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Synthesis and animal imaging of 99mTc-hydrazinonicotinamide-folate as a new folate receptor-targeted tumor imaging agent / 中国医学科学院学报
Acta Academiae Medicinae Sinicae ; (6): 786-789, 2006.
Artículo en Chino | WPRIM | ID: wpr-313684
ABSTRACT
<p><b>OBJECTIVE</b>The synthesis, biodistribution, and animal imaging of 99mTc- hydrazinonicotinamide-folate (99mTc-HYNIC-Folate) were studied as a folate receptor-targeted tumor imaging agent.</p><p><b>METHODS</b>HYNIC-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.</p><p><b>RESULTS</b>The 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) .</p><p><b>CONCLUSION</b>99mTc-HYNIC-Folate has the potential to be used as a noninvasive radiodiagnostic imaging agent for the detection of folate receptor-positive human cancers.</p>
Asunto(s)
Texto completo: Disponible Índice: WPRIM (Pacífico Occidental) Asunto principal: Diagnóstico por Imagen / Farmacocinética / Distribución Tisular / Cintigrafía / Compuestos de Organotecnecio / Radiofármacos / Ratones Endogámicos BALB C / Ratones Endogámicos ICR / Neoplasias Experimentales Tipo de estudio: Estudio diagnóstico Límite: Animales Idioma: Chino Revista: Acta Academiae Medicinae Sinicae Año: 2006 Tipo del documento: Artículo

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Texto completo: Disponible Índice: WPRIM (Pacífico Occidental) Asunto principal: Diagnóstico por Imagen / Farmacocinética / Distribución Tisular / Cintigrafía / Compuestos de Organotecnecio / Radiofármacos / Ratones Endogámicos BALB C / Ratones Endogámicos ICR / Neoplasias Experimentales Tipo de estudio: Estudio diagnóstico Límite: Animales Idioma: Chino Revista: Acta Academiae Medicinae Sinicae Año: 2006 Tipo del documento: Artículo