Antinociceptive effect and mechanism of action of isatin, N-methyl isatin and oxopropyl isatin in mice.

Autor: Giorno TBS; Universidade Federal do Rio de Janeiro, Instituto de Ciências Biomédicas, Laboratório de Farmacologia da Dor e da Inflamação, Brasil., Silva BVD; Universidade Federal do Rio de Janeiro, Instituto de Química-CT, Bloco A. Rio de Janeiro, Brasil., Pinto ADC; Universidade Federal do Rio de Janeiro, Instituto de Química-CT, Bloco A. Rio de Janeiro, Brasil., Fernandes PD; Universidade Federal do Rio de Janeiro, Instituto de Ciências Biomédicas, Laboratório de Farmacologia da Dor e da Inflamação, Brasil. Electronic address: patricia.dias@icb.ufrj.br.
Jazyk: angličtina
Zdroj: Life sciences [Life Sci] 2016 Apr 15; Vol. 151, pp. 189-198. Date of Electronic Publication: 2016 Feb 13.
DOI: 10.1016/j.lfs.2016.02.052
Abstrakt: Aims: There has been growing interest in the synthesis of new derivatives from isatin, found in Isatis genus. Our objectives were to characterize the antinociceptive mechanism of action of isatin, N-methyl-isatin (MI) and N-methyl-3-(2-oxopropyl)-3-hydroxy-2-oxindole (MOI).
Materials and Methods: Substances (0.1-10mg/kg, p.o.) were studied in chemical (paw licking induced by formalin, capsaicin or glutamate) or thermal (hot plate) models of nociception. The involvement of several systems was evaluated using different receptor antagonists.
Key Findings: All three substances inhibit both phases of formalin-induced licking, increase the area under the curve and MI and MOI have a higher effect than that of morphine (in hot plate). Capsaicin and glutamate-induced licking were also reduced by all three substances. In the hot plate model, the antinociceptive effect of isatin was reduced by naloxone and atropine; naloxone, atropine and L-NAME reduced MI effect while naloxone, atropine, L-NAME, mecamylamine and ondansetron reduced MOI effect.
Significance: Our results suggest that isatin, MI and MOI: 1) present activity in models of nociception; 2) capsaicin and glutamate receptors seems to participate in the mechanism of action; 3) opioid, cholinergic, serotoninergic, nitrergic and adrenergic systems may be involved, at least in part, in the mechanism of action of some of these substances.
(Copyright © 2016 Elsevier Inc. All rights reserved.)
Databáze: MEDLINE
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