Muscarinic receptor subtypes of guinea-pig common bile duct

Arch Int Pharmacodyn Ther. 1991 Jul-Aug:312:140-5.

Abstract

The antagonism of carbachol-induced contractions of guinea-pig common bile duct smooth muscle strips by various antagonists has been investigated in order to find out the muscarinic receptor subtype(s) of common bile duct smooth muscle. Atropine, pirenzepine, 4-DAMP and AF-DX 116 were used as nonselective, M1-selective, M1- and M3-selective and M2-selective muscarinic antagonists, respectively. All muscarinic antagonists examined displaced the concentration-response curves to the right, parallelly and in a concentration-dependent manner, without affecting maximum response. Schild analysis of data was consistent with competitive antagonism. pA2 values of the antagonists were as follows: atropine, 9.59; pirenzepine, 7.32; 4-DAMP, 8.99; AF-DX 116, 6.85. When these pA2 values are compared with those obtained in the ileum, it may be concluded that the muscarinic receptors of the guinea-pig common bile duct mediating cholinomimetic-induced contractions, are of the M3 subtype, but not of the M1 and M2 subtypes.

MeSH terms

  • Animals
  • Atropine / pharmacology
  • Carbachol / pharmacology
  • Common Bile Duct / innervation*
  • Female
  • Guinea Pigs
  • Male
  • Muscarinic Antagonists
  • Muscle Contraction / drug effects*
  • Muscle, Smooth / drug effects
  • Muscle, Smooth / innervation*
  • Muscle, Smooth / physiology
  • Parasympatholytics / pharmacology*
  • Piperidines / pharmacology
  • Pirenzepine / analogs & derivatives
  • Pirenzepine / pharmacology
  • Receptors, Muscarinic / metabolism*

Substances

  • Muscarinic Antagonists
  • Parasympatholytics
  • Piperidines
  • Receptors, Muscarinic
  • Pirenzepine
  • Atropine
  • 4-diphenylacetoxy-1,1-dimethylpiperidinium
  • Carbachol
  • otenzepad