| 摘要 |
Tracers that can be used for PET or SPECT imaging of the distribution of Pgp are disclosed. The tracers are metalloprobes that can comprise a radioactive metal ion such as 67Ga or 68Ga. Methods of synthesizing the tracers, and methods of imaging heart and other tissues are also disclosed. The tracers can be used to obtain high signal-to-background ratios for imaging tissues in vivo such as heart or tumor tissue. In various embodiments, disclosed tracers can exhibit, a) enhanced first pass extraction into heart tissue compared to presently available probes, b) linearity with true blood flow, c) enhanced detection of myocardial viability compared to presently available probes, d) reduced liver retention compared to presently available probes, and e) more efficient clearance from non-cardiac and adjoining tissues compared to presently available probes. |
| 主权项 |
1. A compound, chelate, complex or salt thereof comprising a structure selected from the group consisting ofwherein each of R1, R2, R7 and R8 is independently selected from the group consisting of H, C1-C6 linear alkyl, C3-C6 branched chain alkyl, C3-C6 cycloalkyl, C1-C6 linear alkoxy, C3-C6 branched chain alkoxy and C3-C6 cycloalkoxy; each of R3, R4, R5 and R6 is independently selected from the group consisting of H, C1-C6 linear alkoxy, C3-C6 branched chain alkoxy, C3-C6 cycloalkoxy, C1-C6 linear haloalkoxy, C3-C6 branched chain haloalkoxy, C3-C6 cyclohaloalkoxy, C1-C6 linear hydroxyalkoxy, C3-C6 branched chain hydroxyalkoxy, C3-C6 cyclohydroxyalkoxy, alkoxymethyl, alkoxyethyl, alkoxyalkoxymethyl, alkoxyalkoxyethyl, benzyl, alkoxybenzyl, napthyl and alkoxynaphthyl; and R9 is selected from the group consisting of H, methylene, carbonyl, sulfur, C1-C8 linear alkyl, C3-C8 branched chain alkyl, C3-C8 cycloalkyl, C1-C8 linear alkoxy, C3-C8 branched chain alkoxy and C3-C8 cycloalkoxy, with a proviso that at least one of R3, R4, R5 and R6 is not H. |
