Group-Specific Reagents as Probes for Measuring Agonist-Mediated Conformational Changes of β-Adrenergic and Muscarinic Acetylcholine Receptors

  • Georges Vauquelin
  • Serge Bottari
Part of the Methodological Surveys in Biochemistry and Analysis book series (MSBA, volume 13)


This article deals especially with radioligand studies performed in conjunction with group-specific reagents as probes for determining receptor conformational status, this being an aspect of agonist-mediated excitation and of ‘population’ diversity. One such probe is the alkylating agent N-ethylmaleimide (NEM). It causes, with agonists present, inactivation of β-adrenergic receptors and affinity changes in muscarinic receptors. The approaches and the results obtainable are exemplified first for β-adrenergic receptors, e.g. with turkey erythrocytes and human adipose membranes, and then for muscarinic receptor sites (‘RH’ and ‘RL’ in particular) in rat forebrain. The approaches are potentially applicable to other hormone or neurotransmitter types of receptor.


Muscarinic Receptor Equilibrium Dissociation Constant Adenylate Cyclase System Agonist Affinity Receptor Inactivation 
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Copyright information

© Plenum Press, New York 1984

Authors and Affiliations

  • Georges Vauquelin
    • 1
  • Serge Bottari
    • 2
  1. 1.Laboratory of Protein Chemistry, Institute of Molecular BiologyFree University Brussels (V.U.B.)St. Genesius-RodeBelgium
  2. 2.Laboratory of Gynecology and Obstetrics, Hopital Universitaire BrugmannFree University BrusselsBrusselsBelgium

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