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Table of Contents
Vol. 67, No. 4, 2003
Issue release date: April 2003
Section title: Review
Pharmacology 2003;67:182–194
(DOI:10.1159/000068404)

Profound, Non-Opioid Analgesia Produced by the High-Efficacy 5-HT1A Agonist F 13640 in the Formalin Model of Tonic Nociceptive Pain

Bardin L. · Tarayre J.P. · Malfetes N. · Koek W. · Colpaert F.C.
Centre de Recherche Pierre-Fabre, Castres, France

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Article / Publication Details

First-Page Preview
Abstract of Review

Received: October 05, 2002
Accepted: October 31, 2002
Published online: March 05, 2003
Issue release date: April 2003

Number of Print Pages: 13
Number of Figures: 5
Number of Tables: 5

ISSN: 0031-7012 (Print)
eISSN: 1423-0313 (Online)

For additional information: http://www.karger.com/PHA

Abstract

Previously, we have reported that in rat models of chronic pain, in particular, the very-high-efficacy 5-HT1A agonist F 13640 induces unprecedented pain relief by novel neuroadaptative mechanisms that involve inverse tolerance and cooperation with nociceptive stimulation in producing analgesia. The present studies detailed the actions of F 13640 and other compounds in the formalin model of tonic nociceptive pain. Intraperitoneal injection of F 13640 (0.01–2.5 mg/kg; t –15 min) caused a dose-dependent and complete inhibition of the paw elevation and paw licking that occurred both early (0–5 min) and late (22.5–27.5 min) after the intraplantar injection of diluted formaldehyde (2.5%) in the rat. The extent to which F 13640 and other 5-HT1A receptor ligands inhibited these pain behaviors correlated (p < 0.05) with the extent to which they activated 5-HT1A receptors. Under similar conditions, some inhibitory effects were also observed with various agents that are known to produce analgesia by different peripheral and/or central mechanisms (e.g., opioids, NA/5-HT reuptake inhibitors, COX-2 inhibitors and other nonsteroidal anti-inflammatory drugs, gabapentin, and ABT-594). However, with the possible exception of morphine, the effects of all of these agents at nontoxic doses were lower than those of F 13640, in particular in inhibition of early paw elevation. The 5-HT1A antagonist WAY 100635, but not naloxone, antagonized the actions of F 13640. These results help to establish large-magnitude 5-HT1A receptor activation as a new molecular mechanism of profound, central analgesia and suggest that F 13640 may be particularly effective against pain arising from severe tonic nociceptive stimulation.

© 2003 S. Karger AG, Basel


Article / Publication Details

First-Page Preview
Abstract of Review

Received: October 05, 2002
Accepted: October 31, 2002
Published online: March 05, 2003
Issue release date: April 2003

Number of Print Pages: 13
Number of Figures: 5
Number of Tables: 5

ISSN: 0031-7012 (Print)
eISSN: 1423-0313 (Online)

For additional information: http://www.karger.com/PHA


Copyright / Drug Dosage / Disclaimer

Copyright: All rights reserved. No part of this publication may be translated into other languages, reproduced or utilized in any form or by any means, electronic or mechanical, including photocopying, recording, microcopying, or by any information storage and retrieval system, without permission in writing from the publisher or, in the case of photocopying, direct payment of a specified fee to the Copyright Clearance Center.
Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in government regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug.
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