AF-DX 116 discriminates between muscarinic M2 receptors of the heart and vasculature |
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| Authors: | S P Duckles H I Yamamura V Lee |
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| Affiliation: | 1. Department of Pharmacology, College of Medicine, University of California, Irvine, California 92717, USA;2. Department of Pharmacology, College of Medicine, University of Arizona, Tucson, Arizona 85724, USA;1. Center for Species Survival, Smithsonian Conservation Biology Institute, National Zoological Park, 1500 Remount Road, Front Royal, VA 22630, United States;2. Department of Environmental Science and Policy, George Mason University, 4400 University Drive, Fairfax, VA 22030, United States;3. Interdisciplinary Studies, George Mason University, 4400 University Drive, Fairfax, VA 22030, United States;4. School of Integrative Studies, George Mason University, 4400 University Drive, Fairfax, VA 22030, United States;1. Los Alamos National Laboratory, Earth and Environmental Sciences, MS J966, Los Alamos, NM 87545, United States;2. University of California, Los Angeles, CA 90095, United States;3. Sandia National Laboratory, Albuquerque, NM 87185, United States;1. Boehringer Ingelheim Pharma GmbH und Co. KG, Binger Str. 173, 55216, Ingelheim am Rhein, Germany;2. Department of Technical Biochemistry, Technical University of Dortmund, Emil-Figge-Str. 66, 44227, Dortmund, Germany;3. Centre for Microbial Electrochemical Systems (CEMES), University of Queensland, Gehrmann Laboratories Building (60), Brisbane, QLD, 4072, Australia;4. Natural Products Laboratory, Institute of Biology, Leiden University, Sylviusweg 72, 2333 BE, Leiden, The Netherlands;1. Research Unit Analytical BioGeoChemistry, Helmholtz Zentrum München, German Research Center for Environmental Health, Ingolstaedter Landstrasse 1, 85764 Neuherberg, Germany;2. Laboratoire de Biologie Moléculaire de la Cellule, UMR5239 CNRS/ENS Lyon/UCBL/HCL, Ecole normale supérieure de Lyon 46, allée d’Italie, 69364 Lyon cedex 07, France;3. Chair of Analytical Food Chemistry, Technische Universität München, Alte Akademie 10, D-85354 Freising-Weihenstephan, Germany;1. Department of Pharmaceutical Sciences, University of Perugia, Via del Liceo, 1, 06128 Perugia, Italy;2. Institute of Biochemistry and Molecular Medicine, University of Bern, Bühlstrasse, 28, CH-3012 Bern, Switzerland |
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| Abstract: | The newly developed muscarinic antagonist, AF-DX 116, has been reported to have a higher affinity in vivo for muscarinic receptors in the heart than in the vasculature. Therefore two in vitro preparations, the rabbit ear artery and spontaneously beating right atrium, were compared. AF-DX 116 had a 29 times greater affinity for muscarinic receptors in the cardiac preparation than in the ear artery, with a pA2 in the heart of 7.42 compared to a value of 5.95 in the ear artery. Thus AF-DX 116 shows promise as an approach to differentiating sub-classes of muscarinic M2 receptors. |
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