Abstract
Some antagonists exhibit tissue selectivity in their pharmacological antagonism of muscarinic responses1. However, the affinity constants for equilibrium binding of classical antagonists to muscarinic receptors in subcellular preparations have shown only small variations in different peripheral tissues and regions of the brain2–6. The binding curves do not deviate significantly from the simple Langmuir isotherm, indicating apparent homogeneity of the receptor population in any given region 5–8. In contrast, heterogeneity has been detected by agonist binding studies8,9 but this may arise from different environmental or coupling restraints on the agonist-induced conformational change10,11 and cannot be taken as evidence for different receptor subtypes. We report here binding studies using a new anti-muscarinic drug, pirenzepine, in which we found heterogeneity of binding that correlates well with the pharmacological activity.
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Hammer, R., Berrie, C., Birdsall, N. et al. Pirenzepine distinguishes between different subclasses of muscarinic receptors. Nature 283, 90–92 (1980). https://doi.org/10.1038/283090a0
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DOI: https://doi.org/10.1038/283090a0
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