Synthesis of pyridyl derivatives for the future functionalization of biomolecules labeled with the fac-[188Re(CO)3(H2O)3]+ precursor

Jiaoyun Xia; Yongxian Wang; Gucai Li; Junfeng Yu; Duanzhi Yin

doi:10.1007/s10967-007-7145-8

Journal of Radioanalytical and Nuclear Chemistry

Volume/Issue:: Volume 279: Issue 1

Synthesis of pyridyl derivatives for the future functionalization of biomolecules labeled with the fac-[¹⁸⁸Re(CO)₃(H₂O)₃]⁺ precursor

Authors:

Jiaoyun Xia

Jiaoyun Xia Changsha University of Science and Technology College of Chemistry and Environmental Engineering No. 45 Chiling Road Changsha Hunan 410076 P.R. China

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Yongxian Wang

Yongxian Wang Chinese Academy of Sciences Radiopharmaceutical Centre, Shanghai Institute of Applied Physics No. 2019 Jialuo Road, Jiading Shanghai 201800 P.R. China

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Gucai Li

Gucai Li Hunan Institute of Engineering Department of Chemistry and Chemical Engineering No. 17 Shuyuan Road Xiangtan Huan 411101 P.R. China

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Junfeng Yu

Junfeng Yu Chinese Academy of Sciences Radiopharmaceutical Centre, Shanghai Institute of Applied Physics No. 2019 Jialuo Road, Jiading Shanghai 201800 P.R. China

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, and

Duanzhi Yin

Duanzhi Yin Chinese Academy of Sciences Radiopharmaceutical Centre, Shanghai Institute of Applied Physics No. 2019 Jialuo Road, Jiading Shanghai 201800 P.R. China

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Pages:: 245–252

Online Publication Date:: 21 Jul 2008

Publication Date:: 01 Jan 2009

Article Category:: Research Article

DOI:: https://doi.org/10.1007/s10967-007-7145-8

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Abstract

In this paper, we investigated three ligand systems, symmetric and asymmetric pyridyl-containing tridentate ligands (L¹NH₂ = (bis(2-pyridylmethyl)-amino)-ethylamine, L²H = (bis(2-pyridylmethyl)-amino)-acetic acid, L³NH₂ = [(6-amino-hexyl)-pyridyl-2-methyl-amino]-acetic acid) as bifunctional chelating agents for labeling biomolecules. These ligands reacted with the precursor fac-[¹⁸⁸Re(CO)₃(H₂O)₃]⁺ and yielded the radioactive complexes fac-[¹⁸⁸Re(CO)₃L] (L = three ligands), which were identified by RP-HPLC. The corresponding stable rhenium tricarbonyl complexes (1–3) were allowed for macroscopic identification of the radiochemical compounds. ¹⁸⁸Re tricarbonyl complexes, with log P_o/w values ranging from −1.36 to −0.32, were obtained with yields of ≥90% using ligand concentrations within the 10⁻⁶−10⁻⁴M range. Challenge studies with cysteine and histidine revealed the high stability properties of these radioactive complexes, and biodistribution studies in normal mice indicated a fast rate of blood clearance and high rate of total radioactivity excretion, primarily through the renal-urinary pathway. In summary, these asymmetric and symmetric pyridyl-containing tridentate ligands are potent bifunctional chelators for the future biomolecules labeling of fac-[¹⁸⁸Re(CO)₃(H₂O)₃]⁺.

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Journal of Radioanalytical and Nuclear Chemistry

Print ISSN:: 0236-5731

Online ISSN:: 1588-2780

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Journal of Radionalytical and Nuclear Chemistry
Language	English
Size	A4
Year of Foundation	1968
Volumes per Year	1
Issues per Year	12
Founder	Akadémiai Kiadó
Founder's Address	H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
Publisher	Akadémiai Kiadó Springer Nature Switzerland AG
Publisher's Address	H-1117 Budapest, Hungary 1516 Budapest, PO Box 245. CH-6330 Cham, Switzerland Gewerbestrasse 11.
Responsible Publisher	Chief Executive Officer, Akadémiai Kiadó
ISSN	0236-5731 (Print)
ISSN	1588-2780 (Online)