Evidence for M1 muscarinic cholinoceptors mediating facilitation of noradrenaline release in guinea-pig carotid artery

Naunyn Schmiedebergs Arch Pharmacol. 1992 Oct;346(4):391-4. doi: 10.1007/BF00171079.

Abstract

The muscarinic agonists acetylcholine (1-50 mumol/l), carbachol (1-10 mumol/l) and McN-A-343 (1-50 mumol/l, selective for M1 receptors) increased, in a concentration-dependent manner, the electrically-evoked tritium overflow from guinea-pig carotid arteries preincubated with [3H]-noradrenaline. The increase caused by acetylcholine was not modified by hexamethonium (300 mumol/l) but was reduced by the muscarinic receptor antagonists methylatropinium (0.5 and 1 nmol/l, non-selective), pirenzepine (1 and 5 nmol/l, M1-selective), methoctramine (1 and 5 mumol/l, M2-selective) and p-fluoro-hexahydro-sila-difenidol (0.1-1 mumol/l, M3-selective). The order of potencies (expressed as negative logarithms of concentrations that reduced by 50% the facilitatory effect of acetylcholine) was: methyl-atropinium (9.93) > pirenzepine (8.83) > p-fluoro-hexahydro-siladifenidol (6.81) > or = methoctramine (6.20). These results demonstrate the existence of facilitatory M1 receptors modulating noradrenaline release in blood vessels.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholine / pharmacology
  • Animals
  • Carotid Arteries / drug effects
  • Carotid Arteries / metabolism
  • Drug Interactions
  • Guinea Pigs
  • Muscle, Smooth, Vascular / drug effects*
  • Muscle, Smooth, Vascular / metabolism
  • Norepinephrine / metabolism*
  • Parasympatholytics / pharmacology*
  • Parasympathomimetics / pharmacology*
  • Receptors, Muscarinic / drug effects*
  • Receptors, Muscarinic / metabolism

Substances

  • Parasympatholytics
  • Parasympathomimetics
  • Receptors, Muscarinic
  • Acetylcholine
  • Norepinephrine