Technetium-1,2-dihydroxy-1,2-bis(dihydroxyphospinyl)ethane (99mTc-DHPE). A promising new skeletal imaging agent

Abstract

99mTc-sodium pertechnetate was reduced and complexed with 1,2-dihydroxy-1,2-bis(dihydroxyphosphinyl)ethane (DHPE) with a yield higher than 95%. When administered to rats, 99mTc-DHPE demonstrated very good skeletal uptake, a high clearance from blood to the bones a low concentration in muscles and other organs, satisfactory biological stability and a clearance mainly through the kidneys. The biodistribution of 99mTc-DHPE in rats compared to that of 99mTc-methylenediphosphonate (99mTc-MDP) at 2 and 24 h post injection, showed higher skeletal uptake, substantially higher blood clearance, but also higher concentration in muscles which, however, caused no significant degradation in image quality. These characteristics suggest that 99mTc-DHPE is a promising new skeletal imaging agent.

Substituent Effect on the Structure and Biological Property of99mTc-Labeled Diphosphonates: Theoretical Studies

“…In a continuing effort to find better bone-imaging agents, in the present work molecular modeling was performed to investigate the effect of tether between two phosphates on the geometric and electronic structures as well as the biological behavior of 99m Tc-labled diphosphonate complexes, such as 99m Tc-labeled 1,2-dihydroxy-1,2-bis(dihydroxyphosphonyl)ethane (DHPE), 12 2,3-dihydroxy-2,3-bis(dihydroxyphosphonyl) butane (DHPB), 13 and 2,4-dihydroxy-2,4-bis-(dihydroxyphosphonyl)pentane (DHPP). 13 These compounds can be viewed as longer-chain analogues of MDP with the backbone P-C n -P (see Table 1).…”