Paik, Chang H.; Quadri, Syed M.; Reba, Richard C. published the article 《Interposition of different chemical linkages between antibody and 111In-DTPA to accelerate clearance from non-target organs and blood》. Keywords: indium 111 DTPA antibody linkage biodistribution.They researched the compound: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate( cas:70539-42-3 ).Computed Properties of C18H20N2O12. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:70539-42-3) here.
Two chem. labile linkages, disulfide and diester, and 2 stable linkages, thioether and hydrocarbon, were introduced between antibody and 111In-DTPA in order to modify their biodistributions. The biodistributions of the new linkages were evaluated in rats with target antigens localized in lungs. For comparison purpose, the antibody-DTPA conjugate with a peptide linkage was used as a control conjugate. The antibody conjugates with the stable linkages produced a biodistribution similar to that of the peptide-linked conjugate during a 48 h period. The disulfide and diester conjugates, however, cleared from blood much faster and were retained in normal organs much less than the peptide conjugate. The disulfide and the diester conjugate amplified the lung (target) to blood ratio by 15- and 6-fold, resp., at 48 h, as compared to the corresponding target to blood ratio of the control conjugate. Compared to the control conjugate, a 3-fold higher target to liver ratio was also obtained by the disulfide conjugate and a 4-fold higher target to kidney ratio was obtained by the diester conjugate at 48 h.
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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem