High-throughput assays to measure intracellular Ca²⁺ mobilization in cells that express recombinant S1P receptor subtypes

Methods Mol Biol. 2012:874:77-87. doi: 10.1007/978-1-61779-800-9_7.

Abstract

Intracellular Ca(2+) mobilization is a useful readout to screen for agonists or antagonists of G-protein -coupled receptors (GPCRs). Here, we describe methods to conduct high-throughput screening of stably or transiently transfected HTC4 cells expressing the individual S1P1-5 receptor subtypes. The cells are grown in 96-well plates and loaded with the cell permeable fluorescent Ca(2+) indicator dye Fura-2-AM. Changes in intracellular Ca(2+) levels in response to S1P or test compounds are detected using a FlexStation II scanning fluorometer with integrated fluidics transfer capabilities.

Publication types

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

MeSH terms

  • Animals
  • Calcium / analysis*
  • Calcium / metabolism
  • Calcium Signaling*
  • Fluorometry
  • Fura-2 / analogs & derivatives
  • High-Throughput Screening Assays*
  • Rats
  • Receptors, Lysosphingolipid / metabolism*
  • Recombinant Proteins / metabolism
  • Tumor Cells, Cultured

Substances

  • Receptors, Lysosphingolipid
  • Recombinant Proteins
  • fura-2-am
  • Calcium
  • Fura-2