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Page 1
Discovery of isoxazole analogues of sazetidine-A as selective α4β2-nicotinic acetylcholine receptor partial agonists for the treatment of depression.
Liu J, Yu LF, Eaton JB, Caldarone B, Cavino K, Ruiz C, Terry M, Fedolak A, Wang D, Ghavami A, Lowe DA, Brunner D, Lukas RJ, Kozikowski AP. Liu J, et al. Among authors: fedolak a. J Med Chem. 2011 Oct 27;54(20):7280-8. doi: 10.1021/jm200855b. Epub 2011 Sep 30. J Med Chem. 2011. PMID: 21905669 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. Among authors: fedolak a. 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. Among authors: fedolak a. 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.
Dissociation between duration of action in the forced swim test in mice and nicotinic acetylcholine receptor occupancy with sazetidine, varenicline, and 5-I-A85380.
Caldarone BJ, Wang D, Paterson NE, Manzano M, Fedolak A, Cavino K, Kwan M, Hanania T, Chellappan SK, Kozikowski AP, Olivier B, Picciotto MR, Ghavami A. Caldarone BJ, et al. Among authors: fedolak a. Psychopharmacology (Berl). 2011 Sep;217(2):199-210. doi: 10.1007/s00213-011-2271-y. Epub 2011 Apr 13. Psychopharmacology (Berl). 2011. PMID: 21487659 Free PMC article.
11 results