Synthesis and evaluation of a new class of technetium-99m monocationic radiotracers from dithienyldiazalkanes

N. C. Goomer, P. V. Kulkarni, A. Constantinescu, P. Antich, R. W. Parkey, J. R. Corbett

Research output: Contribution to journalArticle

2 Scopus citations

Abstract

Monocationic 99mTc complexes, [99mTcO2(THEN)]+ and [99mTcO2(THPN)]+ derived from a new class of N2S2 chelators diethienyldiazalkanes, namely 1,6-di(2-thienyl)-2,5-diazahexane (THEN) and 1 7-di-(2-thienyl)-4,4-dimethyl-2,6-diazaheptane (THPN), have been synthesized using Sn(II) tartrate reduction of [99mTc]pertechnetate at pH 9 and extraction of the complexes as ion pairs with trifluoromethane sulfonate anion (CF3SO3-) in high radiochemical yield (~90%). Radiochemical analysis of the 99mTc complexes using chromatography (Whatman Cellulose CEL300 DEAE anion exchange strip, MEK) and paper chromatography (Whatman I, acetone) revealed high radiochemical purity (>90%). High octanol-saline partition coefficients (>37) of [99mTcO2THEN)]+ and [99mTcO2(THPN)]+ indicated a lipophilic nature of the complexes. Relative stability of the 99mTc complex was high as measured by DTPA challenge studies. Biodistribution of [99mTcO2(THEN)]+ and [99mTcO2(THPN)]+ in rats at 15 min post-injection showed heart-to-blood activity ratios of 0.26 and 0.46, respectively, with rapid blood clearance. Further studies involving the variation of substituents on the basic core structure of this new class of 99mTc complexes may provide radiotracers suitable for myocardial imaging.

Original languageEnglish (US)
Pages (from-to)657-662
Number of pages6
JournalNuclear Medicine and Biology
Volume21
Issue number4
DOIs
StatePublished - May 1994

ASJC Scopus subject areas

  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging
  • Cancer Research

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    Goomer, N. C., Kulkarni, P. V., Constantinescu, A., Antich, P., Parkey, R. W., & Corbett, J. R. (1994). Synthesis and evaluation of a new class of technetium-99m monocationic radiotracers from dithienyldiazalkanes. Nuclear Medicine and Biology, 21(4), 657-662. https://doi.org/10.1016/0969-8051(94)90032-9