Potentiation by alcuronium of the antimuscarinic effect of N-methylscopolamine in guinea pig left atria

Eur J Pharmacol. 1995 Jan 5;272(1):103-6. doi: 10.1016/0014-2999(94)00664-s.

Abstract

Alcuronium is known to stabilize allosterically the binding of the muscarinic antagonist N-methylscopolamine to muscarinic M2 receptors and thus to elevate the equilibrium binding of N-methylscopolamine in homogenized cardiac tissue. In order to check for a functional consequence of this effect, the action of alcuronium alone and in combination with N-methylscopolamine was determined in contracting guinea pig left auricles with oxotremorine-M as the negative inotropic agonist. For sake of comparison, the allosteric modulator W84 = hexane-1,6-bis(dimethyl-3'- phthalimidopropyl-ammonium bromide) was included. Alcuronium displayed a weak antimuscarinic action (pA2 = 5.7). In conjunction with 10(-7) M N-methylscopolamine, alcuronium (> or = 10(-6) M) induced a more pronounced antimuscarinic effect than expected for a combination of competitive antagonists. The extent of overadditivity with combinations of W84 and 10(-7) M N-methylscopolamine was smaller. In conclusion, alcuronium potentiates the antimuscarinic effect of N-methylscopolamine in contracting cardiac preparations with high effectivity.

Publication types

  • Comparative Study

MeSH terms

  • Alcuronium / pharmacology*
  • Allosteric Regulation / drug effects
  • Animals
  • Atrial Function
  • Binding Sites
  • Cholinesterase Inhibitors / pharmacology
  • Computer Simulation
  • Guinea Pigs
  • Heart Atria / drug effects*
  • Heart Atria / metabolism
  • In Vitro Techniques
  • Isoindoles
  • Myocardial Contraction / drug effects
  • N-Methylscopolamine
  • Oxotremorine / analogs & derivatives
  • Oxotremorine / pharmacology
  • Parasympatholytics / metabolism
  • Parasympatholytics / pharmacology*
  • Phthalimides / pharmacology
  • Receptors, Muscarinic / drug effects*
  • Receptors, Muscarinic / metabolism
  • Regression Analysis
  • Scopolamine Derivatives / metabolism
  • Scopolamine Derivatives / pharmacology*

Substances

  • Cholinesterase Inhibitors
  • Isoindoles
  • Parasympatholytics
  • Phthalimides
  • Receptors, Muscarinic
  • Scopolamine Derivatives
  • hexamethylenebis(dimethyl-(3-phthalimidopropyl)ammonium bromide)
  • Oxotremorine
  • oxotremorine M
  • Alcuronium
  • N-Methylscopolamine