RefDoc
Haut

Faire une nouvelle recherche
Make a new search
Lancer la recherche


Titre du document / Document title

Pharmacological assessment of the rat formalin test utilizing the clinically used analgesic drugs gabapentin, lamotrigine, morphine, duloxetine, tramadol and ibuprofen : Influence of low and high formalin concentrations

Auteur(s) / Author(s)

MUNRO Gordon (1) ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

(1) Department of Pharmacology, NeuroSearch A/S, 93 Pederstrupvej, 2750, Ballemp, DANEMARK

Résumé / Abstract

The formalin test is used as a primary behavioural screen for assaying the antinociceptive activity of compounds in laboratory rodents. After hindpaw formalin injection, nociceptive behaviours are expressed in a biphasic pattern and correlate closely with the concentration of formalin injected. Here, the antinociceptive efficacy of six compounds used in the clinical treatment of chronic pain was compared in rats injected with either 1% or 5% formalin. Predictably, the anti-inflammatory drug ibuprofen (30-300 mg/kg) attenuated second phase (16-40 min) nociceptive behaviours in 5% formalin-injected rats; 1% formalin-injected rats were unaffected. The anti-epileptic drugs gabapentin (50-200 mg/kg) and lamotrigine (10-60 mg/kg) were antinociceptive only during second phase in both 1% and 5% tests. Notably, they were 2-4 times more potent in 1% vs 5% formalin-injected rats. The dual monoamine reuptake inhibitor duloxetine (3-60 mg/kg) consistently attenuated nociceptive behaviours during first phase and interphase in both tests. However second phase nociception was only attenuated in 5% formalin-injected rats giving rise to a 6 fold increase in potency compared with 1% formalin-injected rats. The μ-opioid receptor agonist morphine (1-6 mg/kg) and the combined μ-opioid receptor agonist/monoamine reuptake inhibitor tramadol (5-50 mg/kg) both attenuated nociceptive behaviours throughout the duration of both the 1% and 5% tests; no difference in antinociceptive potency occurred for either compound during second phase. Thus, for mechanistically-distinct compounds the predictive antinodceptive capacity of the formalin test can vary with the concentration of formalin injected, likely as a result of peripheral and central nociceptive signalling mechanisms being differentially engaged.

Revue / Journal Title

European journal of pharmacology    ISSN  0014-2999   CODEN EJPHAZ 

Source / Source

2009, vol. 605, no1-3, pp. 95-102 [8 page(s) (article)] (1 p.)

Langue / Language

Anglais

Editeur / Publisher

Elsevier, Amsterdam, PAYS-BAS  (1967) (Revue)

Mots-clés anglais / English Keywords

Neurotransmitter

;

Catecholamine

;

Enzyme

;

Oxidoreductases

;

Prostaglandin-endoperoxide synthase

;

Enzyme inhibitor

;

Arylpropionic acid derivatives

;

Serotonin

;

Norepinephrine

;

Reuptake inhibitor

;

Opiates

;

Triazine derivatives

;

Vertebrata

;

Mammalia

;

Rodentia

;

Non steroidal antiinflammatory agent

;

Antidepressant agent

;

Psychotropic

;

Anticonvulsant

;

Narcotic analgesic

;

Pain

;

Nociception

;

Hyperalgesia

;

Sensitization

;

Analgesia

;

Ibuprofen

;

Tramadol

;

Duloxetine

;

Morphine

;

Lamotrigine

;

Gabapentin

;

Drug

;

Rat

;

Animal

;

Evaluation

;

Mots-clés français / French Keywords

Neurotransmetteur

;

Catécholamine

;

Enzyme

;

Oxidoreductases

;

Prostaglandin-endoperoxide synthase

;

Inhibiteur enzyme

;

Dérivé de l'acide arylpropionique

;

Sérotonine

;

Noradrénaline

;

Inhibiteur recapture

;

Opiacés

;

Dérivé de la triazine

;

Vertebrata

;

Mammalia

;

Rodentia

;

Antiinflammatoire non stéroïde

;

Antidépresseur

;

Psychotrope

;

Anticonvulsivant

;

Analgésique narcotique

;

Douleur

;

Nociception

;

Hyperalgésie

;

Sensibilisation

;

Analgésie

;

Ibuprofène

;

Tramadol

;

Duloxétine

;

Morphine

;

Lamotrigine

;

Gabapentine

;

Médicament

;

Rat

;

Animal

;

Evaluation

;

Mots-clés espagnols / Spanish Keywords

Neurotransmisor

;

Catecolamina

;

Enzima

;

Oxidoreductases

;

Prostaglandin-endoperoxide synthase

;

Inhibidor enzima

;

Arilpropionico ácido derivado

;

Serotonina

;

Noradrenalina

;

Inhibidor recaptura

;

Opiados

;

Triazina derivado

;

Vertebrata

;

Mammalia

;

Rodentia

;

Antiinflamatorio no esteroide

;

Antidepresor

;

Psicotropo

;

Anticonvulsivante

;

Analgésico narcotico

;

Dolor

;

Nocicepción

;

Hiperalgesia

;

Sensibilización

;

Analgesia

;

Ibuprofeno

;

Tramadol

;

Duloxetina

;

Morfina

;

Lamotrigina

;

Gabapentina

;

Medicamento

;

Rata

;

Animal

;

Evaluación

;

Mots-clés d'auteur / Author Keywords

Analgesia

;

Central sensitization

;

Hyperalgesia

;

Nociception

;

Pain

;

Localisation / Location

INIST-CNRS, Cote INIST : 13322, 35400018742511.0150

Nº notice refdoc (ud4) : 21279008



Faire une nouvelle recherche
Make a new search
Lancer la recherche
Bas