α2-Adrenoceptors and 5-HT receptors mediate the antinociceptive effect of new pyrazolines, but not of dipyrone

Godoy, Maria Celoni M; Fighera, Michele Rechia; Souza, Fabiane R; Flores, Ariane Ethur; Rubin, Maribel Antonello; Oliveira, Marli R.; Zanatta, Nilo; Martins, Marcos A. P.; Bonacorso, Hélio G.; Mello, Carlos Fernando

doi:10.1016/j.ejphar.2004.05.045

Cited by 62 publications

(37 citation statements)

References 24 publications

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“…The findings obtained in this investigation proved the hypothesis that the tested triazole-pyrazoline derivative compounds have significant antinociceptive activities in mice and supported the previous studies reporting the analgesic activities of the compounds containing triazole and/or pyrazoline groups (Turan-Zitouni et al, 2001;Godoy et al, 2004;Tabarelli et al, 2004;Dündar et al, 2007;Salgin-Gökşen et al, 2007;Milano et al, 2008;Kaplancıklı et al, 2009;Karthikeyan, 2009;Girisha et al, 2010). …”

Section: Resultssupporting

confidence: 77%

“…Inhibition of cyclo-oxygenase activity and arachidonic acid cascade and reduction in the synthesis of peripherally formed prostaglandins have been suggested as some probable peripheral mechanisms underlying the analgesic and anti-inflammatory effects of pyrazoline derivatives (Tabarelli et al, 2004). Besides peripherally mediated antinociceptive action, centrally mediated antinociceptive activities have also been reported for some pyrazoline derivative compounds (Godoy et al, 2004;Tabarelli et al, 2004;Milano et al, 2008;Kaplancıklı et al, 2009;Girisha et al, 2010). Activation of opioidergic system (Tabarelli et al, 2004;Prokopp et al, 2006;Milano et al, 2008;Kaplancıklı et al, 2009), decrease of on/off cell firing in the periaqueductal gray (Tabarelli et al, 2004), and activation of spinal serotonergic and adrenergic systems (Godoy et al, 2004) have been suggested as possible mechanisms of central analgesic action.…”

Section: Introductionmentioning

confidence: 99%

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Antinociceptive activities of some triazole and pyrazoline moieties-bearing compounds

2011

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This study was designed to evaluate the potential antinociceptive activities of some triazole-pyrazoline derivatives. All of the test compounds (100 mg/kg) increased the reaction times of mice in hotplate and tailclip tests and decreased the total licking times of animals at both phases of formalin test. Compounds 3a, 3b, and 3c were more potent than the others in all nociception tests. None of the test compounds changed the spontaneous locomotor activities of animals. The findings obtained in this study supported the results of previous studies reporting the analgesic activities of triazole and/or pyrazoline derivatives.

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Section: Resultssupporting

confidence: 77%

Section: Introductionmentioning

confidence: 99%

Antinociceptive activities of some triazole and pyrazoline moieties-bearing compounds

2011

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“…The reduction, inhibition of production or antagonism of interleukin-5 was not associated with a decrease on neurogenic pain [42][43][44][45][46], justifying the fact that ellagic acid is Values are mean ± SEM (n = 9) of differences in weight between right and left ear plugs a P \ 0.01, b P \ 0.001 when compared with vehicle control group (ANOVA, Tukey's post hoc test) ineffective in neurogenic pain although it reduces production of interleukin-5 [47].…”

Section: Discussionmentioning

confidence: 63%

Antinociceptive effect of Lafoensia pacari A. St.-Hil. independent of anti-inflammatory activity of ellagic acid

et al. 2011

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This study was performed to determine the antinociceptive and anti-inflammatory activities of ethanolic extract of Lafoensia pacari A. St.-Hil. (PEtExt) stem bark and its fractions using various animal models such as acetic acid-induced abdominal writhing, formalin-induced pain and croton oil-induced ear edema tests. The PEtExt inhibited the acetic acid-induced abdominal writhing, reduced the pain reaction time on both phases of the formalin test and decreased the edema in a dose-dependent manner. Pre-treatment with naloxone did not reverse the antinociceptive effect. Only the ethyl acetate fraction showed antinociceptive and anti-inflammatory effects. Our results also showed that this extract contains compounds with analgesic action independent of anti-inflammatory activity.

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“…Regarding this point, it is interesting that while the anti-inflammatory properties of pyrazolederived compounds have been associated with the presence of carbonyl groups at positions 3 and/or 5 of the pyrazole moiety (11), a limited amount of information is available about the effect of substitutions in the pyrazole ring on the antinociceptive action of pyrazole derivatives. Indeed, pyrazole-derived compounds lacking such carbonyl groups have little or no anti-inflammatory activity, but some of them present a significant antinociceptive action (4,5,12,13). Accumulated evidence in the literature and in studies by our group suggests that the presence of a phenyl group at the 1 position of the pyrazole ring increases antinociceptive activity (7).…”

mentioning

confidence: 89%

A pyrazolyl-thiazole derivative causes antinociception in mice

Prokopp

Rubin

Sauzem

et al. 2006

Braz J Med Biol Res

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The present study investigates the antinociceptive effect of the pyrazolyl-thiazole derivative 2-(5-trichloromethyl-5-hydroxy-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)-4-(4-bromophenyl)-5-methylthiazole (B50) in mice. Male albino Swiss mice (30-40 g) were used in the acetic acid-induced abdominal writhes and tail-immersion tests. B50 caused dose-dependent antinociception (8, 23 and 80 µmol/kg, sc) in the acetic acid writhing assay (number of writhes: vehicle: 27.69 ± 6.15; B50 (8 µmol/kg): 16.92 ± 3.84; B50 (23 µmol/kg): 13.85 ± 3.84; B50 (80 µmol/kg): 9.54 ± 3.08; data are reported as means ± SEM for 9 animals per group). On the other hand, B50 did not cause antinociception in the tail immersion assay. Naloxone (2.75 µmol/kg, sc) prevented B50-induced antinociception (number of writhes: vehicle-saline: 31.11 ± 3.15; vehicle-naloxone: 27.41 ± 3.70; B50 (80 µmol/kg)-saline: 8.70 ± 3.33; B50 (80 µmol/kg)-naloxone: 31.84 ± 4.26; morphine-saline: 2.04 ± 3.52; morphine-naloxone: 21.11 ± 4.26; 8-9 animals per group). The removal of the methyl group of the thiazole ring of B50 or substitution of the bromo substituent with the methyl at position 4 of the phenyl group, which is attached to the thiazole ring of B50, resulted in loss of activity, suggesting that these substituents are important for antinociceptive activity. B50 had no effect on spontaneous locomotion or rotarod performance, indicating that the antinociceptive effect of B50 is not related to nonspecific motor effects. The antinociceptive profile of B50 seems to be closer to nonsteroidal anti-inflammatory drugs than to classic opioid agents, since it had no analgesic effect in a thermally motivated test. Key wordsThe pyrazole ring is a heterocycle compound containing two contiguous nitrogen atoms and three carbon atoms. Until 1995, in a few cases, only 5-trifluoromethyl-5-hydroxy-1H-pyrazolines and pyrazolidines could be synthesized, and pyrazolines other than 5-trifluoromethylated ones had been detected only by special nuclear magnetic resonance techniques (1). In 1999, Bonacorso et al. (2) described for the first time the synthesis and structural elucidation by nuclear magnetic resonance, Austin Model 1 calculations and X-ray diffraction of a novel series of twelve 3-aryl(alkyl)-5-hydroxy-1-

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α2-Adrenoceptors and 5-HT receptors mediate the antinociceptive effect of new pyrazolines, but not of dipyrone

Cited by 62 publications

References 24 publications

Antinociceptive activities of some triazole and pyrazoline moieties-bearing compounds

Antinociceptive activities of some triazole and pyrazoline moieties-bearing compounds

Antinociceptive effect of Lafoensia pacari A. St.-Hil. independent of anti-inflammatory activity of ellagic acid

A pyrazolyl-thiazole derivative causes antinociception in mice

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