TY - JOUR
T1 - Synthesis and evaluation of a new class of technetium-99m monocationic radiotracers from dithienyldiazalkanes
AU - Goomer, N. C.
AU - Kulkarni, P. V.
AU - Constantinescu, A.
AU - Antich, P.
AU - Parkey, R. W.
AU - Corbett, J. R.
N1 - Funding Information:
Acknow[ed~e~enrs-Dr. Goomer extends thanks to Sh. C. N. Desai, Senior Executive, and Sh. R. G. Deshpande, Chief Executive, of the Board of Radiation and Isotopes Technology, Bombay, India for their interest, support and encouragement. Award of a Fellowship from the Department of Radiology, U.T. Southwestern Medical Center, Dallas, Tex., U.S.A. is gratefully acknowledged. Thanks are due to Cathy Starnes for meticulous typing of the manuscript.
PY - 1994/5
Y1 - 1994/5
N2 - 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.
AB - 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.
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U2 - 10.1016/0969-8051(94)90032-9
DO - 10.1016/0969-8051(94)90032-9
M3 - Article
C2 - 9234324
AN - SCOPUS:0028240743
SN - 0969-8051
VL - 21
SP - 657
EP - 662
JO - International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology
JF - International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology
IS - 4
ER -