Defunctionalized lobeline analogues: structure-activity of novel ligands for the vesicular monoamine transporter.

@article{Zheng2005DefunctionalizedLA,
  title={Defunctionalized lobeline analogues: structure-activity of novel ligands for the vesicular monoamine transporter.},
  author={Guangrong Zheng and Linda P. Dwoskin and Agripina Gabriela Deaciuc and Seth D. Norrholm and Peter A. Crooks},
  journal={Journal of medicinal chemistry},
  year={2005},
  volume={48 17},
  pages={
          5551-60
        }
}
(-)-Lobeline (2R,6S,10S), an antagonist at nicotinic acetylcholine receptors (nAChRs), inhibits the neurochemical and behavioral effects of methamphetamine and inhibits dopamine transporter (DAT) and vesicular monoamine transporter (VMAT2) function. VMAT2 is a target for the development of treatments for methamphetamine abuse. Structural modification of lobeline affords the defunctionalized analogues meso-transdiene (MTD) and lobelane, which have high potency and selectivity for VMAT2. To… CONTINUE READING
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