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

Kathleen H Mortell; 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

doi:10.1016/j.bmcl.2005.11.108

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. Epub 2005 Dec 27.

Authors

Kathleen H Mortell¹, 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

Affiliation

¹ Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA. kathleen.mortell@abbott.com

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.

MeSH terms

Amino Acids / chemistry*
Animals
Benzene / chemistry
Calcium Channel Blockers / chemistry*
Calcium Channel Blockers / pharmacology*
Calcium Channels / chemistry*
Calcium Channels / metabolism*
Ligands
Molecular Structure
Pain / drug therapy
Pain / metabolism
Protein Subunits / metabolism
Rats
Structure-Activity Relationship

Substances

Amino Acids
Calcium Channel Blockers
Calcium Channels
Ligands
Protein Subunits
Benzene