Muscarinic receptor binding characteristics of a human neuroblastoma SK-N-SH and its clones SH-SY5Y and SH-EP1

Eur J Pharmacol. 1989 Jun 8;165(1):71-7. doi: 10.1016/0014-2999(89)90771-1.

Abstract

The present study examines the muscarinic receptor binding characteristics of parent human neuroblastoma (SK-N-SH) and its neuroblast (SH-SY5Y) and epithelial-like (SH-EP1) clones using [3H]methylscopolamine [( 3H]NMS). Specific [3H]NMS binding to intact SK-N-SH and SH-SY5Y cells was saturable with a Kd of 0.2 nM and Bmax of 100-150 fmol/mg protein. Specific [3H]NMS binding to whole cell preparations of SH-EP 1 could not be detected. Pharmacological analysis of the binding site both in whole cells and membranes of SK-N-SH are indicative of an homogeneous receptor population possessing low affinity for the M1-selective antagonist pirenzepine. The muscarinic receptors expressed by the neuroblast clone, SH-SY5Y were further characterized and shown to have the properties of an homogeneous M3 subtype with low affinity for the M1-selective antagonist pirenzepine and the M2-cardioselective AFDX-116 but high affinity for 4-diphenylacetoxy-N-methyl piperidine methiodide (4-DAMP). In conclusion the SH-SY5Y neuroblastoma should provide an important human neuronal cell model with which to define the regulation of post-receptor events driven by a single receptor population.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Arecoline / pharmacology
  • Atropine / pharmacology
  • Carbachol / pharmacology
  • Cell Membrane / drug effects
  • Cell Membrane / metabolism
  • Humans
  • Neuroblastoma / metabolism*
  • Piperidines / pharmacology
  • Pirenzepine / analogs & derivatives
  • Pirenzepine / metabolism
  • Pirenzepine / pharmacology
  • Receptors, Muscarinic / drug effects
  • Receptors, Muscarinic / metabolism*
  • Tumor Cells, Cultured / drug effects
  • Tumor Cells, Cultured / metabolism

Substances

  • Piperidines
  • Receptors, Muscarinic
  • Pirenzepine
  • Arecoline
  • Atropine
  • 4-diphenylacetoxy-1,1-dimethylpiperidinium
  • Carbachol
  • otenzepad