✦ LIBER ✦

Session 10: Neuroscience IV, Receptors, Proteins-Chemistry and Pharmacology

Publisher: John Wiley and Sons
Year: 2003
Tongue: French
Weight: 576 KB
Volume: 46
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.759

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✦ Synopsis

We report here the radiosynthesis, in vitro, and in vivo characterisation of novel b-amyloid binding radiotracers and compare them to the recently reported [ 11 C]-6-OH-BTA-1, currently being tested in Alzheimer's patients 1 . The compounds in the Table below were radiolabelled with 11 C and their binding affinity for Ab1-40 aggregates measured. They were evaluated using in vitro and ex vivo autoradiography in transgenic mice expressing ß-amyloid protein. Structure Affinity Ki, nM cLog P Measured Log P Tg mice Ex vivo Autorad in vitro O N H 3 C H N CH 3 37 3.70 4.21 (Wilson) No Specific Binding Yes, requires xylene wash N N N Br CH3 CH 3 10 4.653 3.47 (Wilson)

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