MEDI 490 |
| The most abundant subtype of cerebral nicotinic acetylcholine receptors, -nAChRs play a critical role in various brain functions and pathological states. Imaging agents suitable for visualization and quantification of the -nAChRs by positron emission tomography (PET) techniques would present unique opportunities to define the function and pharmacology of the nAChRs in the living human brain. They would therefore provide a useful tool to diagnose and monitor response to therapy in various diseases. In this study, we report the synthesis, nAChR binding affinity, and pharmacological properties of a new series of 3-pyridyl ether analogs of A-85380. Some of these nAChR ligands were radiolabeled with positron-emitting isotope 11C and evaluated in animal studies as potential PET radiotracers for imaging of cerebral nAChRs with improved brain kinetics compared with 2-[18F]-fluoro-A-85380, the radiotracer for PET imaging of -nAChRs in humans. |
|
General Poster Session
7:00 PM-9:00 PM, Wednesday, 13 September 2006 Moscone Center -- Hall D, Poster
Sci-Mix
Division of Medicinal Chemistry |