Specificity of Muscarinic Acetylcholine Receptor Regulation by Receptor Activity

Robert G. Siman, William L Klein*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

21 Scopus citations


Abstract— Regulation of muscarinic acetylcholine receptor concentration by receptor activity in neuron‐like NG108‐15 hybrid cells is a highly specific process. Receptor levels, monitored by binding of [3H]quinuclidinyl benzilate ([3H]QNB), decreased 50‐75% following 24‐h incubation of cells with muscarinic agonists, but none of the following cellular processes was altered by this chronic receptor stimulation: (1) glycolytic energy metabolism, measured by [3H]deoxy‐d‐glucose ([3H]DG) uptake and retention; (2) rate of cell division; (3) transport, measured by [3H]valine and [3H]uridine uptake; (4) RNA biosynthesis, measured by [3H]uridine incorporation; (5) protein biosynthesis, measured by [3H]valine and [35S]methionine incorporation into total protein and into protein fractions obtained by polyacrylamide gel electrophoresis. In contrast, chronic stimulation did cause a threefold decrease in the capacity of carbachol to stimulate phosphatidylinositol (PI) turnover, a receptor‐mediated response. In addition to cholinomimetics, the neuroeffector adenosine (1 mm for 24 h) also caused a decrease in [3H]QNB binding levels, but chronic stimulation of α‐adrenergic, opiate, prostaglandin E1, and prostaglandin F receptors found on NG108‐15 cells caused no changes. The data indicate that loss of muscarinic receptors caused by receptor stimulation is not a consequence of fundamental changes evoked in overall cellular physiology but reflects a specific regulation of cholinoceptive cell responsiveness.

Original languageEnglish (US)
Pages (from-to)1099-1108
Number of pages10
JournalJournal of Neurochemistry
Issue number5
StatePublished - Jan 1 1981


  • 2
  • Cell culture
  • d
  • Deoxy
  • glucose
  • Neuron
  • Phosphatidylinositol
  • Synaptic plasticity

ASJC Scopus subject areas

  • Biochemistry
  • Medicine(all)
  • Cellular and Molecular Neuroscience


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