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Review
. 2010 May 12;110(5):2858-902.
doi: 10.1021/cr900325h.

Coordinating radiometals of copper, gallium, indium, yttrium, and zirconium for PET and SPECT imaging of disease

Thaddeus J Wadas  1 , Edward H Wong, Gary R Weisman, Carolyn J Anderson
Affiliations
Review

Coordinating radiometals of copper, gallium, indium, yttrium, and zirconium for PET and SPECT imaging of disease

Thaddeus J Wadas et al. Chem Rev. .
No abstract available

PubMed Disclaimer

Figures

Figure 1
Figure 1
Cartoon depicting the fundamental principle of Positron Emission Tomography (PET). As the targeting group interacts with the cell surface receptor, the positron emitting radio-metal decays by ejecting β+ particles from its nucleus. After traveling a short distance in the electron rich tissue, the positron recombines with an electron in a process called annihilation. During annihilation, the mass of the positron and electron are converted into two high energy photons (511 keV gamma rays), which are released approximately 180° apart to ensure that energy and momentum are conserved. Although attenuation is possible, these two gamma rays are usually energetic enough to escape the organism and be collected by the detectors of a PET scanner.
Figure 2
Figure 2
Selected acyclic chelators
Figure 3
Figure 3
Selected macrocyclic chelators
Figure 4
Figure 4
Cu-L6
Figure 5
Figure 5
Cu-GTS (L7)
Figure 6
Figure 6
Cu-PTSM (L8)
Figure 7
Figure 7
Cu-EDTA (L10)
Figure 8
Figure 8
Cu-DTPA (L12)
Figure 9
Figure 9
Cu-L17
Figure 10
Figure 10
Cu-L18
Figure 11
Figure 11
Cu-TACHPYR (L19)
Figure 12
Figure 12
Cu-NO2A (L28)
Figure 13
Figure 13
Cu-NOTA (L29)
Figure 14
Figure 14
Cu-NOTAM (L30)
Figure 15
Figure 15
Cu-L33
Figure 16
Figure 16
Cu-L35
Figure 17
Figure 17
Cu-DOTA (L39)
Figure 18
Figure 18
Cu-CB-DO2A (L37)
Figure 19
Figure 19
Cu-TE1A (L50)
Figure 20
Figure 20
Cu-L51
Figure 21
Figure 21
Cu-L52
Figure 22
Figure 22
Cu-H2TETA (L49)
Figure 23
Figure 23
Cu-L55
Figure 24
Figure 24
Cu-CB-TE2A (L57)
Figure 25
Figure 25
Cu-CB-TEAMA (L58)
Figure 26
Figure 26
Cu-TE2P (L54)
Figure 27
Figure 27
Cu-L62
Figure 28
Figure 28
Cu-L63
Figure 29
Figure 29
Cu-L64
Figure 30
Figure 30
Ga-L1
Figure 31
Figure 31
Ga-L2
Figure 32
Figure 32
Ga-BAT-TM (L4)
Figure 33
Figure 33
Ga-EC (L5)
Figure 34
Figure 34
Ga-EDTA (L10)
Figure 35
Figure 35
Ga-BAPEN (L16)
Figure 36
Figure 36
Ga-NOTA (L29)
Figure 37
Figure 37
Ga-TACN-TM (L27)
Figure 38
Figure 38
Ga-DOTA (L39)
Figure 39
Figure 39
Ga-DOTA-D-PheNH2 (L40)
Figure 40
Figure 40
Ga-DO3A-TPP (L44)
Figure 41
Figure 41
Ga-CB-DO2A (L37)
Figure 42
Figure 42
Ga-CB-TE2A (L57)
Figure 43
Figure 43
Ga-tris(benzohydroxamate)
Figure 44
Figure 44
InCl-BAT-TM (L4)
Figure 45
Figure 45
In-L2•DMF
Figure 46
Figure 46
In-EC (L5)
Figure 47
Figure 47
In-EDTA (L9)
Figure 48
Figure 48
In-DTPA (L12)
Figure 49
Figure 49
In-DTPA-BA2 (L13)
Figure 50
Figure 50
InCl-HNOTA (L29)
Figure 51
Figure 51
In-TACN (L26)-tris(2′-methylcarboxylmethyl)
Figure 52
Figure 52
In-TACN-TM (L27)
Figure 53
Figure 53
In-DOTA-AA (L41)
Figure 54
Figure 54
In-DOTA-TPP (L44)
Figure 55
Figure 55
In-TE3A (L53)
Figure 56
Figure 56
YF2-EDTA (L10)
Figure 57
Figure 57
Y-DTPA (L12)
Figure 58
Figure 58
Y-DTPA-BA2 (L13)
Figure 59
Figure 59
Y(triflate)2-NOTAM (L30)
Figure 60
Figure 60
[Y-DOTA]− (L39)
Figure 61
Figure 61
Y-DOTA-D-Phe-NH2 (L40)
Figure 62
Figure 62
Y-DO3AP (L42)
Figure 63
Figure 63
Zr-EDTA (L10)
Figure 64
Figure 64
Zr-DTPA (L12)
Figure 65
Figure 65
Selected RGD analogues used in αvβ3 targeting radiopharmaceuticals.
Figure 66
Figure 66
Small-animal PET/CT of PTH-treated mice. Calvarium uptake of 64Cu-CB-TE2A-c(RGDyK) was higher in PTH-treated mice (7.4 MBq [199 mCi],115 ng, SUV 0.53) than in control mice (7.7 MBq [209 mCi], 121 ng, SUV 0.22) (50- to 60-min summed dynamic image). (A) In PTH-treated mice, uptake was reduced in all tissues, including calvarium, after injection of c(RGDyK) (PTH[left]: 159 mCi, 84 ng, SUV 5 0.33; block [right]: 164 mCi, 87 ng, SUV 5 0.18) (static image obtained 60 min after injection, 10-minscan). (B) Arrowheads indicate calvarium of each animal. Fiducials (*) are indicated. Reprinted with permission from reference . Copyright 2007 Society of Nuclear Medicine.
Figure 67
Figure 67
Selected somatostatin analogues used in somatostatin receptor targeting radiopharmaceuticals.
Figure 68
Figure 68
(A) Representative small animal PET image at 4 h of rat injected with 64Cu-CB-TE2A-sst2-ANT. Left image is representative slice from small-animal PET/CT fusion image and right image is small-animal PET projection view of same animal. Calculated SUV for the tumor in left hind limb was determined to be 2.7 and SUV for tumor in right hind limb was determined to be 2.8. (B) Representative small-animal PET image at 4 h of rat injected with 64Cu-CB-TE2Asst2-ANT and sst2-ANT as blocking agent. Left image is representative slice from small-animal PET/CT fusion image and right image is small-animal PET projection view of same animal. In animal receiving blockade, SUV for tumor in left hind limb was calculated to be 0.74 and SUV for tumor in right hind limb was calculated to be 0.51. (C) Graphical plot of change in average SUV over time. Even after 24 h, SUV remains high, suggesting enhanced binding of 64Cu-CB-TE2A-sst2-ANT for SST2 receptor. (D) Graphical representation that demonstrates change in observed SUV when excess cold sst2-ANT is coinjected with radiopharmaceutical, indicating that binding of radiopharmaceutical to SSTR-positive tumor is receptor-mediated. Reprinted with permission from reference . Copyright 2008 Society of Nuclear Medicine.
Figure 69
Figure 69
Selected bombesin analogues used in targeting the GRP receptor.
Figure 70
Figure 70
Coronal CT image (A) with clear subcutaneous localization of SKOV-3 tumor (arrow). Fusion of microPET and CT images (B) (168 h after injection) enables adequate quantitative measurement of 89Zr-bevacizumab in the tumor. Reprinted with permission from reference . Copyright 2007 Society of Nuclear Medicine.
Figure 71
Figure 71
Selected α-MSH analogues that target the melanocortin-1 (MC-1) receptor.
Figure 72
Figure 72
Whole-body SPECT/CT, PET/CT and PET images of B16 melanoma tumor-bearing C57 mice 2 h post tail vein injection of radiolabeled CHX-A”-Re(Arg11)CCMSH. (A) SPECT/CT images of tumor-bearing mice injected intravenously with 12.95 MBq (350 μCi) of 111In-CHX-A”-Re(Arg11)CCMSH with (blocked) or without (nonblocked) a 20-μg nonradiolabeled peptide block. PET/CT and PET imaging of melanoma-bearing mice 2 h post tail vein injection of (B) 4.44 MBq (120 μCi) of 86Y-CHX-A”-Re(Arg11)CCMSH with a 20-μg NDP block (blocked) and without block (nonblocked) or (C) 3.7 MBq (100 μCi) of 68Ga-CHX-A”-Re(Arg11)CCMSH with (blocked) and without (nonblocked) a 60-μg NDP block, respectively. Tumor (T), kidney (K) and (BL) bladder locations are highlighted for each mouse. Reprinted with permission from reference . Copyright 2009 Elsevier Limited.
Figure 73
Figure 73
The synthetic antagonist DPC11870 targets the leukotriene B4 (LTB4) receptor.
See this image and copyright information in PMC

References

    1. Society of Nuclear Medicine 2009. http://interactive.snm.org/index.cfm?PageID=5571&RPID=969.
    1. Welch MJ, Redvanly CS, editors. Handbook of Radiopharmaceuticals: Radiochemistry and Applications. John Wiley & Sons Inc.; Hoboken, NJ: 2003.
    1. Blower PJ, Lewis JS, Zweit J. Nucl. Med. Biol. 1996;23(8):957. - PubMed
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