High-affinity no-carrier-added 99mTc-labeled chemotactic peptides for studies of inflammation in vivo

Bioconjugate Chemistry
K E BaidooH N Wagner

Abstract

Nalpha-for-Nle-Leu-Phe-Nle-Tyr-Lys, a chemotactic peptide that binds with high affinity to the chemoattractant receptor on granulocytes and monocytes, was labeled with 99mTc using the diaminedithiol (DADT) chelating system to coordinate the Tc. 99mTc labeling of the DADT-coupled peptide was accomplished in 84% overall yield (room temperature for 10 min) using [99mTc]glucoheptonate as the donor of prereduced Tc. HPLC analysis showed two major 99mTc-labeled peptide peaks, 99mTc-DADT-Pep-I and 99mTc-DADT-Pep-II, were obtained in a ratio of 1:0.85. Using an iodoacetamide-derivatized gel to remove unlabeled peptide from the 99mTc labeling mixtures, essentially no-carrier-added (nca) high-specific activity 99mTc-labeled chemotactic peptides were obtained. The 99Tc analogues of the peptides were synthesized (72% yield) in a similar fashion and correlated with 99mTc complexes I and II by HPLC. In vitro competitive receptor binding assays of the isolated 99Tc analogues were performed against the tritiated chemotactic peptide [3H]N-for-Met-Leu-Phe ([3H]fMLF) using isolated granulocytes. The 99Tc-derivatized peptides showed similar binding affinities to the chemoattractant receptor as the unlabeled Nalpha-for-Nle-Leu-Phe-Nle-Tyr-Lys. The ...Continue Reading

References

Oct 5, 1989·The New England Journal of Medicine·R H RubinH W Strauss
Nov 1, 1985·Journal of Pharmacological Methods·G A McPherson
May 1, 1959·Archives of Biochemistry and Biophysics·G L ELLMAN

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Citations

Jun 6, 2000·Advanced Drug Delivery Reviews·J W Babich, A J Fischman
Jun 29, 2002·Nuclear Medicine and Biology·K VerbekeA Verbruggen
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Feb 18, 2006·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·Oscar R PozziMartín M Edreira

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