TY - JOUR
T1 - Radiolabeling and in vitro and in vivo characterization of [ 18F]FB-[R8,15,21, L17]-VIP as a PET imaging agent for tumor overexpressed VIP receptors
AU - Cheng, Dengfeng
AU - Yin, Duanzhi
AU - Li, Gucai
AU - Wang, Mingwei
AU - Li, Shiqiang
AU - Zheng, Mingqiang
AU - Cai, Hancheng
AU - Wang, Yongxian
PY - 2006/12
Y1 - 2006/12
N2 - In an effort to develop a peptide-based radiopharmaceutical for the detection of tumors overexpressed vasoactive intestinal peptide receptors with positron emission tomography, we have prepared a novel [R8,15,21, L17]-VIP peptide for 18F-labeling. This peptide inhibited 125I-VIP binding to rats lung membranes with high affinity [half-maximal inhibitory concentrations (IC50) of 0.12 nm]. Additionally, [R8,15,21, L17]-VIP showed higher stability than native vasoactive intestinal peptide in vivo of mice. With N-succinimidyl 4-[18F] fluorobenzoate as labeling prosthetic group, [ 18F]FB-[R8,15,21, L17]-VIP was obtained in >99% radiochemical purity within 100 min in decay-for-corrected radiochemical yield of 33.6 ± 3% (n = 5) and a specific radioactivity 255 GBq/μmol at the end of synthesis. Stability of [18F]FB-[R8,15,21, L17]-VIP in vitro and in vivo were investigated. Biodistribution of this trace was carried out in mice with induced C26 colorectal tumor. Fast clearance of [18F]FB-[R8,15,21, L17]-VIP from non-target tissues and specific uptakes by tumors realized higher tumor-to-muscle ratio (3.55) and tumor-to-blood ratio (2.37) 60 min postinjection. Clear difference was observed between the blocking and unblocking experiments in biodistribution and whole body radioautography. [ 18F]FB-[R8,15,21, L17]-VIP has demonstrated its potential for diagnosing tumors overexpressed vasoactive intestinal peptide receptors both in vitro and in vivo.
AB - In an effort to develop a peptide-based radiopharmaceutical for the detection of tumors overexpressed vasoactive intestinal peptide receptors with positron emission tomography, we have prepared a novel [R8,15,21, L17]-VIP peptide for 18F-labeling. This peptide inhibited 125I-VIP binding to rats lung membranes with high affinity [half-maximal inhibitory concentrations (IC50) of 0.12 nm]. Additionally, [R8,15,21, L17]-VIP showed higher stability than native vasoactive intestinal peptide in vivo of mice. With N-succinimidyl 4-[18F] fluorobenzoate as labeling prosthetic group, [ 18F]FB-[R8,15,21, L17]-VIP was obtained in >99% radiochemical purity within 100 min in decay-for-corrected radiochemical yield of 33.6 ± 3% (n = 5) and a specific radioactivity 255 GBq/μmol at the end of synthesis. Stability of [18F]FB-[R8,15,21, L17]-VIP in vitro and in vivo were investigated. Biodistribution of this trace was carried out in mice with induced C26 colorectal tumor. Fast clearance of [18F]FB-[R8,15,21, L17]-VIP from non-target tissues and specific uptakes by tumors realized higher tumor-to-muscle ratio (3.55) and tumor-to-blood ratio (2.37) 60 min postinjection. Clear difference was observed between the blocking and unblocking experiments in biodistribution and whole body radioautography. [ 18F]FB-[R8,15,21, L17]-VIP has demonstrated its potential for diagnosing tumors overexpressed vasoactive intestinal peptide receptors both in vitro and in vivo.
KW - Colorectal tumor
KW - F
KW - Imaging
KW - Positron emission tomography
KW - Radiolabeling
KW - Vasoactive intestinal peptide
UR - http://www.scopus.com/inward/record.url?scp=33845582681&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=33845582681&partnerID=8YFLogxK
U2 - 10.1111/j.1747-0285.2006.00453.x
DO - 10.1111/j.1747-0285.2006.00453.x
M3 - Article
C2 - 17177894
AN - SCOPUS:33845582681
SN - 1747-0277
VL - 68
SP - 319
EP - 325
JO - Chemical Biology and Drug Design
JF - Chemical Biology and Drug Design
IS - 6
ER -