Identification of subtypes of muscarinic receptors that regulate Ca2+ and K+ channel activity in sympathetic neurons

Life Sci. 2001 Apr 27;68(22-23):2481-7. doi: 10.1016/s0024-3205(01)01042-6.

Abstract

Many different G protein-coupled receptors modulate the activity of Ca2+ and K+ channels in a variety of neuronal types. There are five known subtypes (M1-M5) of muscarinic acetylcholine receptors. Knockout mice lacking the M1, M2, or M4 subtypes are studied to determine which receptors mediate modulation of voltage-gated Ca2+ channels in mouse sympathetic neurons. In these cells, muscarinic agonists modulate N- and L-type Ca2+ channels and the M-type K+ channel through two distinct, G-protein mediated pathways. The fast and voltage-dependent pathway is lacking in the M2 receptor knockout mice. The slow and voltage-independent pathway is absent in the M1 receptor knockout mice. Neither pathway is affected in the M4 receptor knockout mice. Muscarinic modulation of the M current is absent in the M1 receptor knockout mice, and can be reconstituted in a heterologous expression system using cloned channels and M1 receptors. Our results using knockout mice are compared with pharmacological data in the rat.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Calcium Channels / metabolism*
  • Electrophysiology
  • Enzyme Inhibitors / pharmacology
  • Ethylmaleimide / pharmacology
  • GTP-Binding Proteins / metabolism
  • Mice
  • Mice, Knockout
  • Muscarinic Agonists / pharmacology
  • Neurons / drug effects
  • Neurons / metabolism*
  • Oxotremorine / pharmacology
  • Potassium Channels / metabolism*
  • Protein Isoforms / genetics
  • Protein Isoforms / metabolism*
  • Rats
  • Receptors, Muscarinic / genetics
  • Receptors, Muscarinic / metabolism*
  • Signal Transduction / genetics
  • Signal Transduction / physiology
  • Superior Cervical Ganglion / cytology*
  • Superior Cervical Ganglion / drug effects
  • Superior Cervical Ganglion / physiology
  • Time Factors

Substances

  • Calcium Channels
  • Enzyme Inhibitors
  • Muscarinic Agonists
  • Potassium Channels
  • Protein Isoforms
  • Receptors, Muscarinic
  • Oxotremorine
  • GTP-Binding Proteins
  • Ethylmaleimide