Pharmacological characterization of the muscarinic receptors mediating contraction of canine saphenous vein

J Auton Pharmacol. 1995 Dec;15(6):437-41. doi: 10.1111/j.1474-8673.1995.tb00408.x.

Abstract

1. The muscarinic receptor subtype mediating contraction of the canine saphenous vein has been characterized using a range of muscarinic agonists and subtype-selective antagonists. 2. Oxotremorine M and (+)-cis-dioxolane behaved as full agonists, while in comparison L-660,863 ((+/-)-3-(3-amino-1,2,4-oxadiazole-5-yl)quinuclidine) acted as a partial agonist. SDZ ENS 163 (thiopilocarpine), pilocarpine and McN-A-343 (0.1 microM-0.3 mM) did not elicit a response. The profile of agonist potencies suggests a low receptor reserve for contraction. 3. The rank order of antagonist apparent affinities was 4-DAMP (4-diphenylacetoxy-N-methylpiperidine methiodide; 8.41) > pirenzepine (8.10) > himbacine (7.34) > or = p-F-HHSiD (para-fluoro-hexahydrosiladifenidol; 7.15) > methoctramine (6.23). This antagonist apparent affinity profile is consistent with the activation of muscarinic M1 receptors.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Dioxolanes / pharmacology*
  • Dogs
  • Female
  • In Vitro Techniques
  • Muscarinic Agonists / pharmacology*
  • Muscle Contraction
  • Muscle, Smooth, Vascular / drug effects*
  • Muscle, Smooth, Vascular / metabolism
  • Oxotremorine / pharmacology*
  • Piperidines / metabolism
  • Pirenzepine / metabolism
  • Receptor, Muscarinic M1
  • Receptors, Muscarinic / drug effects*
  • Receptors, Muscarinic / physiology
  • Saphenous Vein / drug effects*
  • Saphenous Vein / metabolism

Substances

  • Dioxolanes
  • Muscarinic Agonists
  • Piperidines
  • Receptor, Muscarinic M1
  • Receptors, Muscarinic
  • Pirenzepine
  • Oxotremorine
  • 4-diphenylacetoxy-1,1-dimethylpiperidinium