@article{8319b0dee0e949e790319d18b70e7147,
title = "Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of α4β2 nicotinic acetylcholine receptors (α4β2-nAChRs) in the brain with positron emission tomography",
abstract = "The most abundant subtype of cerebral nicotinic acetylcholine receptors (nAChR), α4β2, plays a critical role in various brain functions and pathological states. Imaging agents suitable for visualization and quantification of α4β2 nAChRs by positron emission tomography (PET) would present unique opportunities to define the function and pharmacology of the nAChRs in the living human brain. In this study, we report the synthesis, nAChR binding affinity, and pharmacological properties of several novel 3-pyridyl ether compounds. Most of these derivatives displayed a high affinity to the nAChR and a high subtype selectivity for α4β2-nAChR. Three of these novel nAChR ligands were radiolabeled with the positron-emitting isotope 11C and evaluated in animal studies as potential PET radiotracers for imaging of cerebral nAChRs with improved brain kinetics.",
keywords = "Nicotinic acetylcholine receptor, PET, Radioligand, nAChR",
author = "Yongjun Gao and Ravert, {Hayden T.} and Hiroto Kuwabara and Yingxian Xiao and Endres, {Christopher J.} and John Hilton and Holt, {Daniel P.} and Anil Kumar and Mohab Alexander and Wong, {Dean F.} and Dannals, {Robert F.} and Horti, {Andrew G.}",
note = "Funding Information: The authors thank Paige Finley for her help with the animal experiments, Robert C. Smoot for radiochemistry assistance, and James Fox, David J. Clough and Karen Edmonds for PET scanner operation. We are grateful to Judy W. Buchanan for editorial help. This research was supported by the Department of Radiology of Johns Hopkins University School of Medicine and U.S. Public Health Service grants from the National Institutes of Health (DA020777 and MH079017). The National Institute of Mental Health Psychoactive Drug Screening Program (Grant N01 MH32004) supported some of the in vitro studies.",
year = "2009",
month = jul,
day = "1",
doi = "10.1016/j.bmc.2009.05.021",
language = "English",
volume = "17",
pages = "4367--4377",
journal = "Bioorganic and Medicinal Chemistry",
issn = "0968-0896",
number = "13",
}