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Preparation and biological evaluation of 99m Tc–ropinirole as a novel radiopharmaceutical for brain imaging
Author(s) -
Motaleb M. A.,
Ibrahem I. T.,
Ayoub V. R.,
Geneidi A. S.
Publication year - 2016
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3380
Subject(s) - ropinirole , chemistry , clearance , technetium 99m , pharmacology , technetium , in vivo , nuclear medicine , radiochemistry , receptor , medicine , scintigraphy , biochemistry , nuclear chemistry , urology , dopamine agonist , microbiology and biotechnology , biology , agonist
Noninvasive brain imaging is a process that allows scientists and physicians to view and monitor the areas of the brain. The aim of this study was to formulate a novel radiopharmaceutical for the detection of brain disorders at early stages in susceptible patients. 99m Tc–ropinirole was prepared by the direct complexation of ropinirole with technetium‐99m. The results showed that the radiochemical yield 99m Tc–ropinirole was 92 ± 2.87% and the radiochemical yield was evaluated by paper chromatography and HPLC. In vitro studies showed that the formed complex was stable for up to 6 h. In vivo uptake of 99m Tc–ropinirole in the brain was 4.87 ± 0.15% injected dose/g organ at 30 min post‐injection, which cleared from the brain with time till it reaches 2.3% at 2 h post‐injection indicating that the brain uptake of 99m Tc–ropinirole is higher than that of the commercially available 99m Tc‐HMPAO, which is 2.25% at 30 min. Pre‐dosing mice with cold ropinirole reduced the brain uptake to 0.26 ± 0.01% injected dose/g organ, so this confirms the high specificity and selectivity of this radiotracer for the assessment of the dopamine receptors.