… -(S)-pyrrolidinyl) methoxy) pyridine with low picomolar affinity for α4β2 nicotinic acetylcholine receptor and wide range of lipophilicity: Potential probes for imaging with …

…, OA Pavlova, SI Chefer, AW Hall, V Kurian…

Index: Zhang, Yi; Pavlova, Olga A.; Chefer, Svetlana I.; Hall, Andrew W.; Kurian, Varughese; Brown, LaVerne L.; Kimes, Alane S.; Mukhin, Alexey G.; Horti, Andrew G. Journal of Medicinal Chemistry, 2004 , vol. 47, # 10 p. 2453 - 2465

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Citation Number: 56

Abstract

Potential positron emission tomography (PET) ligands with low picomolar affinity at the nicotinic acetylcholine receptor (nAChR) and with lipophilicity (log D) ranging from-1.6 to+ 1.5 have been synthesized. Most members of the series, which are derivatives of 5- substituted-6-halogeno-A-85380, exhibited a higher binding affinity at α4β2-nAChRs than epibatidine. An analysis, by molecular modeling, revealed an important role of the ...