Publications [#65254] of Michael R. Zalutsky

Papers Published

1. Vaidyanathan, G. and Affleck, D.J. and Zalutsky, M.R., No-carrier-added synthesis of a 4-methyl-substituted meta-iodobenzylguanidine analogue, Appl. Radiat. Isot. (UK), vol. 62 no. 3 (2005), pp. 435 - 40 [001]
   (last updated on 2007/04/15)

   Abstract:
   Radioiodinated meta-iodobenzylguanidine (MIBG) is used in the diagnosis and therapy of various neuroendocrine tumors. As a part of our efforts to develop an MIBG analogue with improved characteristics for these applications, a synthesis of 3-[¹³¹I]iodo-4-methylbenzylguanidine ([¹³¹I]MeIBG) was developed. Unlabeled MeIBG and the tin precursor, N,N'-(bis-tert-butyloxycarbonyl)-N-(4-methyl-3trimethylstannylbenzyl) guanidine were synthesized in two steps from 3-iodo-4-methylbenzylalcohol. Radioiodinated MeIBG was synthesized at a no-carrier-added level by the iododestannylation of the tin precursor in about 85% radiochemical yield. The accumulation of [¹³¹I]MeIBG (38.9±3.0% of input counts) by human neuroblastoma SK-N-SH cells in vitro was 87% that of [¹²⁵I]MIBG (44.5±3.0%) and a number of Uptake-1 inhibiting conditions reduced the uptake of both tracers in this cell line to a similar degree suggesting that introduction of a methyl substituent at the 4-position of MIBG did not adversely affect its biological characteristics. [All rights reserved Elsevier]

   Keywords:
   cellular biophysics;chemical reactions;iodine compounds;organic compounds;patient diagnosis;radiation therapy;radiochemistry;tin compounds;tumours;