@article {pmid24970911,
	title = {{P}reclinical evaluation of a high-affinity 18{F}-trifluoroborate octreotate derivative for somatostatin receptor imaging}},
	journal = {J. Nucl. Med.},
	volume = {55},
	number = {9},
	year = {2014},
	month = {Sep},
	pages = {1499{\textendash}1505},
	abstract = {{Recent studies have highlighted the high sensitivity of PET imaging with (68)Ga-labeled octreotide derivatives for the detection and staging of neuroendocrine tumors. A somatostatin receptor ligand that is easily radiolabeled with (18)F-fluoride could improve the availability of PET imaging of neuroendocrine tumors. We report an alkyltrifluoroborate-octreotate conjugate that is radiolabeled in a 1-step (18)F exchange reaction in high yield and with high specific activity.\\ We conjugated a new alkyltrifluoroborate to octreotate to obtain AMBF3-TATE, which was stored in 50-nmol aliquots for radiolabeling. (18)F labeling was performed by (18)F-(19)F isotope exchange with (18)F-fluoride, and the tracer was purified by C18 cartridge separation. The radiochemical yield was 20\%-25\%. PET imaging and biodistribution were performed on mice bearing AR42J tumor xenografts.\\ AMBF3-TATE bound the somatostatin receptor subtype 2 with high affinity (inhibition constant, 0.13 {\^A}{\textpm} 0.03 nM). Starting with 29.6-37 GBq (0.8-1 Ci) of (18)F-fluoride, more than 7.4 GBq (>200 mCi) of (18)F-AMBF3-TATE were obtained in 25 min (n = 5) with greater than 99\% radiochemical purity at high specific activity (>111 GBq [3 Ci]/{\^I}{\textonequarter}mol). (18)F-AMBF3-TATE was stable in plasma. PET imaging and biodistribution showed rapid renal excretion with low liver activity. High tumor uptake (10.11\% {\^A}{\textpm} 1.67\% injected dose/g},
	author = {Liu, Z. and Pourghiasian, M. and Benard, F. and Pan, J. and Lin, K. S. and Perrin, D. M.}
}
