Relationship between agonist binding, phosphorylation and immunoprecipitation of the m3-muscarinic receptor, and second messenger responses

Br J Pharmacol. 1995 Sep;116(2):1723-8. doi: 10.1111/j.1476-5381.1995.tb16654.x.

Abstract

1. Phosphoinositidase C-linked m3-muscarinic receptors expressed in Chinese hamster ovary cells (CHO-m3 cells) are phosphorylated on serine following agonist stimulation. 2. m3-Muscarinic receptor phosphorylation is concentration-dependent requiring a carbachol concentration of 13.2 microM for half maximal stimulation. 3. The phosphorylation concentration-response curve lies to the left of the curve for carbachol binding to muscarinic receptors (KD = 100 microM) in membranes from CHO-m3 cells. In contrast, receptor phosphorylation closely correlates with receptor-mediated phosphoinositidase C activation (EC50 for inositol 1,4,5 trisphosphate accumulation during the peak and plateau phases were 7.14 microM and 5.92 microM respectively) but not with rapid agonist-mediated calcium elevation (EC50 = 0.32 microM) measured in fura-2-AM loaded cells. 4. These data suggest a dissociation of receptor phosphorylation from agonist occupation. Such an apparent 'receptor reserve' for m3-muscarinic receptor phosphorylation may be indicative of a mechanism that is dependent on a small amplification of the receptor signal, though probably dissociated from the calcium signal.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding, Competitive*
  • CHO Cells
  • Carbachol / pharmacology*
  • Cells, Cultured
  • Cricetinae
  • Dose-Response Relationship, Drug
  • Phosphorylation
  • Precipitin Tests
  • Receptors, Muscarinic / drug effects*
  • Receptors, Muscarinic / physiology*
  • Second Messenger Systems / physiology*
  • Signal Transduction / physiology*
  • Time Factors

Substances

  • Receptors, Muscarinic
  • Carbachol