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Synthesis and liposome encapsulation of a novel 18 F‐conjugate of ω ‐conotoxin GVIA for the potential imaging of N ‐type Ca 2+ channels in the brain by positron emission tomography
Author(s) -
Azarian Vahe,
Gangloff Anne,
Seimbille Yann,
Delaloye Sibylle,
Czernin Johannes,
Phelps Michael E.,
Silverman Daniel H.S.
Publication year - 2006
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1029
Subject(s) - chemistry , conjugate , liposome , specific activity , in vivo , radiochemistry , stereochemistry , biochemistry , enzyme , mathematical analysis , mathematics , microbiology and biotechnology , biology
ω ‐Conotoxin GVIA is a potent, irreversible antagonist of N ‐type voltage gated Ca 2+ channels. A radiofluorinated analogue of GVIA could be useful in assessing regional synaptic density of the brain, in vivo , using positron emission tomography. N ‐hydroxy succinimidyl 4‐[ 18 F]fluorobenzoate was employed to site‐specifically label GVIA, preserving native binding affinity. The tracer was characterized with MALDI‐TOF mass spectrometry and colorimetric protein assay. Radiochemical decay‐corrected yield of the lysine‐24 labeled analogue of [ 18 F]GVIA was 5%. Specific activity of this species was determined to be 1.2 × 10 5 Ci/mmol. Encapsulation of the tracer in sulfatide containing liposomes, a potential method for enhancing blood–brain penetrance, was accomplished with 40% efficiency. Copyright © 2006 John Wiley & Sons, Ltd.