Structure-activity relationships of alpha-amino acid ligands for the alpha2delta subunit of voltage-gated calcium channels.
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.
Mortell
Kathleen H
KH
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA. kathleen.mortell@abbott.com
Anderson
David J
DJ
Lynch
James J
JJ
Nelson
Sherry L
SL
Sarris
Kathy
K
McDonald
Heath
H
Sabet
Reza
R
Baker
Scott
S
Honore
Prisca
P
Lee
Chih-Hung
CH
Jarvis
Michael F
MF
Gopalakrishnan
Murali
M
D000596:Amino Acids / Q000737:chemistry*; D000818:Animals; D001554:Benzene / Q000737:chemistry; D002121:Calcium Channel Blockers / Q000737:chemistry* / Q000494:pharmacology*; D015220:Calcium Channels / Q000737:chemistry* / Q000378:metabolism*; D008024:Ligands; D015394:Molecular Structure; D010146:Pain / Q000188:drug therapy / Q000378:metabolism; D021122:Protein Subunits / Q000378:metabolism; D051381:Rats; D013329:Structure-Activity Relationship
D000596:Amino Acids; D002121:Calcium Channel Blockers; D015220:Calcium Channels; D008024:Ligands; D021122:Protein Subunits; D001554:Benzene