![[Feedback]](/icons/banner/feedbackACT.gif){kind=icon}
![[For Subscribers]](/icons/banner/subscriberACT.gif){kind=icon}
![[Archive]](/icons/banner/archiveACT.gif){kind=icon}
![[Search]](/icons/banner/searchACT.gif){kind=icon}
![[Contents]](/icons/banner/tocACT.gif){kind=icon}
|
|
|
|
|
||
T Pelissier, A Alloui, F Caussade, C Dubray, A Cloarec, J Lavarenne and A Eschalier
Equipe Neuro Psycho Pharmacologie Universite d'Auvergne, Faculte de Medecine, Clermont-Ferrand, France.
Rats (Sprague-Dawley), submitted to a mechanical noxious stimulus (paw pressure), were tested to determine 1) the antinociceptive effects of p.o. (200, 400 and 800 mg/kg), i.v. (50, 100, 200 and 300 mg/kg) and intrathecal (i.t.) (100 and 200 micrograms/rat) administrations of paracetamol; 2) the influence of i.t. administered tropisetron, a 5- hydroxytryptamine3 (5-HT3) receptor antagonist (0.5, 1 or 10 micrograms/rat) on paracetamol-induced antinociception; 3) the influence of indomethacin (25 mg/kg s.c.), naloxone (10 micrograms/rat i.t.) and yohimbine (1 mg/kg i.v.) on the effect of paracetamol (200 mg/kg i.v.) to determine the involvement of prostaglandins, opioids and alpha-2 adrenoceptors. The displacement by paracetamol of radioligand binding to various receptors was also investigated. Paracetamol induced a significant antinociceptive effect after p.o., i.v. and i.t. administration. A total inhibition of the effect of paracetamol, administered p.o. or i.t., occurred at the dose of 0.5 microgram/rat of tropisetron, whereas 10 micrograms/rat of this antagonist was needed to totally inhibit the action of i.v. administered paracetamol. Indomethacin, naloxone and yohimbine failed to modify paracetamol antinociceptive action. In vitro studies failed to show any binding of paracetamol to 5-HT3 and several other receptors and to 5-HT uptake sites. It is concluded that paracetamol has a central antinociceptive effect, based on an indirect involvement of spinal 5-HT3 receptors.
This article has been cited by other articles:
|
|
 |
|
  T. Ishida, T. Sato, M. Irifune, K.-i. Tanaka, N. Nakamura, and T. Nishikawa Effect of acetaminophen, a cyclooxygenase inhibitor, on Morris water maze task performance in mice J Psychopharmacol, September 1, 2007; 21(7): 757 - 767. [Abstract] [PDF]
|
|
|
|
 |
|
 E. D. Hogestatt, B. A. G. Jonsson, A. Ermund, D. A. Andersson, H. Bjork, J. P. Alexander, B. F. Cravatt, A. I. Basbaum, and P. M. Zygmunt Conversion of Acetaminophen to the Bioactive N-Acylphenolamine AM404 via Fatty Acid Amide Hydrolase-dependent Arachidonic Acid Conjugation in the Nervous System J. Biol. Chem., September 9, 2005; 280(36): 31405 - 31412. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 M. K. Herbert, R. Weis, P. Holzer, and N. Roewer Peristalsis in the Guinea Pig Small Intestine In Vitro Is Impaired by Acetaminophen but Not Aspirin and Dipyrone Anesth. Analg., January 1, 2005; 100(1): 120 - 127. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 F. Libert, J. Bonnefont, E. Bourinet, E. Doucet, A. Alloui, M. Hamon, J. Nargeot, and A. Eschalier Acetaminophen: A Central Analgesic Drug That Involves a Spinal Tropisetron-Sensitive, Non-5-HT3 Receptor-Mediated Effect Mol. Pharmacol., September 1, 2004; 66(3): 728 - 734. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 R. B. Raffa, D. J. Stone Jr., and R. J. Tallarida Discovery of "Self-Synergistic" Spinal/Supraspinal Antinociception Produced by Acetaminophen (Paracetamol) J. Pharmacol. Exp. Ther., October 1, 2000; 295(1): 291 - 294. [Abstract] [Full Text]
|
|
 |
 |
 |
|
 |
 |
 |
