Filters
Results 1 - 1 of 1
Results 1 - 1 of 1.
Search took: 0.015 seconds
AbstractAbstract
[en] To assess the suitability of Tc labeled 5α-reductase (5α-Rds) inhibitors for non-invasive targeting of prostate cancer (PCa) using Male Sprague Dawely Rat (MSDR) model. In this work, dutasteride (Cpd-1) a 5α-Rds inhibitor was derivatized to its dithiocarbamate analogue (Cpd-2) for subsequent synthesis of Tc(CO)-dutasteride dithiocarbamate (Cpd-3) using tricarbonyl technique. To determine the structure of Cpd-3, for the first time a reference Re(CO)-dutasteride dithiocarbamate (Cpd-4) was synthesized and characterized with NMR, ESIMS, HPLC and elemental analysis. HPLC was used to establish the identity of Cpd-3 using Cpd-4 as a reference standard. The suitability of Cpd-3 as a new 5α-Rds targeting agent was investigated, both in vitro and vivo. The Cpd-3 has shown ≥98 % in vitro stability at room temperature and was remained ≥90 % stable up to 6 h. In serum Cpd-3 has revealed an analogous behavior with a small decrease in stability after 16 h. High uptake (26.25 ± 1.10 %, after 4 h of i.v.) of Cpd-3 was observed in the prostate (target tissue) of MSDR model with reasonably good target to non-target ratio. Blocking the target site with excess Cpd-2 considerably decreased the uptake of Cpd-3 to 4.10 ± 0.75 % in PCa. High in vitro stability in saline and serum and in vivo uptake in prostate of MSDR model plausibly attracts the opportunity of using Cpd-3 as a novel radiopharmaceutical for non invasive targeting of prostate.
Primary Subject
Secondary Subject
Source
Available from: http://dx.doi.org/10.1515/ract-2019-3156
Record Type
Journal Article
Journal
Country of publication
ANIMALS, BETA DECAY RADIOISOTOPES, BETA-MINUS DECAY RADIOISOTOPES, BODY, CARBONIC ACID DERIVATIVES, CARBOXYLIC ACID SALTS, CHEMICAL REACTIONS, CHROMATOGRAPHY, DISEASES, DRUGS, ENZYMES, GLANDS, HOURS LIVING RADIOISOTOPES, INTERMEDIATE MASS NUCLEI, INTERNAL CONVERSION RADIOISOTOPES, ISOMERIC TRANSITION ISOTOPES, ISOTOPES, LABELLED COMPOUNDS, LIQUID COLUMN CHROMATOGRAPHY, MALE GENITALS, MAMMALS, MATERIALS, MEDICINE, NEOPLASMS, NUCLEAR MEDICINE, NUCLEI, ODD-EVEN NUCLEI, ORGANIC COMPOUNDS, ORGANIC NITROGEN COMPOUNDS, ORGANS, PROTEINS, RADIOACTIVE MATERIALS, RADIOISOTOPES, RADIOLOGY, RODENTS, SEPARATION PROCESSES, SPECTRA, TECHNETIUM ISOTOPES, TEMPERATURE RANGE, THERAPY, VERTEBRATES, YEARS LIVING RADIOISOTOPES
Reference NumberReference Number
INIS VolumeINIS Volume
INIS IssueINIS Issue
External URLExternal URL