Diterpenoids from caribbean gorgonians act as noncompetitive inhibitors of the nicotinic acetylcholine receptor

@article{Eterovi1993DiterpenoidsFC,
  title={Diterpenoids from caribbean gorgonians act as noncompetitive inhibitors of the nicotinic acetylcholine receptor},
  author={Vesna A. Eterovi{\'c} and Richard M. Hann and Pedro A. Ferchmin and Abimael D Rodr{\'i}guez and Lian Li and Yung-Hui Lee and Mark G. McNamee},
  journal={Cellular and Molecular Neurobiology},
  year={1993},
  volume={13},
  pages={99-110}
}
1. Three cyclic diterpenoids isolated from gorgonians of theEunicea genus and characterized as eupalmerin acetate (EUAC), 12,13-bisepieupalmerin (BEEP), and eunicin (EUNI) were found to be pharmacologically active on the nicotinic acetylcholine receptor (AChR). 2. The receptor from the BC3H-1 muscle cell line was expressed inXenopus laevis oocytes and studied with a two-electrode voltage clamp apparatus. 3. All three compounds reversibly inhibited ACh-induced currents, with IC50's from 6 to 35… CONTINUE READING