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Synthesis, characterization and identification of the hexakis (trimethylphosphite) (Tc-99m)technetium(I) cation as a myocardial imaging agent

Conference · · J. Nucl. Med.; (United States)
OSTI ID:6861670

Hexakis(trimethylphosphite)(Tc-99m)technetium(I), a monocationic complex, was synthesized for evaluation as a myocardial imaging agent. The above product was synthesized by reacting a methanolic solution of NaTcO/sub 4/ with trimethyl phosphite in an inert atmosphere at 100/sup 0/ for 30 min. Using the Tc-99 isotope, mg quantities were isolated for full characterization by precipitation from the reaction mixture using sodium tetraphenylborate. Recrystallization from methanol gave crystals of the tetraphenylborate salt. Elemental analyses, Tc-99 and P-31 NMR, mass spectra, X-ray photoelectron spectra, ir and X-ray crystal structure were all consistent with a hexacoordinate octahedral structure of the proposed monocation. The products formed from the Tc-99 isotope and the Tc-99m isotope were shown to be identical by HPLC using simultaneous radiometric and UV detection. The myocardial imaging properties of the title compound were evaluated by rat biodistribution and dog imaging. Five minutes after intravenous administration in rats, 3% dose/gm was in the heart with tissue ratios of heart/blood of 30, heart/liver of 4, heart/lung of 2. These compare to T1-201 values of 6% dose/gm in the heart with tissue ratios of heart/blood of 24, heart/liver of 6, heart/lung of 1. Imaging in an anesthetized dog revealed excellent myocardial uptake with persistent images through a 60 minute period. From these data the hexakis(trimethylphosphite)(Tc-99m)technetium(I) cation was identified as a myocardial imaging agent suitable for further evaluation.

Research Organization:
Mallinckrodt, Inc., St. Louis, MO
OSTI ID:
6861670
Report Number(s):
CONF-840619-
Journal Information:
J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 25:5; ISSN JNMEA
Country of Publication:
United States
Language:
English