Scaffold-based design and synthesis of potent N-type calcium channel blockers.

@article{Zamponi2009ScaffoldbasedDA,
  title={Scaffold-based design and synthesis of potent N-type calcium channel blockers.},
  author={Gerald W Zamponi and Zhong-Ping Feng and Lingyun Zhang and Hossein Pajouhesh and Yanbing Ding and Francesco Belardetti and Hassan Pajouhesh and David H Dolphin and Lester A. Mitscher and Terrance P. Snutch},
  journal={Bioorganic & medicinal chemistry letters},
  year={2009},
  volume={19 22},
  pages={
          6467-72
        }
}
The therapeutic agents flunarizine and lomerizine exhibit inhibitory activities against a variety of ion channels and neurotransmitter receptors. We have optimized their scaffolds to obtain more selective N-type calcium channel blockers. During this optimization, we discovered NP118809 and NP078585, two potent N-type calcium channel blockers which have good selectivity over L-type calcium channels. Upon intraperitoneal administration both compounds exhibit analgesic activity in a rodent model… CONTINUE READING

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