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Design and development of 6-hydrazinonicotinyl-fatty acid-mimetic 99mTc-complex as a potential myocardial imaging agent
González, Joel; García, María Fernanda; Cabral, Pablo; Calzada, Victoria; Cerecetto, Hugo.
Afiliação
  • González, Joel; Universidad de la República. Centro de Investigaciones Nucleares, Facultad de Ciencias. Área de Radiofarmacia. UY
  • García, María Fernanda; Universidad de la República. Centro de Investigaciones Nucleares, Facultad de Ciencias. Área de Radiofarmacia. UY
  • Cabral, Pablo; Universidad de la República. Centro de Investigaciones Nucleares, Facultad de Ciencias. Área de Radiofarmacia. UY
  • Calzada, Victoria; Universidad de la República. Centro de Investigaciones Nucleares, Facultad de Ciencias. Área de Radiofarmacia. UY
  • Cerecetto, Hugo; Universidad de la República. Centro de Investigaciones Nucleares, Facultad de Ciencias. Área de Radiofarmacia. UY
Braz. J. Pharm. Sci. (Online) ; 60: e23542, 2024. tab, graf
Article em En | LILACS | ID: biblio-1533991
Biblioteca responsável: BR40.1
Localização: BR40.1
ABSTRACT
Abstract The goal of this work is to identify new fatty acid-mimetic 99mTc-complexes to be used as myocardial imaging agents that allow studying heart abnormalities in high-risk patients. In this sense, we designed a fatty acid-mimetic substructure including an amide moiety that, among other properties, could improve myocardial residence time. A diamide with a chain length of 15 atoms and porting a 6-hydrazinonicotinyl (HYNIC) chelator, and an analog with a short carbon-chain, were prepared with convergent organic synthetic procedures and radiolabeled with 99mTc using tricine as the sole coligand. The in vivo proofs of concept were performed using healthy mice. The new 99mTc-complexes were obtained with adequate radiochemical purity. The lipophilicities were in agreement with the length of the chains. While both 99mTc-complexes showed uptake in the myocardial muscle, the designed radiopharmaceutical with the longest chain length had preferential target-uptake and target-retention compared to other complexes described in the bibliography. Further studies, involving imaging assays, synthetic modifications, and assay of new coligands for 99mTc-HYNIC complexes, are currently ongoing.
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Texto completo: 1 Índice: LILACS Assunto principal: Compostos Radiofarmacêuticos / Ácidos Graxos / Amidas Limite: Animals Idioma: En Revista: Braz. J. Pharm. Sci. (Online) Assunto da revista: Farmacologia / Terapˆutica / Toxicologia Ano de publicação: 2024 Tipo de documento: Article

Texto completo: 1 Índice: LILACS Assunto principal: Compostos Radiofarmacêuticos / Ácidos Graxos / Amidas Limite: Animals Idioma: En Revista: Braz. J. Pharm. Sci. (Online) Assunto da revista: Farmacologia / Terapˆutica / Toxicologia Ano de publicação: 2024 Tipo de documento: Article