Synthesis and Characterization of Rhenium and Technetium-99m Labeled Insulin Academic Article uri icon

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abstract

  • A (99m)Tc-labeled insulin analogue was synthesized through a direct labeling method in which the [(99m)Tc(CO)(3)](+) core was combined with a protected insulin derivative (9) bearing a M(I) chelate linked to the first amino acid of the B-chain (B1). Regioselective labeling was achieved by careful control over the pH and the reaction time. Following a TFA-anisole mediated deprotection step (decay-corrected yield of 30 +/- 11%, n = 4), the identity of the final (99m)Tc-labeled product was confirmed by HPLC. Displacement of (125)I-insulin from the insulin receptor (IR) by the Re analogue 6 was similar to that of native insulin (17.8 nM vs 11.7 nM, respectively). The extent of autophosphorylation and Akt activation, as indicated by production of phospho-Akt (pAkt), showed no statistical difference between 6 and native insulin in both assays. These results support the use of the reported (99m)Tc-insulin derivative as a tracer for studying insulin biochemistry in vivo.

authors

  • Sundararajan, Chitra
  • Besanger, Travis R
  • Labiris, Renee
  • Guenther, Katharina J
  • Strack, Thomas
  • Garafalo, Robert
  • Kawabata, Thomas T
  • Finco-Kent, Deborah
  • Zubieta, Jon
  • Babich, John W
  • Valliant, John F

publication date

  • March 25, 2010

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