Synthesis and animal imaging of 99mTc-hydrazinonicotinamide-folate as a new folate receptor-targeted tumor imaging agent.
- Author:
Li-qin LIU
1
;
Shi-zhen WANG
;
Fang LI
;
Bao TENG
;
Ke-zhan WANG
;
Fei-chan QIU
Author Information
- Publication Type:Journal Article
- MeSH: Animals; Female; Mice; Mice, Inbred BALB C; Mice, Inbred ICR; Neoplasms, Experimental; diagnostic imaging; Organotechnetium Compounds; chemical synthesis; pharmacokinetics; Radionuclide Imaging; Radiopharmaceuticals; chemical synthesis; pharmacokinetics; Tissue Distribution
- From: Acta Academiae Medicinae Sinicae 2006;28(6):786-789
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVEThe synthesis, biodistribution, and animal imaging of 99mTc- hydrazinonicotinamide-folate (99mTc-HYNIC-Folate) were studied as a folate receptor-targeted tumor imaging agent.
METHODSHYNIC-Folate was synthesized by a muti-step reaction and radiolabeled with 99mTc using tricine and trisodium phenylphosphine-3, 3', 3"-trisulfonate (TPPTS) as coligands. The radiochemical purity and stability of 99mTc HYNIC-Folate was measured. The biodistributions of 99mTc-HYNIC-Folate in normal mice and tumor-bearing mice were detected. Whole-body gamma imaging was performed using an athymic mouse tumor xenograft model.
RESULTSThe ligand HYNIC-Folate was successfully synthesized and characterized by hydrogen nuclear magnetic resonance (1HNMR) and mass spectrometry (MS). The radiochemical purity of 99mTc-HYNIC-Folate was 96% under optimal conditions. Data from gamma scintigraphy and the biodistribution in tumor-bearing mice showed that 99mTc-HYNIC-Folate predominantly accumulated in tumor, its uptake rate per gram tissue alpham was 5. 620+/- 0. 753. The uptakes of 99mTc-HYNIC-Folate in the other non-target tissues were very low, except it was high in the kidneys ( am was 41. 959 +/-6. 759) .
CONCLUSION99mTc-HYNIC-Folate has the potential to be used as a noninvasive radiodiagnostic imaging agent for the detection of folate receptor-positive human cancers.
