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Discovery of (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging properties.
Gao Y, Kuwabara H, Spivak CE, Xiao Y, Kellar K, Ravert HT, Kumar A, Alexander M, Hilton J, Wong DF, Dannals RF, Horti AG. Gao Y, et al. J Med Chem. 2008 Aug 14;51(15):4751-64. doi: 10.1021/jm800323d. Epub 2008 Jul 8. J Med Chem. 2008. PMID: 18605717
Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.
Kulkarni SS, Zou MF, Cao J, Deschamps JR, Rodriguez AL, Conn PJ, Newman AH. Kulkarni SS, et al. J Med Chem. 2009 Jun 11;52(11):3563-75. doi: 10.1021/jm900172f. J Med Chem. 2009. PMID: 19445453 Free PMC article.
Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography.
Gao Y, Ravert HT, Kuwabara H, Xiao Y, Endres CJ, Hilton J, Holt DP, Kumar A, Alexander M, Wong DF, Dannals RF, Horti AG. Gao Y, et al. Bioorg Med Chem. 2009 Jul 1;17(13):4367-77. doi: 10.1016/j.bmc.2009.05.021. Epub 2009 May 15. Bioorg Med Chem. 2009. PMID: 19481945 Free PMC article.