Synthesis, in vitro acetylcholine-storage-blocking activities, and biological properties of derivatives and analogues of trans-2-(4-phenylpiperidino)cyclohexanol (vesamicol).

@article{Rogers1989SynthesisIV,
  title={Synthesis, in vitro acetylcholine-storage-blocking activities, and biological properties of derivatives and analogues of trans-2-(4-phenylpiperidino)cyclohexanol (vesamicol).},
  author={Glenn A. Rogers and Stanley M. Parsons and Dave C Anderson and L M Nilsson and Ben A Bahr and W D Kornreich and Rick Kaufman and Robert S. Jacobs and Bernard Kirtman},
  journal={Journal of medicinal chemistry},
  year={1989},
  volume={32 6},
  pages={1217-30}
}
Eighty-four analogues and derivatives of the acetylcholine-storage-blocking drug trans-2-(4-phenylpiperidino)-cyclohexanol (vesamicol) were synthesized, and their potencies were evaluated with the acetylcholine active-transport assay utilizing purified synaptic vesicles from Torpedo electric organ. The parent drug exhibits enantioselectivity, with (-)-vesamicol being 25-fold more potent than (+)-vesamicol. The atomic structure and absolute configuration of (+)-vesamicol were determined by X-ray… CONTINUE READING

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