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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.
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.
Discovery of highly potent and selective α4β2-nicotinic acetylcholine receptor (nAChR) partial agonists containing an isoxazolylpyridine ether scaffold that demonstrate antidepressant-like activity. Part II.
Yu LF, Eaton JB, Fedolak A, Zhang HK, Hanania T, Brunner D, Lukas RJ, Kozikowski AP. Yu LF, et al. Among authors: zhang hk. J Med Chem. 2012 Nov 26;55(22):9998-10009. doi: 10.1021/jm301177j. Epub 2012 Nov 2. J Med Chem. 2012. PMID: 23092294 Free PMC article.
The potent and selective α4β2*/α6*-nicotinic acetylcholine receptor partial agonist 2-[5-[5-((S)Azetidin-2-ylmethoxy)-3-pyridinyl]-3-isoxazolyl]ethanol demonstrates antidepressive-like behavior in animal models and a favorable ADME-tox profile.
Yu LF, Brek Eaton J, Zhang HK, Sabath E, Hanania T, Li GN, van Breemen RB, Whiteaker P, Liu Q, Wu J, Chang YC, Lukas RJ, Brunner D, Kozikowski AP. Yu LF, et al. Among authors: zhang hk. Pharmacol Res Perspect. 2014 Apr;2(2):e00026. doi: 10.1002/prp2.26. Epub 2014 Mar 12. Pharmacol Res Perspect. 2014. PMID: 25505580 Free PMC article.
From a Designer Drug to the Discovery of Selective Cannabinoid Type 2 Receptor Agonists with Favorable Pharmacokinetic Profiles for the Treatment of Systemic Sclerosis.
Jiang BE, Jiang X, Zhang Q, Liang Q, Qiu ZL, Sun XB, Yang JJ, Chen S, Yi C, Chai X, Liu M, Yu LF, Lu W, Zhang HK. Jiang BE, et al. Among authors: zhang q, zhang hk. J Med Chem. 2021 Jan 14;64(1):385-403. doi: 10.1021/acs.jmedchem.0c01023. Epub 2020 Dec 31. J Med Chem. 2021. PMID: 33382613
220 results