Friedrich Hölderlin e la filosofia

Imaging Cholinergic Receptors in the Brain by Positron Emission Tomography

“…As the first full α7 nAChR agonist, AR-R17779 ( 44 ) features a 1-aza-bicyclo[2.2.2]­octane scaffold and shows reasonable binding affinity ( K i = 92 nM) and selectivity toward α7 nAChRs over α4β2 nAChRs ( K i = 16 μM) . Some derivatives of AR-R17779 ( 44 ) were patented as α7 nAChR agonists; however, there is no available pharmacological data . The radiolabeling of one compound in this series with [ 11 C]­phosgene resulted in radioligand [ 11 C] 2 ( 45 ) .…”

“… 132 Some derivatives of AR-R17779 ( 44 ) were patented as α7 nAChR agonists; however, there is no available pharmacological data. 133 The radiolabeling of one compound in this series with [ 11 C]phosgene resulted in radioligand [ 11 C] 2 ( 45 ). 134 Ex vivo biodistribution studies of [ 11 C] 2 ( 45 ) in rats demonstrated reasonable brain uptake with 0.8–1.2%ID/g among various brain regions.…”