Radioiodinated 2'-iododiazepam: a potential imaging agent for SPECT investigations of benzodiazepine receptors.
J Nucl Med
; 34(6): 932-7, 1993 Jun.
Article
em En
| MEDLINE
| ID: mdl-8389843
ABSTRACT
2'-Iododiazepam (2'-IDZ) is the diazepam analogue iodinated at the 2'-position of C-5 phenyl ring which was synthesized and evaluated as a potential radiopharmaceutical for investigating brain benzodiazepine receptors by SPECT. The 125I-2'-iododiazepam was synthesized by halogen exchange reaction and purified by HPLC. In vitro competitive binding studies with 3H-diazepam, using rat cortical synaptosomal membranes, showed that the affinity of 2'-IDZ for benzodiazepam receptors was higher than that in diazepam and flumazenil (RO15-1788). Biodistribution studies in mice showed that the brain uptake of 2'-iododiazepam was rapid and profound, and in the brain higher accumulation was found in the cortex than in other regions. Furthermore, the cortical uptake was displaced by benzodiazepinergic compounds. In vivo uptake was assessed by autoradiographic studies. Thus, 2'-iododiazepam bound to benzodiazepine receptors in vivo and therefore holds great potential for in vivo benzodiazepine receptor studies.
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Base de dados:
MEDLINE
Assunto principal:
Benzodiazepinonas
/
Encéfalo
/
Tomografia Computadorizada de Emissão de Fóton Único
/
Receptores de GABA-A
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Diazepam
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Radioisótopos do Iodo
Limite:
Animals
Idioma:
En
Revista:
J Nucl Med
Ano de publicação:
1993
Tipo de documento:
Article
País de afiliação:
Japão