Development of nonreducible technetium-99m(III) cations as myocardial perfusion imaging agents: initial experience in humans

Journal Article · Tue Dec 01 04:00:00 EST 1987 · J. Nucl. Med.; (United States)

OSTI ID:5606128

Deutsch, E; Vanderheyden, J L; Gerundini, P; Libson, K; Hirth, W; Colombo, F; Savi, A; Fazio, F

A series of 15 nonreducible technetium-99m (III) complexes of formula tr-(/sup 99m/TcL(Y)2)+ has been prepared by a general synthetic route based on reductive addition of Y to the technetium-99m (/sup 99m/Tc) intermediate (/sup 99m/TcL(O))+. In these complexes, selected for potential use as myocardial imaging agents, L represents one of the two tetradentate Schiff base ligands N,N'-ethylenebis(acetylacetone iminato), (en), or N,N'-propylene-1,2-bis(acetylacetone iminato), (pn), while Y represents a monodentate phosphine, phosphite or isonitrile ligand as exemplified by P(CH3)3, P(OCH3)3 and CN-C(CH3)3. Of these 15 complexes, several with octanol/saline partition coefficients in the range 0.04-20 exhibit significant myocardial uptake in rats and dogs. Of these, none exhibit detectable myocardial washout, providing strong support for the hypothesis that myocardial washout occurs only for those /sup 99m/Tc(III) cations that undergo in vivo reduction to the neutral /sup 99m/Tc(II) form. Evaluation of the prototypical complex tr-(/sup 99m/Tc(en)(P(CH3)3)2)+ in seven normal volunteers and patients establishes that it is only a mediocre myocardial imaging agent in man.

• Research Organization: Univ. of Cincinnati, OH
• OSTI ID: 5606128
• Journal Information: J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 28:12; ISSN JNMEA
• Country of Publication: United States
• Language: English

Related Subjects

550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BODY
CARDIOVASCULAR SYSTEM
CATIONS
CHARGED PARTICLES
CHEMICAL PREPARATION
COMPLEXES
DISTRIBUTION
DOGS
DRUGS
EVALUATION
HEART
HOURS LIVING RADIOISOTOPES
IMINES
INTERMEDIATE MASS NUCLEI
IONS
ISOMERIC NUCLEI
ISOMERIC TRANSITION ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PERFUSED ORGANS
RADIOISOTOPES
RADIOPHARMACEUTICALS
RATS
RODENTS
SYNTHESIS
TECHNETIUM 99
TECHNETIUM ISOTOPES
TISSUE DISTRIBUTION
VERTEBRATES
YEARS LIVING RADIOISOTOPES