Selective labelling of M1-receptors in autonomic ganglia with 3H-pirenzepine

Arzneimittelforschung. 1985;35(1A):325-8.

Abstract

Using the classical muscarinic antagonist 3H-N-methyl-scopolamine as radioligand and unlabelled pirenzepine (PZ) as displacing agent, a heterogeneous muscarinic receptor population consisting of about 70% M1-receptors and 30% M2-receptor, can be demonstrated in crude membranes of calf sympathetic ganglia. In the same preparation only low and variable specific binding is detectable when 3H-PZ is used as marker ligand. The situation clearly improves when synaptosomes are prepared from the ganglia. Then binding of 3H-PZ can be measured with a favourable specific to non specific binding ratio and with features compatible with the selective labelling of ganglionic M1-receptor sites. It is concluded that the 3H-PZ binding assay in synaptosomes of autonomic ganglia is a novel method for the characterization of the peripheral M1-receptor.

MeSH terms

  • Animals
  • Atropine / metabolism
  • Benzodiazepinones / metabolism*
  • Binding, Competitive
  • Cattle
  • Ganglia, Autonomic / metabolism*
  • Ganglia, Sympathetic / metabolism
  • In Vitro Techniques
  • N-Methylscopolamine
  • Pirenzepine
  • Quinuclidinyl Benzilate
  • Radioligand Assay
  • Receptors, Muscarinic / classification
  • Receptors, Muscarinic / metabolism*
  • Scopolamine Derivatives / metabolism
  • Synaptosomes / metabolism

Substances

  • Benzodiazepinones
  • Receptors, Muscarinic
  • Scopolamine Derivatives
  • Pirenzepine
  • Quinuclidinyl Benzilate
  • Atropine
  • N-Methylscopolamine