@article { ISI:000414990400018,
	title = {Octadentate Picolinic Acid-Based Bispidine Ligand for Radiometal Ions},
	journal = {Chem. Eur. J.},
	volume = {23},
	number = {63},
	year = {2017},
	month = {NOV 13},
	pages = {15945-15956},
	abstract = {<p>The synthesis of the octadentate bispidine ligand bearing two picolinic acid pendant arms (H(2)bispa(2)), and its coordination chemistry with radionuclides relevant for nuclear medicine, namely indium(III) (In-111), lutetium(III) (Lu-177), and lanthanum(III) (as surrogate for Ac-225), are reported. The non-radioactive metal complexes of the N6O2-type bispa ligand were characterized by H-1 and (CNMR)-C-13 spectroscopy, elemental analysis, mass spectrometry and single-crystal X-ray analysis. Experimental structural data, computational analysis, complex stabilities determined by potentiometric titration, and {\textquoteleft}{\textquoteleft}radiostabilities{\&$\#$39;\&$\#$39;} determined by competition studies in the presence of human serum reveal complex stabilities of H(2)bispa(2) comparable to those of the macrocyclic {\textquoteleft}{\textquoteleft}gold standard{\&$\#$39;\&$\#$39;} DOTA. After an incubation time of 1day, 86 and 87\% of {[}Lu-177(bispa(2))](+) and {[}Lu-177(DOTA)](-), respectively, remain intact. Importantly, unlike DOTA, H(2)bispa(2) is radiolabeled quantitatively with In-111(III) and Ac-225(III) under ambient conditions, which is an essential aspect when working with heat-sensitive antibodies as targeting vectors. In the case of In-111(III), room temperature radiolabeling of H(2)bispa(2) yields molar activities as high as 70 MBq nmol(-1) within 10 minutes. These are promising results for radiopharmaceutical applications of H(2)bispa(2).</p>},
	issn = {0947-6539},
	doi = {10.1002/chem.201702284},
	author = {Comba, Peter and Jermilova, Una and Orvig, Chris and Patrick, Brian O. and Ramogida, Caterina F. and Rueck, Katharina and Schneider, Christina and Starke, Miriam}
}
