Abstract
Numerous radiolabeled peptides have been utilized for in vivo imaging of a variety of cell surface receptors. For applications in PET using [ 18F]fluorine, peptides are radiolabeled via a prosthetic group approach. We previously developed solution-phase 18F- "click" radio-labeling and solid-phase radiolabeling using 4-[ 18F]fiuorobenzoic and 2-[18F]fluoropropionic acids. Here we compare the three different radiolabeling approaches and report the effects on PET imaging and pharmacokinetics. The prosthetic groups did have an effect; metabolites with significantly different polarities were observed.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 5901-5904 |
| Number of pages | 4 |
| Journal | Journal of Medicinal Chemistry |
| Volume | 51 |
| Issue number | 19 |
| DOIs | |
| State | Published - Oct 9 2008 |
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ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery
Cite this
In vivo positron emission tomography (PET) imaging with an αvβ6 specific peptide radiolabeled using 18F-"click" chemistry : Evaluation and comparison with the corresponding 4-[18F]fluorobenzoyl- and 2-[18F] fluoropropionyl-peptides. / Hausner, Sven H.; Marik, Jan; Gagnon, M. Karen J; Sutcliffe, Julie.
In: Journal of Medicinal Chemistry, Vol. 51, No. 19, 09.10.2008, p. 5901-5904.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - In vivo positron emission tomography (PET) imaging with an αvβ6 specific peptide radiolabeled using 18F-"click" chemistry
T2 - Evaluation and comparison with the corresponding 4-[18F]fluorobenzoyl- and 2-[18F] fluoropropionyl-peptides
AU - Hausner, Sven H.
AU - Marik, Jan
AU - Gagnon, M. Karen J
AU - Sutcliffe, Julie
PY - 2008/10/9
Y1 - 2008/10/9
N2 - Numerous radiolabeled peptides have been utilized for in vivo imaging of a variety of cell surface receptors. For applications in PET using [ 18F]fluorine, peptides are radiolabeled via a prosthetic group approach. We previously developed solution-phase 18F- "click" radio-labeling and solid-phase radiolabeling using 4-[ 18F]fiuorobenzoic and 2-[18F]fluoropropionic acids. Here we compare the three different radiolabeling approaches and report the effects on PET imaging and pharmacokinetics. The prosthetic groups did have an effect; metabolites with significantly different polarities were observed.
AB - Numerous radiolabeled peptides have been utilized for in vivo imaging of a variety of cell surface receptors. For applications in PET using [ 18F]fluorine, peptides are radiolabeled via a prosthetic group approach. We previously developed solution-phase 18F- "click" radio-labeling and solid-phase radiolabeling using 4-[ 18F]fiuorobenzoic and 2-[18F]fluoropropionic acids. Here we compare the three different radiolabeling approaches and report the effects on PET imaging and pharmacokinetics. The prosthetic groups did have an effect; metabolites with significantly different polarities were observed.
UR - http://www.scopus.com/inward/record.url?scp=53549125801&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=53549125801&partnerID=8YFLogxK
U2 - 10.1021/jm800608s
DO - 10.1021/jm800608s
M3 - Article
C2 - 18785727
AN - SCOPUS:53549125801
VL - 51
SP - 5901
EP - 5904
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 19
ER -