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AFDX-116 discriminates between muscarinic M2 receptors of the heart and the iris smooth muscle

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Summary

Studies with the atypical muscarinic antagonist pirenzepine provide convincing evidence for the classification of muscarinic acetylcholine receptors (mAChRs) into two subtypes, M1 and M2. The present study examines the heterogeneity of the M2 subtype employing the newly developed competitive muscarinic antagonist, AFDX-116. Comparison of the binding affinities of pirenzepine, atropine, and AFDX-116 to mAChRs in microsomes from the rabbit cerebral cortex, heart, and iris smooth muscle shows that iris mAChRs, which are pharmacologically of the M2 subtype, can be distinguished from M2 cardiac receptors based on their affinity for AFDX-116. These results are consistent with the hypothesis that the M2 receptor subtype consists of a heterogeneous population of receptors.

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Abbreviations

mAChRs:

Muscarinic Acetylcholine Receptors

CCh:

Carbachol

NMS:

N-Methylscopolamine

AFDX-116:

11-[[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6Hpyrido[2,3-b][1,4]benzodiazepine-6-one

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Authors and Affiliations

  1. Department of Cell and Molecular Biology, Medical College of Georgia, 30912-2100, Augusta, GA, USA

    Richard E. Honkanen & Ata A. Abdel-Latif

Authors
  1. Richard E. Honkanen
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  2. Ata A. Abdel-Latif
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Honkanen, R.E., Abdel-Latif, A.A. AFDX-116 discriminates between muscarinic M2 receptors of the heart and the iris smooth muscle. Mol Cell Biochem 82, 131–135 (1988). https://doi.org/10.1007/BF00242528

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  • DOI: https://doi.org/10.1007/BF00242528

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