Assignment of muscarinic receptor subtypes mediating G-protein modulation of Ca(2+) channels by using knockout mice

Proc Natl Acad Sci U S A. 1999 Sep 14;96(19):10899-904. doi: 10.1073/pnas.96.19.10899.

Abstract

There are five known subtypes of muscarinic receptors (M(1)-M(5)). We have used knockout mice lacking the M(1), M(2), or M(4) receptors to determine which subtypes mediate modulation of voltage-gated Ca(2+) channels in mouse sympathetic neurons. Muscarinic agonists modulate N- and L-type Ca(2+) channels in these neurons through two distinct G-protein-mediated mechanisms. One pathway is fast and membrane-delimited and inhibits N- and P/Q-type channels by shifting their activation to more depolarized potentials. The other is slow and voltage-independent and uses a diffusible cytoplasmic messenger to inhibit both Ca(2+) channel types. Using patch-clamp methods on acutely dissociated sympathetic neurons, we isolated each pathway by pharmacological and kinetic means and found that each one is nearly absent in a particular knockout mouse. The fast and voltage-dependent pathway is lacking in the M(2) receptor knockout mice; the slow and voltage-independent pathway is absent from the M(1) receptor knockout mice; and neither pathway is affected in the M(4) receptor knockout mice. The knockout effects are clean and are apparently not accompanied by compensatory changes in other muscarinic receptors.

Publication types

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

MeSH terms

  • Animals
  • Calcium Channels / metabolism*
  • Ethylmaleimide / metabolism
  • GTP-Binding Proteins / metabolism*
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Models, Biological
  • Oxotremorine / metabolism
  • Patch-Clamp Techniques
  • Receptors, Muscarinic / classification*
  • Time Factors
  • Virulence Factors, Bordetella / metabolism

Substances

  • Calcium Channels
  • Receptors, Muscarinic
  • Virulence Factors, Bordetella
  • Oxotremorine
  • GTP-Binding Proteins
  • Ethylmaleimide