Development and evaluation of a
Animals
Breast Neoplasms
/ diagnostic imaging
Drug Stability
Estradiol
/ analogs & derivatives
Female
Humans
MCF-7 Cells
Mice
Mice, Nude
Neoplasm Transplantation
Organotechnetium Compounds
/ chemical synthesis
Protein Binding
Radiopharmaceuticals
/ chemical synthesis
Rats
Rats, Wistar
Receptors, Estrogen
/ metabolism
Tissue Distribution
Estrogen receptors
Nitrido complexes
Radiopharmaceuticals
Technetium
Journal
Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine
ISSN: 1872-9800
Titre abrégé: Appl Radiat Isot
Pays: England
ID NLM: 9306253
Informations de publication
Date de publication:
Dec 2019
Dec 2019
Historique:
received:
29
05
2019
revised:
02
08
2019
accepted:
11
08
2019
pubmed:
24
8
2019
medline:
3
4
2020
entrez:
24
8
2019
Statut:
ppublish
Résumé
Estrogen receptors are overexpressed in 70% of breast cancer and identification of their presence is important to select the appropriate treatment. This work proposes the preparation and evaluation of an estradiol derived as potential ER imaging agent. Ethinylestradiol was derivatized to introduce a dithiocarbamate function for Tc coordination. Labeling was achieved through the formation of a symmetric Tc(V)-nitrido complex with a radiochemical purity (RCP) > 95%. Physicochemical evaluation, cell uptake, biodistribution in normal animals and in nude mice bearing induced ER + breast tumors showed promising results.
Identifiants
pubmed: 31442798
pii: S0969-8043(19)30631-1
doi: 10.1016/j.apradiso.2019.108854
pii:
doi:
Substances chimiques
Organotechnetium Compounds
0
Radiopharmaceuticals
0
Receptors, Estrogen
0
Estradiol
4TI98Z838E
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
108854Informations de copyright
Copyright © 2019. Published by Elsevier Ltd.