The Biology and Pharmacology of Calcium Channel α2-δ Proteins Pfizer satellite symposium to the 2003 Society for Neuroscience Meeting Sheraton New Orleans Hotel New Orleans, LA November 10, 2003

Charles P. Taylor, William A. Catterall, Franz Hofmann, Z. David Luo, David J. Wustrow, Michael Vasko, Mark Field, Scott Baron

Research output: Contribution to journalArticle

95 Scopus citations

Abstract

Overall, these presentations reviewed the current state of α2-δ biology and pharmacology. The presentations describing structure-activity studies and mutation studies of drug binding to α2-δ indicated that high-affinity binding of pregabalin and related compounds to α2-δ type 1 protein is necessary for pharmacological actions in models of analgesic, anxiolytic, and anticonvulsant action. These findings suggest that drugs that act by binding to the α2-δ proteins define a novel class of centrally-acting drugs that are fundamentally different from other kinds of anticonvulsant, analgesic or anxiolytic drugs. It is thought that these α2-δ ligand drugs act by reducing the synaptic release of excitatory neurotransmitters and neuromodulators in the brain or spinal cord, particularly when synapses are abnormally hyperactive, or when cytosolic proteins are phosphorylated by protein kinase C or protein kinase A activation.

Original languageEnglish (US)
Pages (from-to)183-188
Number of pages6
JournalCNS Drug Reviews
Volume10
Issue number2
DOIs
StatePublished - 2004

Keywords

  • α-δ Proteins
  • Analgesics
  • Anticonvulsants
  • Calcium channels
  • Gabapentin
  • Pregabalin
  • R217A mice

ASJC Scopus subject areas

  • Pharmacology
  • Neuropsychology and Physiological Psychology

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