Synthesis, characterization and identification of the hexakis (trimethylphosphite) (Tc-99m)technetium(I) cation as a myocardial imaging agent
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-; TRN: 87-018928
- Journal Information:
- J. Nucl. Med.; (United States), Vol. 25:5; Conference: 31. annual meeting of the Society of Nuclear Medicine, Los Angeles, CA, USA, 5 Jun 1984
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
59 BASIC BIOLOGICAL SCIENCES
HEART
SCINTISCANNING
MYOCARDIUM
RADIOPHARMACEUTICALS
CHEMICAL PREPARATION
EVALUATION
UPTAKE
BIOCHEMICAL REACTION KINETICS
DOGS
INTRAVENOUS INJECTION
RATS
TECHNETIUM 99
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BODY
CARDIOVASCULAR SYSTEM
COUNTING TECHNIQUES
DIAGNOSTIC TECHNIQUES
DRUGS
HOURS LIVING RADIOISOTOPES
INJECTION
INTAKE
INTERMEDIATE MASS NUCLEI
ISOMERIC TRANSITION ISOTOPES
ISOTOPES
KINETICS
LABELLED COMPOUNDS
MAMMALS
MUSCLES
NUCLEI
ODD-EVEN NUCLEI
ORGANS
RADIOISOTOPE SCANNING
RADIOISOTOPES
REACTION KINETICS
RODENTS
SYNTHESIS
TECHNETIUM ISOTOPES
VERTEBRATES
YEARS LIVING RADIOISOTOPES
550601* - Medicine- Unsealed Radionuclides in Diagnostics
550201 - Biochemistry- Tracer Techniques