Muscarinic receptor heterogeneity in guinea pig intestinal smooth muscle: binding studies with AF-DX 116

Eur J Pharmacol. 1987 Sep 23;141(3):475-7. doi: 10.1016/0014-2999(87)90568-1.

Abstract

Muscarinic receptor subtypes in longitudinal and circular smooth muscles of the guinea pig ileum were characterized with the use of the cardioselective antagonist AF-DX 116 in binding competition experiments against 0.3 nM [3H] N-methylscopolamine [( 3H]NMS). This compound recognized a heterogeneous receptor population in both smooth muscles, revealing the existence of different percentages of the cardiac (KD = 92-110 nM) and the glandular (KD = 1150-2541 nM) muscarinic receptor subtypes. These results, together with the low potency displayed by AF-DX 116 to inhibit the agonist-stimulated smooth muscle contraction and salivary secretion allow the suggestion that the glandular muscarinic receptor subtype, showing a low affinity for AF-DX 116, is involved in smooth muscle contraction.

MeSH terms

  • Animals
  • Guinea Pigs
  • In Vitro Techniques
  • Male
  • Muscle, Smooth / drug effects
  • Muscle, Smooth / metabolism*
  • Myocardium / metabolism
  • Pirenzepine / analogs & derivatives*
  • Pirenzepine / metabolism
  • Receptors, Muscarinic / metabolism*
  • Salivary Glands / metabolism

Substances

  • Receptors, Muscarinic
  • Pirenzepine
  • otenzepad