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Anesth Analg 2003;97:1059-1063
© 2003 International Anesthesia Research Society

ANESTHETIC PHARMACOLOGY

Interactions of Edrophonium with Neostigmine in the Rat Trachea

Osamu Shibata, MD, Masataka Saito, MD, Maki Yoshimura, MD, Masakazu Yamaguchi, MD, Tetsuji Makita, MD, and Koji Sumikawa, MD

Department of Anesthesiology, Nagasaki University School of Medicine, Nagasaki, Japan

Address correspondence and reprints requests to Osamu Shibata, MD, Department of Anesthesiology, Nagasaki University School of Medicine, 1-7-1 Sakamoto, Nagasaki 852-8501, Japan. Address e-mail to opshiba{at}net.nagasaki-u.ac.jp

The muscarinic M3 receptor of airway smooth muscle has both an orthosteric binding site and an allosteric binding site. Edrophonium may bind to the allosteric site, resulting in the inhibition of the action of the orthosteric site. Therefore, we examined the effects of edrophonium on neostigmine-induced contractile and phosphatidylinositol responses of rat trachea. Neostigmine (100 µM in final concentration) was added, and ring tension was examined by the addition of edrophonium. After the completion of the experiment, Krebs-Henseleit (K-H) solution containing both edrophonium and neostigmine was changed three times with fresh K-H solution, and the tension was recorded. Tracheal slices were incubated with [3H]myo-inositol and 100 µM neostigmine in the presence or absence of edrophonium. The [3H]inositol monophosphate (IP1) was measured. Data were expressed as mean ± SE. Statistical significance (P < 0.05) was determined with analysis of variance. Neostigmine-induced tension and IP1 accumulation were attenuated by edrophonium at concentrations of 100 µM or more. This attenuation was reversed to more than 80% of control levels by washing with fresh K-H solution. The results suggest that edrophonium would bind to the allosteric site, resulting in the inhibition of the action of the orthosteric site of muscarinic M3 receptors of rat trachea.

IMPLICATIONS: We examined the effects of edrophonium on neostigmine-induced contractile and phosphatidylinositol responses of rat trachea. Neostigmine-induced tension and inositol monophosphate accumulation were attenuated by edrophonium. This attenuation was reversed by washing. The results suggest that edrophonium would bind to the allosteric site.






Lippincott, Williams & Wilkins Anesthesia & Analgesia® is published for the International Anesthesia Research Society® by Lippincott Williams & Wilkins with the assistance of Stanford University Libraries' HighWire Press®. Copyright 2006 by the International Anesthesia Research Society. Online ISSN: 1526-7598   Print ISSN: 0003-2999 HighWire Press
Copyright © 2003 by the International Anesthesia Research Society.