Abstract |
To develop new radiopharmaceuticals for interventional radionuclide therapy of locally recurrent prostate cancer, poly[N-(3-aminopropyl) methacrylamide] [ poly(APMA)] polymers were synthesized by free radical precipitation polymerization in acetone- dimethylsulfoxide using N,N'- azobis(isobutyronitrile) as the initiator. The polymers were characterized with nuclear magnetic resonance, size exclusion chromatography, and dynamic light scattering (M(n) = 2.40 x 10(4), M(w)/M(n) = 1.87). Subsequently, poly[APMA] was coupled with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid ( DOTA) using 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride as an activator, followed by conjugation with (64)Cu radionuclide. Prolonged retention of poly[APMA]- DOTA-(64)Cu conjugates within the tumor tissues was demonstrated by micro-positron emission tomography at 24 hours following intra-tumoral injection of the conjugates to human prostate xenografts in mice. The data suggest that the poly[APMA]- DOTA-(64)Cu conjugates might be useful for interventional radionuclide therapy of locally recurrent prostate cancer in humans.
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Authors | Jianchao Yuan, Yezi You, Xin Lu, Otto Muzik, David Oupicky, Fangyu Peng |
Journal | Molecular imaging
(Mol Imaging)
2007 Jan-Feb
Vol. 6
Issue 1
Pg. 10-7
ISSN: 1535-3508 [Print] England |
PMID | 17311761
(Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
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Chemical References |
- Acrylic Resins
- Heterocyclic Compounds, 1-Ring
- Nitriles
- Organometallic Compounds
- Radiopharmaceuticals
- poly(N-(3-aminopropyl)methacrylamide)-DOTA-64Cu conjugate
- 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
- azobis(isobutyronitrile)
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Topics |
- Acrylic Resins
(analysis, chemical synthesis, pharmacokinetics)
- Animals
- Heterocyclic Compounds, 1-Ring
(chemistry)
- Humans
- Light
- Magnetic Resonance Spectroscopy
- Male
- Mice
- Mice, Inbred Strains
- Nitriles
(chemistry)
- Organometallic Compounds
(analysis, chemical synthesis, pharmacokinetics)
- Positron-Emission Tomography
- Prostatic Neoplasms
(chemistry, metabolism, radiotherapy)
- Radiopharmaceuticals
(analysis, chemical synthesis, pharmacokinetics)
- Scattering, Radiation
- Xenograft Model Antitumor Assays
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