Structure-activity relationships of alpha-amino acid ligands for the alpha2delta subunit of voltage-gated calcium channels

  • Bioorg Med Chem Lett. 2006 Mar 1;16(5):1138-41. doi: 10.1016/j.bmcl.2005.11.108.
Kathleen H Mortell  1 ,  David J Anderson ,  James J Lynch 3rd ,  Sherry L Nelson ,  Kathy Sarris ,  Heath McDonald ,  Reza Sabet ,  Scott Baker ,  Prisca Honore ,  Chih-Hung Lee ,  Michael F Jarvis ,  Murali Gopalakrishnan
Affiliations
  • 1. Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA. [email protected]
PMID: 16380257 DOI: 10.1016/j.bmcl.2005.11.108
Abstract

A series of alpha-amino acids were identified as ligands which compete with gabapentin for binding to the Alpha(2)delta subunit of voltage-dependent CA(2+) channels. Potent analogs were identified. Their activity in an in vivo Pain assay is described.

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