Heteronuclear Gd-(99m)Tc Complex of DTPA-Bis(histidylamide) Conjugate as a Bimodal MR/SPECT Imaging Probe

ACS Med Chem Lett. 2012 Feb 27;3(4):299-302. doi: 10.1021/ml200285p. eCollection 2012 Apr 12.

Abstract

The work describes the synthesis and in vivo application of heterotrimetallic complexes of the type {Gd(H2O)[(M(H2O)(CO)3)2(1)]} {1 = DTPA-bis(histidyl-amide); M = Re (3a); (99m)Tc (3b)} for dual modality MR/SPECT imaging. Here, the DTPA-bis(histidylamide) conjugate functions as a trinucleating chelate incorporating Gd in the DTPA core with Re or (99m)Tc in the pair of histidylamide side arms. The two complexes are chemically equivalent as revealed by HPLC, and their "cocktail mixture" (3a + 3b) has demonstrated itself to be essentially a single bimodal imaging probe. The present system has thus overcome the sensitivity difference problem between MRI and SPECT and paved the way for practical applications.

Keywords: MR/SPECT; cocktail mixture; dual modality; heterotrimetallic Gd-[99mTc]2/[Re]2 complexes; imaging probe.