CPD – Education and Self-assessment: Functional imaging in epilepsy

Richardson, Mark P.

doi:10.1053/seiz.2001.0546

Cited by 2 publications

(1 citation statement)

References 171 publications

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“…Positron emission tomography (PET) and single photon emission tomography (SPET) are unique technologies for the noninvasive monitoring of receptor patterns in integrated organisms without affecting their in vivo stability. Various radiopharmaceuticals have been proposed as suitable candidates for the application of these imaging procedures to the evaluation of benzodiazepine receptor distribution ( , ). It has been showed previously that the derivative Iomazenil labeled with the γ-emitting radionuclide I-123 possesses useful biological characteristics, and it is currently employed as imaging agent for the diagnosis of various brain diseases related to alterations of benzodiazepine receptors ().…”

Section: Introductionmentioning

confidence: 99%

Asymmetrical Nitrido Tc-99m Heterocomplexes as Potential Imaging Agents for Benzodiazepine Receptors

et al. 2003

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The design, synthesis, and biological evaluation of nitrido technetium-99m complexes for imaging benzodiazepine receptors are described. The design was performed by selecting the precursor biologically active substrate desmethyldiazepam, and the reactive metal-containing fragment [(99m)Tc(N)(PXP)](2+) (PXP = diphosphine ligand) as molecular building-blocks for assembling the structure of the final radiopharmaceuticals through the application of the so-called 'bifunctional' and 'integrated' approaches. This required the synthesis of the ligands H(2)BZ1, H(2)C1, and H(2)C2 (Figures 1 and 2) derived from desmethyldiazepam. In turn, these ligands were reacted with [(99m)Tc(N)(PXP)](2+) to afford the complexes [(99m)Tc(N)(PXP)(L)] (L = BZ1, C1, C2). The chemical nature of the resulting Tc-99m radiopharmaceuticals was investigated using chromatographic methods, and by comparison with the analogous complexes prepared with the long-lived isotope Tc-99g and characterized by spectroscopic and analytical methods. Results showed that the complexes [(99m)Tc(N)(PXP)(L)] are neutral and possess an asymmetrical five-coordinated structure in which two different bidentate ligands, PXP and L, are coordinated to the same Tc[triple bond]N core. With the ligand H(2)BZ1, two isomers were obtained depending on the syn or anti orientation of the pendant benzodiazepine group relative to the Tc[triple bond]N multiple bond. Biodistribution studies of Tc-99m complexes were carried out in rats, and affinity for benzodiazepine receptors was assessed through in vitro binding experiments on isolated rat's cerebral membranes using the corresponding Tc-99g complexes.

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Section: Introductionmentioning

confidence: 99%