Apparent noncompetitive antagonism of muscarinic receptor mediated Ca2+ mobilization by some muscarinic antagonists

Biochem Biophys Res Commun. 1992 Dec 15;189(2):919-24. doi: 10.1016/0006-291x(92)92291-5.

Abstract

Ca2+ mobilizations in SH-SY5Y and IMR-32 human neuroblastoma cell lines were measured using the fluorescent Ca2+ indicator fura-2. A variety of antagonists (atropine, pirenzepine, 4-DAMP and N-methyl-scopolamine) inhibited carbamyl choline-induced transient Ca2+ mobilization both in a competitive and a noncompetitive manner. The apparent noncompetitive inhibition constants were lower in IMR-32 than in SH-SY5Y cells even when the competitive inhibition constants were similar. This may relate to the previously reported differential expression of muscarinic receptor subtypes in these cell lines.

MeSH terms

  • Atropine / pharmacology*
  • Calcium / metabolism*
  • Fura-2
  • Humans
  • Kinetics
  • Muscarinic Antagonists
  • N-Methylscopolamine
  • Neuroblastoma
  • Parasympatholytics / pharmacology*
  • Piperidines / pharmacology*
  • Pirenzepine / pharmacology*
  • Receptors, Muscarinic / drug effects
  • Receptors, Muscarinic / physiology*
  • Scopolamine Derivatives / metabolism
  • Scopolamine Derivatives / pharmacology*
  • Spectrometry, Fluorescence
  • Tumor Cells, Cultured

Substances

  • Muscarinic Antagonists
  • Parasympatholytics
  • Piperidines
  • Receptors, Muscarinic
  • Scopolamine Derivatives
  • Pirenzepine
  • Atropine
  • 4-diphenylacetoxy-1,1-dimethylpiperidinium
  • Calcium
  • Fura-2
  • N-Methylscopolamine