Publications [#65219] of Michael R. Zalutsky

Papers Published

1. Vaidyanathan, Ganesan and Zalutsky, Michael R., No-carrier-added synthesis of meta-[¹³¹I]iodobenzylguanidine, Applied Radiation and Isotopes, vol. 44 no. 3 (1993), pp. 621 - 628 [0969-8043(93)90179-E]
   (last updated on 2007/04/15)

   Abstract:
   No-carrier-added meta-[¹³¹I]iodobenzylguanidine ([¹³¹I]MIBG) was prepared starting with two different metallated precursors. Attempted preparation of 3-(tri-n-butylstannyl)benzylguanidine was not successful. An alternate two-step strategy using 3-(tri-n-butylstannyl)benzylamine could be used to prepare radioiodinated [¹³¹I]MIBG in an overall radiochemical yield of 30-33%. Synthesis of [¹³¹I]MIBG via the radioiododesilylation of 3-trimethylsilylbenzylguanidine was also investigated. Yields were dependent on temperature, precursor concentration, solvent and nature of the oxidant. Radiochemical yields of 90% were obtained in 5 min at room temperature using either N-chlorosuccinimide or hydrogen peroxide in trifluoroacetic acid as oxidants. The percentage of specific binding in vitro of no-carrier-added MIBG to SK-N-SH neuroblastoma cells remained constant over a 2 log activity range, while the binding of MIBG prepared by isotopic exchange dropped by a factor of seven. In normal mice, heart and adrenal uptake of no-carrier-added [¹³¹I]MIBG was found to be higher than that of [¹³¹I]MIBG prepared by isotopic exchange.

   Keywords:
   Synthesis (chemical);Organometallics;Tin compounds;Radiation chemistry;Radioactive tracers;Radiotherapy;Oncology;Iodine compounds;Radioisotopes;