Estrogens directly potentiate neuronal L-type Ca2+ channels

Proc Natl Acad Sci U S A. 2008 Sep 30;105(39):15148-53. doi: 10.1073/pnas.0802379105. Epub 2008 Sep 24.

Abstract

L-type voltage-gated Ca(2+)channels (VGCC) play an important role in dendritic development, neuronal survival, and synaptic plasticity. Recent studies have demonstrated that the gonadal steroid estrogen rapidly induces Ca(2+) influx in hippocampal neurons, which is required for neuroprotection and potentiation of LTP. The mechanism by which estrogen rapidly induces this Ca(2+) influx is not clearly understood. We show by electrophysiological studies that extremely low concentrations of estrogens acutely potentiate VGCC in hippocampal neurons, hippocampal slices, and HEK-293 cells transfected with neuronal L-type VGCC, in a manner that was estrogen receptor (ER)-independent. Equilibrium, competitive, and whole-cell binding assays indicate that estrogen directly interacts with the VGCC. Furthermore, a L-type VGCC antagonist to the dihydropyridine site displaced estrogen binding to neuronal membranes, and the effects of estrogen were markedly attenuated in a mutant, dihydropyridine-insensitive L-type VGCC, demonstrating a direct interaction of estrogens with L-type VGCC. Thus, estrogen-induced potentiation of calcium influx via L-type VGCC may link electrical events with rapid intracellular signaling seen with estrogen exposure leading to modulation of synaptic plasticity, neuroprotection, and memory formation.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Calcium Channels, L-Type / genetics
  • Calcium Channels, L-Type / metabolism*
  • Cell Line
  • Estradiol / metabolism
  • Estradiol / pharmacology
  • Estrogens / metabolism*
  • Estrogens / pharmacology
  • Humans
  • Mutation
  • Neurons / drug effects
  • Neurons / metabolism*
  • Rats
  • Receptors, Estrogen / genetics
  • Receptors, Estrogen / metabolism
  • Recombinant Proteins / genetics
  • Recombinant Proteins / metabolism

Substances

  • Calcium Channels, L-Type
  • Estrogens
  • L-type calcium channel alpha(1C)
  • Receptors, Estrogen
  • Recombinant Proteins
  • Estradiol