precursor was also shown to afford significant tumor uptake of (111)In, but with much poorer tumor-to-background tissue contrast than that obtained with (111)In-DTPA-folate. Unconjugated (111)In-DTPA showed no tumor affinity.Indium-111-DTPA-folate appears suitable as a radiopharmaceutical for targeting tumor-associated folate receptors. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
|
