Interaction between muscarinic receptor subtype signal transduction pathways mediating bladder contraction

Am J Physiol Regul Integr Comp Physiol. 2002 Sep;283(3):R663-8. doi: 10.1152/ajpregu.00116.2002.

Abstract

M(3) muscarinic receptors mediate cholinergic-induced contraction in most smooth muscles. However, in the denervated rat bladder, M(2) receptors participate in contraction because M(3)-selective antagonists [para-fluoro-hexahydro-sila-diphenidol (p-F-HHSiD) and 4-DAMP] have low affinities. However, the affinity of the M(2)-selective antagonist methoctramine in the denervated bladder is consistent with M(3) receptor mediating contraction. It is possible that two pathways interact to mediate contraction: one mediated by the M(2) receptor and one by the M(3) receptor. To determine whether an interaction exists, the inhibitory potencies of combinations of methoctramine and p-F-HHSiD for reversing cholinergic contractions were measured. In normal bladders, all combinations gave additive effects. In denervated bladders, synergistic effects were seen with the 10:1 and 1:1 (methoctramine:p-F-HHSiD wt/wt) combinations. After application of the sarcoplasmic reticulum ATPase inhibitor thapsigargin to normal tissue, the 10:1 and 1:1 ratios became synergistic, mimicking denervated tissue. Thus in normal bladders both M(2) and M(3) receptors can induce contraction. In the denervated bladder, the M(2) and the M(3) receptors interact in a facilitatory manner to mediate contraction.

Publication types

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

MeSH terms

  • Animals
  • Carbachol / pharmacology
  • Cholinergic Agents / pharmacology
  • Denervation
  • Female
  • In Vitro Techniques
  • Muscarinic Antagonists / pharmacology
  • Muscle Contraction / physiology*
  • Muscle, Smooth / physiology*
  • Piperidines / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptor, Muscarinic M2
  • Receptor, Muscarinic M3
  • Receptors, Muscarinic / metabolism*
  • Second Messenger Systems / drug effects
  • Second Messenger Systems / physiology
  • Signal Transduction / drug effects
  • Signal Transduction / physiology*
  • Urinary Bladder / physiology*
  • Urinary Incontinence / metabolism

Substances

  • Cholinergic Agents
  • Muscarinic Antagonists
  • Piperidines
  • Receptor, Muscarinic M2
  • Receptor, Muscarinic M3
  • Receptors, Muscarinic
  • 4-fluorohexahydrosiladifenidol
  • Carbachol