H4octapa: an acyclic chelator for 111In radiopharmaceuticals

…, CL Ferreira, E Boros, MJ Adam, C Orvig

Index: Price, Eric W.; Cawthray, Jacqueline F.; Bailey, Gwendolyn A.; Ferreira, Cara L.; Boros, Eszter; Adam, Michael J.; Orvig, Chris Journal of the American Chemical Society, 2012 , vol. 134, # 20 p. 8670 - 8683

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Citation Number: 24

Abstract

This preliminary investigation of the octadentate acyclic chelator H4octapa (N4O4) with 111In/115In3+ has demonstrated it to be an improvement on the shortcomings of the current industry “gold standards” DOTA (N4O4) and DTPA (N3O5). The ability of H4octapa to radiolabel quantitatively 111InCl3 at ambient temperature in 10 min with specific activities as high as 2.3 mCi/nmol (97.5% radiochemical yield) is presented. In vitro mouse serum ...