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Pharmacokinetics and brain penetration of LF-3-88, (2-[5-[5-(2(S)-azetidinylmethoxyl)-3-pyridyl]-3-isoxazolyl]ethanol), a selective α4β2-nAChR partial agonist and promising antidepressant.
Yuan Y, Yu LF, Qiu X, Kozikowski AP, van Breemen RB. Yuan Y, et al. J Chromatogr B Analyt Technol Biomed Life Sci. 2013 Jan 1;912:38-42. doi: 10.1016/j.jchromb.2012.11.011. Epub 2012 Nov 23. J Chromatogr B Analyt Technol Biomed Life Sci. 2013. PMID: 23246847 Free PMC article.
Insights into the structural determinants required for high-affinity binding of chiral cyclopropane-containing ligands to α4β2-nicotinic acetylcholine receptors: an integrated approach to behaviorally active nicotinic ligands.
Zhang HK, Eaton JB, Yu LF, Nys M, Mazzolari A, van Elk R, Smit AB, Alexandrov V, Hanania T, Sabath E, Fedolak A, Brunner D, Lukas RJ, Vistoli G, Ulens C, Kozikowski AP. Zhang HK, et al. J Med Chem. 2012 Sep 27;55(18):8028-37. doi: 10.1021/jm3008739. Epub 2012 Sep 7. J Med Chem. 2012. PMID: 22928944 Free PMC article.
Chemistry and behavioral studies identify chiral cyclopropanes as selective α4β2-nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile.
Zhang H, Tückmantel W, Eaton JB, Yuen PW, Yu LF, Bajjuri KM, Fedolak A, Wang D, Ghavami A, Caldarone B, Paterson NE, Lowe DA, Brunner D, Lukas RJ, Kozikowski AP. Zhang H, et al. J Med Chem. 2012 Jan 26;55(2):717-24. doi: 10.1021/jm201157c. Epub 2012 Jan 10. J Med Chem. 2012. PMID: 22171543 Free PMC article.