A POTENTIAL IMAGING AGENT FOR THE GABA(A) RECEPTOR - -123]IODOPHENYL)-2,6,7-TRIOXABICYCLO-[2.2.2]OCTANE

Authors
CULBERT PA CHAN S WEARRING AV CHAMBERLAIN MJ HUNTER DH
Citation
Pa. Culbert et al., A POTENTIAL IMAGING AGENT FOR THE GABA(A) RECEPTOR - -123]IODOPHENYL)-2,6,7-TRIOXABICYCLO-[2.2.2]OCTANE, Nuclear medicine and biology, 20(4), 1993, pp. 469-475
Citations number
22
Categorie Soggetti
Radiology,Nuclear Medicine & Medical Imaging
Journal title
Nuclear medicine and biology
ISSN journal
09698051 → ACNP
Volume
20
Issue
4
Year of publication
1993
Pages
469 - 475
Database
ISI
SICI code
0969-8051(1993)20:4<469:APIAFT>2.0.ZU;2-D
Abstract
Based upon the known high toxicity and high antagonist activity of t-b utylorthobenzoates towards the GABA receptor complex, 1-(4-iodophenyl) -2,6,7-trioxabicyclo-[2-2.2]octane 5 and its radioiodo analogues ([I-1 23]-5 and [I-131]-5 were prepared as potential markers for the gated c hloride channel of GABA(A) receptors. Mice showed rapid clearance of [ I-131]-5 from all organs including the brain. The radioactivity was fo und to proceed into the urine in spite of the high lipophilicity of 5, the high binding affinity of 5 for plasma protein and the apparent ch emical stability of 5 in plasma.