Chemistry and pharmacology of nicotinic ligands based on 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol (AMOP-H-OH) for possible use in depression.

@article{Kozikowski2009ChemistryAP,
  title={Chemistry and pharmacology of nicotinic ligands based on 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol (AMOP-H-OH) for possible use in depression.},
  author={Alan P. Kozikowski and Jason Brek Eaton and Krishna Mohan Bajjuri and Sheela K. Chellappan and Yihua Chen and Sudhakar Karadi and Rong He and Barbara J. Caldarone and Michael L Manzano and Po-wai Yuen and Ronald J. Lukas},
  journal={ChemMedChem},
  year={2009},
  volume={4 8},
  pages={1279-91}
}
AMOP-H-OH (sazetidine-A; 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol) and some sulfur-bearing analogues were tested for their activities in vitro against human alpha4beta2-, alpha4beta4-, alpha3beta4*- and alpha1*-nicotinic acetylcholine receptors (nAChRs). AMOP-H-OH was also assessed in an antidepressant efficacy model. AMOP-H-OH and some of its analogues have high potency and selectivity for alpha4beta2-nAChRs over other nAChR subtypes. Effects are manifested as partial agonism… CONTINUE READING

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