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Titolo:
Peripheral effects of the kappa-opioid agonist EMD 61753 on pain and inflammation in rats and humans
Autore:
Machelska, H; Pfluger, M; Weber, W; Piranvisseh-Volk, M; Daubert, JD; Dehaven, R; Stein, C;
Indirizzi:
Free Univ Berlin, Klinikum Benjamin Franklin, Klin Anaesthesiol & Operative Free Univ Berlin Berlin Germany D-12200 n, Klin Anaesthesiol & Operative Johns Hopkins Univ, Dept Anesthesiol & Crit Care Med, Baltimore, MD USA Johns Hopkins Univ Baltimore MD USA l & Crit Care Med, Baltimore, MD USA NIDA, Preclin Pharmacol Lab, Intramural Res Program, NIH, Baltimore, MD USA NIDA Baltimore MD USA ab, Intramural Res Program, NIH, Baltimore, MD USA Univ Munich, Dept Anesthesiol, Munich, Germany Univ Munich Munich Germany iv Munich, Dept Anesthesiol, Munich, Germany Adolor Corp, Malvern, PA USA Adolor Corp Malvern PA USAAdolor Corp, Malvern, PA USA
Titolo Testata:
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
fascicolo: 1, volume: 290, anno: 1999,
pagine: 354 - 361
SICI:
0022-3565(199907)290:1<354:PEOTKA>2.0.ZU;2-I
Fonte:
ISI
Lingua:
ENG
Soggetto:
NMDA RECEPTOR ANTAGONIST; ADJUVANT ARTHRITIS; MORPHINE; OPIATE; INVOLVEMENT; MODULATION; MECHANISMS; ANALGESIA; PEPTIDES; MODEL;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
31
Recensione:
Indirizzi per estratti:
Indirizzo: Machelska, H Free Univ Berlin, Klinikum Benjamin Franklin, Klin Anaesthesiol & Operative Free Univ Berlin Hindenburgdamm 30 Berlin Germany D-12200 ve
Citazione:
H. Machelska et al., "Peripheral effects of the kappa-opioid agonist EMD 61753 on pain and inflammation in rats and humans", J PHARM EXP, 290(1), 1999, pp. 354-361

Abstract

The objective of the present study was to evaluate the effects of EMD 61753 (asimadoline), a K-opioid receptor agonist with restricted access to the central nervous system, on postoperative pain in patients who underwent knee surgery and on nociceptive thresholds and inflammation in rats treated with Freund's complete adjuvant. Patients treated with EMD 61753 (10 mg p.o.)tended to report an increase in pain, as evaluated by a visual analog scale and by the time to the first request for and the total amount of supplemental analgesic medication. The global tolerability of EMD 61753 was assessed as significantly inferior to that of a placebo by the investigator. In rats, the bilateral intraplantar (i.pl.) injection of EMD 61753 (0.1-3.2 mg) resulted in dose-dependent antinociception in both inflamed and noninflamedpaws, with a peak at 5 min after injection, as evaluated by the paw pressure method. However, at later time points (1 h-4 days), a significant decrease in the paw pressure threshold was observed, confirming its tendency toward a hyperalgesic action in humans. This was accompanied by an increase in paw volume and paw temperature, with a peak at 6 h after injection. EMD 61753 (1.6 mg)-induced analgesia was blocked by the peripheral opioid receptorantagonist naloxone methiodide (2.5-10 mg/kg s.c.) and by the kappa-receptor antagonist nor-binaltorphimine (0.1 mg; i.pl.). In contrast, EMD 61753 (1.6 mg)-induced hyperalgesia and increases in paw volume and paw temperature were blocked neither by naloxone methiodide (10-40 mg/kg s.c.) nor by dizocilpine maleate (0.003-0.009 mg i,pl.), a N-methyl-D-aspartic acid receptor antagonist. These data show differentially mediated peripheral actions ofEMD 61753: K-opioid receptor-induced analgesia and nonopioid, non-N-methyl-D-aspartic acid hyperalgesic and proinflammatory effects.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/04/20 alle ore 00:22:52