JOURNAL HOME CME HOME THIS MONTH PAST ISSUES ETOC COLLECTIONS
AUTHORS REVIEWERS EDITORIAL BOARD FEEDBACK RSS HELP
A&A International Anesthesia Research Society
QUICK SEARCH:   [advanced]


     

This Article
Right arrow Full Text
Right arrow Full Text (PDF)
Right arrow Alert me when this article is cited
Right arrow Alert me if a correction is posted
Services
Right arrow Email this article to a colleague
Right arrow Similar articles in this journal
Right arrow Similar articles in ISI Web of Science
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via ISI Web of Science (2)
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Wittmann, M.
Right arrow Articles by Barann, M.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Wittmann, M.
Right arrow Articles by Barann, M.
Related Collections
Right arrow Pharmacology

Anesth Analg 2006;103:747-752
© 2006 International Anesthesia Research Society
doi: 10.1213/01.ane.0000229706.84471.4d

ANALGESIA

The Effects of Morphine on Human 5-HT3A Receptors

Maria Wittmann, MD, I. Peters, MS, T. Schaaf, MS, H. C. Wartenberg, MD, S. Wirz, MD, J. Nadstawek, MD, B. W. Urban, PhD, and M. Barann, PhD

From the Klink und Poliklinik für Anästhesiologie und Operative Intensivmedizin, Universitätskliniken Bonn, Bonn, Germany.

Address correspondence and reprint requests to Dr. med. Maria Wittmann, Universitätskliniken Bonn, Sigmund-Freud-Straße-Str. 25 D-53105, Bonn, Germany. Address e-mail to maria.wittmann{at}gmx.de.

Abstract

5-HT3 receptors are ligand-gated ion channels that are involved in the modulation of emesis and pain. In this study, we investigated whether the opioid analgesic, morphine, exerts specific effects on human 5-HT3 receptors. Whole-cell patches from HEK-293 cells stably transfected with the human 5-HT3A receptor cDNA were used to determine the effects of morphine on the 5-HT-induced currents using the patch clamp technique. At negative membrane potentials, 5-HT induced inward currents in a concentration-dependent manner. The 5-HT3 receptor antagonist, ondansetron, (0.3 nM) reversibly inhibited the 5-HT-induced signals. Morphine reversibly suppressed 5-HT-induced peak currents as a function of concentration (IC50 = 1.1 µM, Hill coefficient = 1.2). The block by morphine decreased with increasing 5-HT concentrations, suggesting a competitive effect. In addition, the activation, as well as the inactivation, kinetics of the currents were significantly slowed in the presence of morphine. The morphine antagonist, naloxone, also inhibited 5-HT-induced currents (e.g., at 3 µM by 17%). The effects of morphine and naloxone were not additive. The potency of morphine and the competitivity of the blocking effect points to a specific mechanism at a receptor site rather than an unspecific membrane effect.




This article has been cited by other articles:


Home page
 Anesth. Analg.Home page
M. Wittmann, T. Schaaf, I. Peters, S. Wirz, B. W. Urban, and M. Barann
The Effects of Fentanyl-Like Opioids and Hydromorphone on Human 5-HT3A Receptors
Anesth. Analg., July 1, 2008; 107(1): 107 - 112.
[Abstract] [Full Text] [PDF]

Home page
 Anesth. Analg.Home page
M. Barann, I. Linden, S. Witten, and B. W. Urban
Molecular Actions of Propofol on Human 5-HT3A Receptors: Enhancement as Well as Inhibition by Closely Related Phenol Derivatives
Anesth. Analg., March 1, 2008; 106(3): 846 - 857.
[Abstract] [Full Text] [PDF]


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 © 2006 by the International Anesthesia Research Society.