Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor.

@article{Polepally2014MichaelAA,
  title={Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor.},
  author={Prabhakar Reddy Polepally and Krzysztof Huben and Eyal Vardy and Vincent Setola and Philip D Mosier and Bryan L. Roth and Jordan Kordian Zjawiony},
  journal={European journal of medicinal chemistry},
  year={2014},
  volume={85},
  pages={818-29}
}
The neoclerodane diterpenoid salvinorin A is a major secondary metabolite isolated from the psychoactive plant Salvia divinorum. Salvinorin A has been shown to have high affinity and selectivity for the κ-opioid receptor (KOR). To study the ligand-receptor interactions that occur between salvinorin A and the KOR, a new series of salvinorin A derivatives bearing potentially reactive Michael acceptor functional groups at C-2 was synthesized and used to probe the salvinorin A binding site. The… CONTINUE READING