Autoradiographic Localization of Subtypes of Muscarinic Agonist and Antagonist Binding Sites: Alterations Following CNS Lesions

  • D. R. Gehlert
  • H. I. Yamamura
  • W. R. Roeske
  • J. K. Wamsley
Part of the Advances in Behavioral Biology book series (ABBI, volume 30)


The use of radiolabelled ligands, specific for muscarinic receptors, has allowed the demonstration of several subtypes of muscarinic receptors. Agonists have been postulated to bind to three distinct affinity states which are believed to be different conformational states of the same receptor (4, 6, 7), while classical muscarinic antagonists are believed to bind to all of these agonist states with equal high affinity. However, the non-classical muscarinic antagonist pirenzepine has been shown to have selective antagonism in both the clinic and the laboratory. Low doses of pirenzepine will reduce gastric secretion with little effect on salivation, gut motility, ciliary muscle function in the eye, or vagal tone in the heart (20, 21, 25). Experimentally, pirenzepine has been found to selectively bind with high affinity to a dense receptor population in membrane preparations from several organs including parts of the brain and peripheral ganglia (42, 47; Yamamura et al., this book), while binding to a very low density of receptors in other peripheral organs, such as smooth muscle and heart (3, 42). The selective nature of pirenzepine binding has led to the postulation of two separate muscarinic receptors designated as M1 and M2 (17, 23, 43).


Muscarinic Receptor Thiamine Deficiency Ventral Horn Muscarinic Agonist High Affinity Site 
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Copyright information

© Plenum Press, New York 1986

Authors and Affiliations

  • D. R. Gehlert
    • 1
  • H. I. Yamamura
    • 2
  • W. R. Roeske
    • 2
  • J. K. Wamsley
    • 1
  1. 1.Departments of Psychiatry and PharmacologyUniversity of Utah School of MedicineSalt Lake CityUSA
  2. 2.Departments of Pharmacology, Biochemistry, Psychiatry, Internal Medicine and the Arizona Research LaboratoriesUniversity of Arizona Health Sciences CenterTucsonUSA

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