scholarly journals A Novel Antinociceptive Sulphated Polysaccharide of the Brown Marine Alga Spatoglossum Schroederi

2011 ◽  
Vol 6 (6) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Wladimir R. L. Farias ◽  
Paula Cristina W. C. Lima ◽  
Natália Velloso F. C. Rodrigues ◽  
Rômmulo Celly L. Siqueira ◽  
Renata M. F. Amorim ◽  
...  
Keyword(s):  
Marine Alga ◽  
Sugar Content ◽  
Antinociceptive Effect ◽  
Deae Cellulose ◽  
Brown Seaweed ◽  
Exchange Chromatography ◽  
Sulfated Polysaccharides ◽  
Second Phase ◽  
Hot Plate ◽  
Hot Plate Test

Sulfated polysaccharides (SP) of brown algae (Phaeophyta) are composed mainly of α- L-fucose, being classified as fucans, with recognized role in inflammation but not in nociception, which was already described for SP obtained from red algae. Here the SP of the brown marine alga S. schroederi (named Ss-SP) was isolated and assayed for the antinociceptive effect. Ss-SP was isolated by DEAE-cellulose, analyzed by agarose gel electrophoresis and evaluated in nociception models (Formalin, Hot plate, Von Frey) using Swiss mice (20-25g). Anion exchange chromatography provided four major fractions being F1 (Ss-SP) that of highest metachromatic activity and sugar content. Ss-SP inhibited both phases of the formalin test. In the first phase the paw licking (55.2±8.07s) was reduced by 45% (30.5±6.51s) and 40% (32.85±8.66s) at 0.1 and 1 μg/kg, respectively. In the second phase, Ss-SP was also inhibitory about 39%, but only at 1 mg/kg (83.0±15.70s) compared to formalin (136.8±10.27s). This inhibitory effect suggests a mixed mechanism similar to morphine, which was not confirmed in the hot plate test, a model of pain associated with central neurotransmission. However, Ss-SP reduced the animal reaction in response to stimulation withVon Frey filament at the 2nd and 3rd h (20.8±6.86% versus carrageenan: 47.9±5.83%; 33.3±7.71% versus carrageenan: 62.5±9.83%). Accordingly, the paw edema induced by carrageenan (0.08±0.01g) was potently reduced in 45.35% by Ss-SP pre-treatment (0.02±0.003g), corroborating the anti-inflammatory activity demonstrated for brown seaweed polysaccharides. In conclusion our data revealed for the first time the antinociceptive effect of Ss-SP which could be used as a new source of analgesic substances.

scholarly journals Enhancement of morphine-induced antinociception after electroconvulsive shock in mice

2021 ◽  
Vol 17 ◽  
pp. 174480692199262
Author(s):  
Ken Iwata ◽  
Yukio Takamatsu ◽  
Nagafumi Doi ◽  
Kazutaka Ikeda
Keyword(s):  
Dose Response ◽  
Response Curve ◽  
Antinociceptive Effect ◽  
Dose Response Curve ◽  
Expression Level ◽  
Morphine Injection ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test ◽  
Pain Patients

Electroconvulsive therapy (ECT) has been applied for chronic pain for decades. The amounts of opioids to treat pain are sometimes reduced after a series of ECT. The effect of ECT on morphine-induced analgesia and its mechanism underlying the reduction of morphine requirement has yet to be clarified. Therefore, we administered electroconvulsive shocks (ECS) to mice and investigated the antinociceptive effect of morphine in a hot plate test. We examined the expression level of µ-opioid receptor in the thalami of mice 25 h after administration of ECS compared to the thalami of mice without ECS administration using western blotting. ECS disturbed the development of a decrease in the percentage of maximal possible effect (%MPE), which was observed 24 h after a morphine injection, when ECS was applied 25, 23, 21, and 12 h before the second administration of morphine. We also examined the effect of ECS on the dose-response curve of %MPE to morphine-antinociception. Twenty-five hours after ECS, the dose-response curve was shifted to the left, and the EC50 of morphine given to ECS-pretreated mice decreased by 30.1% compared to the mice that were not pretreated with ECS. We also found that the expression level of µ-opioid receptors was significantly increased after ECS administration. These results confirm previous clinical reports showing that ECT decreased the required dose of opioids in neuropathic pain patients and suggest the hypothesis that this effect of ECT works through the thalamus.

Antinociceptive Effect of Clomipramine Through Interaction with Serotonin 5-Нт2 And 5-Нт3 Receptor Subtypes

Folia Medica ◽  
2012 ◽  
Vol 54 (4) ◽  
pp. 69-77 ◽  
Author(s):  
Ilia D. Kostadinov ◽  
Delian P. Delev ◽  
Ivanka I. Kostadinova
Keyword(s):  
Acetic Acid ◽  
Analgesic Effect ◽  
Antinociceptive Effect ◽  
Positive Control ◽  
Control Group ◽  
Receptor Subtypes ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test ◽  
Acid Test

Abstract INTRODUCTION: Tricyclic antidepressants are used in the treatment of various pain syndromes. The antidepressant clomipramine inhibits predominantly the reuptake of serotonin in the central nervous system. The mechanism of its analgesic effect is not fully understood. The AIM of the present study was to find experimentally any dose-effect dependence in the analgesic effect of clomipramine and the involvement of the 5-НТ2 and 5-НТ3 receptors in the mechanism of this effect. Material and methods: Fifty male Wistar rats were used in the study allocated to five groups (10 animals each): a saline treated control group, one positive control group treated with metamizole and three experimental groups treated with intraperitoneally administered clomipramine in doses of 5, 10 and 20 mg/kg bw, respectively. To study the role of 5-НТ2 and 5-НТ3 receptors in this effect we used another five groups (10 animals each): control, positive control and three experimental groups treated with clomipramine only, clomipramine and granisetrone and clomipramine and cyproheptadine, respectively. Three nociceptive tests were used: the hot plate test, analgesimeter and the acetic acid-induced writhing test. To gauge the antinociceptive action we used the increased latency in the hot plate test expressed as maximum possible effect % (%MPE), the increase in paw pressure to withdraw the hind paw in analgesimeter and decrease in the number of spinal cord writhes in the acetic acid test. RESULTS: Clomipramine in a dose of 20 mg/kg bw significantly increased the %MPE in hot plate test and the pressure to withdraw the hind paw in the analgesimeter when compared with the control. In the acetic acid test clomipramine decreased non-significantly the number of writhes compared with the controls. Granisetrone reduced non-significantly the antinociceptive effect of clomipramine in all tests. Cyproheptadine potentiated the analgesic effect of clomipramine in acetic acid test and decreased it significantly in the hot plate test. In analgesimeter cyproheptadine decreased significantly the paw pressure to withdraw the tested hind paw at 1 hour and non-significantly at 2 hours. CONCLUSION: Clomipramine in the dose of 20 mg/kg bw has a pronounced antinociceptive affect towards thermal and mechanical pain stimulation. The 5-HT2 and 5-HT3 receptor subtypes are very likely involved in the mechanism of this effect.

Effect of gender on antinociceptive effect of paroxetine in hot plate test in mice

2006 ◽  
Vol 30 (2) ◽  
pp. 292-296 ◽  
Author(s):  
Erdem N. Duman ◽  
Murat Kesim ◽  
Mine Kadioglu ◽  
Cunay Ulku ◽  
Nuri I. Kalyoncu ◽  
...  
Keyword(s):  
Antinociceptive Effect ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test

The mineralocorticoid receptor antagonist spironolactone enhances morphine antinociception

2013 ◽  
Vol 4 (4) ◽  
pp. 259-259
Author(s):  
Viljami Jokinen ◽  
Tuomas O. Lilius ◽  
Mikko S. Neuvonen ◽  
Antti J. Väänänen ◽  
Mikko O. Niemi ◽  
...  
Keyword(s):  
Antinociceptive Effect ◽  
Morphine Tolerance ◽  
Tail Flick ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Mineralocorticoid Receptor Antagonist ◽  
P Glycoprotein ◽  
Antinociceptive Effects ◽  
The Brain ◽  
Glycoprotein Inhibition

Abstract Aims Spironolactone, an antimineralocorticoid, has been reported to potentiate the cataleptic effect of morphine in the rat. Since no previous research exists on the matter and the interaction might be clinically significant, the effects of spironolactone on morphine antinociception and pharmacokinetics in the rat were investigated. Methods Male SD rats were used to assess the effects of spironolactone on acute morphine-induced antinociception, development of morphine tolerance, and established morphine tolerance in the tail-flick and hot plate tests. Spironolactone was also administered with loperamide to assess whether spironolactone enhances the brain distribution of the acknowledged P-glycoprotein substrate across the blood-brain barrier. Results Spironolactone had no antinociceptive effects of its own but when co-administrated with morphine the antinociceptive effect of morphine was greatly enhanced. Morphine concentrations in the brain were increased fourfold in the spironolactone co-administrated group. Spironolactone did not inhibit the formation of pro-nociceptive morphine-3-glucuronide, nor did inhibit the development of tolerance. The peripherally restricted opioid, loperamide, had no antinociceptive effects by itself, but co-administration with spironolactone produced a clear change in the hot plate test. Conclusions Although mineralocorticoids have been proposed to take part in pain signaling, in our setting spironolactone did not have antinociceptive properties of its own. The increased antinociceptive effect of morphine is apparently caused by the increased morphine brain concentrations. We suggest this to be due to P-glycoprotein inhibition, as indicated by the loperamide assay. The clinical relevance of P-glycoprotein inhibition by spironolactone should be studied.

scholarly journals Comparison the analgesic activity of watery suspension of Nigella sativa Linn. seeds with Naproxen in mice

2010 ◽  
Vol 9 (3) ◽  
pp. 56
Author(s):  
W. H. Al-Shebani, And F. J. Al-Tahan
Keyword(s):  
Reaction Time ◽  
Analgesic Activity ◽  
Nigella Sativa ◽  
Antinociceptive Effect ◽  
Analgesic Action ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test ◽  
The Third ◽  
Significant Increment

The present study was designed to investigated the antinociceptive effect of the waterysuspension of Nigella sativa seeds compared with that of Naproxen by using hot plate test, whichmainly measures the threshold of stimulus required to elicit a response , in mice at 30, 60, 90, 120minutes after administration of the test agents. Twenty four albino Swiss mice of either sex weredivided in four groups with (6) animals each, the first group was treated orally with 1000 mg/kgBW of watery suspension of Nigella seeds, the second group was treated orally with naproxen atdose of 500 mg/kg BW ,the third group drenched with 500mg/kg BW of watery suspension ofNigella seeds and 250 mg/kg BW of naproxen ,whereas the last group serve as control. Nigellasativa seeds suspension significantly (p<0.05) prolonged the latency of response at all posttreatmentobservation times (30, 60, 90 and 120 minutes) , the analgesic action of naproxen wasdiminished with time compared with Nigella seeds.Combination of equal amounts of Nigellaseeds and Naproxen (half the originally used doses) caused significant increment (p<0.05) ofanalgesic reaction time longer than shown by each agent when given alone indicating an obvioussynergistic effect between watery suspension of Nigella seeds and Naproxen.

COMPARATIVE STUDY OF THE ANTINOCICEPTIVE EFFECT OF ETIFOXINE AND RETIGABINE IN RATS

2018 ◽  
Vol 28 (2) ◽  
pp. 455-460
Author(s):  
Vesela Kokova ◽  
Elisaveta Apostolova ◽  
Lyudmil Peychev ◽  
Zhivko Zhivko ◽  
Kostadin Kanalev
Keyword(s):  
Potassium Channels ◽  
Antinociceptive Effect ◽  
Anticonvulsant Drug ◽  
Single Administration ◽  
Latency Time ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test ◽  
Withdrawal Latency ◽  
Low Threshold

Introduction: Etifoxine is a nonbenzodiazepine anxiolytic and anticonvulsant drug. It enhances GABAergic transmission directly by binding to β2 and/or β3 subunits of the GABAA receptor complex and indirectly via stimulation of neurosteroid production after the activation of 18 kDa translocator protein (TSPO). Retigabine is an anticonvulsant drug which activates low-threshold voltage-gated potassium channels. Anticonvulsant drugs reduce hyperexcitability and are currently extensively studied for possible antinociceptive activity. The aim of this study is to compare the antinociceptive effect of etifoxine and retigabine in rats. Materials and methods: The research included forty male Wistar rats, divided into five groups (n = 8). They were treated intraperitoneally with: 1st group (control) – saline 0,1ml/100g bw, 2nd group–metamizole natrii 150 mg/kg bw, 3rd group – etifoxine 50 mg/kg bw, 4th group –retigabine 5 mg/kg bw and 5th group – retigabine 15 mg/kg bw. The antinociceptive effect was evaluated with hot plate test and analgesy-meter test. The statistical analysis was performed using SPSS.17. Results: Etifoxine did not prolong the latency time in hot plate test and did not increase the withdrawal latency in analgesy-meter test, compared to the animals treated with saline. In hot plate test, retigabine in dose 15 mg/kg bw significantly increased the latency time at the second and third hour, compared to the control group (p<0.05). In analgesy-meter test, a significant increase of the withdrawal latency between retigabine and control animals occurred only at dose 15 mg/kg bw at first hour after single administration (p<0.05). Conclusions: The obtained experimental data show that etifoxine in dose 50 mg/kg bw does not have antinociceptive effect. Single administration of retigabine 15 mg/kg bw reduced painful thermal and mechanical stimuli in rats. The presence of KCNQ channels in the neuronal pathways of pain suggests that the antinociceptive effect of retigabine is maybe based on the activation of low-threshold potassium channels.

Evaluation of the Anti-Inflammatory and Antinociceptive Properties of p-Cymene in Mice

2012 ◽  
Vol 67 (1-2) ◽  
pp. 15-21 ◽  
Author(s):  
Leonardo R. Bonjardim ◽  
Edisleide S. Cunha ◽  
Adriana G. Guimarães ◽  
Michele F. Santana ◽  
Makson G. B. Oliveira ◽  
...  
Keyword(s):  
Nervous System ◽  
Leukocyte Migration ◽  
Autonomous Nervous System ◽  
Second Phase ◽  
Thermal Stimulus ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test ◽  
The Central Nervous System ◽  
Anti Inflammatory

We attempted to identify the antinociceptive and anti-inflammatory actions of the monoterpene p-cymene. Firstly, behavioural screening was carried out to verify the influence of p-cymene [25, 50, and 100 mg/kg intraperitoneal (i.p.)] on the central nervous system (CNS) activity. The antinociceptive activity of p-cymene was evaluated by the acetic acidinduced writhing response, formalin, and hot-plate test, respectively. The leukocyte migration induced by injection of carrageenan was used to assess the anti-inflammatory activity. p-Cymene showed depressant activity on CNS after 4 h of treatment and also a possible action on the autonomous nervous system (ANS), mainly at the dose of 100 mg/kg (i.p.). It was found that p-cymene (50 and 100 mg/kg, i.p.) significantly (p < 0.05) reduced the writhing responses induced by acetic acid. p-Cymene also decreased the licking time in the first and second phase, respectively, of the formalin test. The results of the hot-plate test showed that all doses of p-cymene increased significantly the latency time of the response to the thermal stimulus in both licking and jumping parameters. In addition, there was a significantly (p < 0.05) decreased leukocyte migration at all doses of p-cymene. The experimental data demonstrate that p-cymene possesses antinociceptive and anti-inflammatory activities

scholarly journals Mannitol Enhances the Antinociceptive Effects of Diphenhydramine as an Alternative Local Anesthetic

2020 ◽  
Vol 2020 ◽  
pp. 1-6
Author(s):  
Jo-Young Son ◽  
Jae-Seong Lim ◽  
Jae-Hyung Park ◽  
Jae-Hyeong Park ◽  
Myeong-Shin Kim ◽  
...  
Keyword(s):  
Local Anesthetic ◽  
Subcutaneous Injection ◽  
Antinociceptive Effect ◽  
Latency Time ◽  
Sprague Dawley ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test ◽  
Withdrawal Latency ◽  
Antinociceptive Effects

Mannitol has recently been reported to be effective in enhancing the antinociceptive efficacy of lidocaine. No single study to date, however, has compared diphenhydramine with and without mannitol for nociceptive processing as an alternative local anesthetic. In this study, we examined the antinociceptive efficacy enhancements of diphenhydramine when combined with mannitol. Male Sprague-Dawley rats weighing 230–260 g were used in a hot plate test to evaluate the antinociceptive effects of diphenhydramine. All chemicals were dissolved in isotonic normal saline and administered subcutaneously into the plantar surface of the right hind paw at 10 min before the hot plate test. A subcutaneous injection of 0.5% or 1% diphenhydramine produced significant inhibition of the withdrawal latency time compared with the vehicle treatment. Antinociceptive effects appeared 10 min after the diphenhydramine injections and persisted for over 30 min. The antinociceptive effects of 1% diphenhydramine were not statistically different from those of 1% lidocaine. Although a subcutaneous injection of a 0.5 M mannitol solution alone did not affect the withdrawal latency time, 1% diphenhydramine with 0.5 M mannitol significantly enhanced antinociception. A subcutaneous injection of 1% diphenhydramine with epinephrine (1 : 100,000) solution did not increase the antinociceptive effect of the diphenhydramine. These results suggest that diphenhydramine with mannitol can be used as an alternative local anesthetic.

scholarly journals Antinociceptive Activity ofTrichilia catiguaHydroalcoholic Extract: New Evidence on Its Dopaminergic Effects

2011 ◽  
Vol 2011 ◽  
pp. 1-8 ◽  
Author(s):  
Alice F. Viana ◽  
Izaque S. Maciel ◽  
Emerson M. Motta ◽  
Paulo C. Leal ◽  
Luiz Pianowski ◽  
...  
Keyword(s):  
Dopaminergic System ◽  
Oral Treatment ◽  
Antinociceptive Effect ◽  
Native Plant ◽  
Behavioral Models ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Antinociceptive Effects ◽  
New Evidence

Trichilia catiguais a native plant of Brazil; its barks are used by some local pharmaceutical companies to prepare tonic drinks, such as Catuama. The present study was addressed to evaluate the effects ofT. catiguahydroalcoholic extract in mouse nociception behavioral models, and to evaluate the possible mechanisms involved in its actions. Male Swiss mice were submitted to hot-plate, writhing and von Frey tests, after oral treatment withT.catiguaextract (200 mg kg−1, p.o.). The extract displayed antinociceptive effect in all three models. For characterization of the mechanisms involved in the antinociceptive action of the extract, the following pharmacological treatments were done: naloxone (2.5 mg kg−1, s.c.), SR141716A (10 mg kg−1, i.p.), SCH23390 (15 μg kg−1, i.p.), sulpiride (50 mg kg−1, i.p.), prazosin (1 mg kg−1, i.p.), bicuculline (1 mg kg−1, i.p.) ordl-p-chlorophenylalanine methyl ester (PCPA, 100 mg kg−1, i.p.). In these experiments, the action ofT. catiguaextract was evaluated in the hot-plate test. The treatment with SCH23390 completely prevented the antinociceptive effect, while naloxone partially prevented it. The possible involvement of the dopaminergic system in the actions ofT. catiguaextract was substantiated by data showing the potentiation of apomorphine-induced hypothermia and by the prevention of haloperidol-induced catalepsy. In conclusion, the antinociceptive effects ofT. catiguaextract seem to be mainly associated with the activation of dopaminergic system and, to a lesser extent, through interaction with opioid pathway.

scholarly journals Antinociceptive Activity ofMelicope ptelefoliaEthanolic Extract in Experimental Animals

2010 ◽  
Vol 2010 ◽  
pp. 1-6 ◽  
Author(s):  
Mohd Roslan Sulaiman ◽  
Azyyati Mohd Padzil ◽  
Khozirah Shaari ◽  
Syamimi Khalid ◽  
Wan Mastura Shaik Mossadeq ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Oral Administration ◽  
Ethanolic Extract ◽  
Antinociceptive Activity ◽  
Second Phase ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Experimental Animals ◽  
Antinociceptive Effects ◽  
Abnormal Behaviors

Melicope ptelefoliais a medicinal herb commonly used in Malaysia to treat fever, pain, wounds, and itches. The present study was conducted to evaluate the antinociceptive activity of theMelicope ptelefoliaethanolic extract (MPEE) using animal models of nociception. The antinociceptive activity of the extract was assessed using acetic acid-induced abdominal writhing, hot-plate, and formalin-induced paw licking tests. Oral administration of MPEE produced significant dose-dependent antinociceptive effects when tested in mice and rats using acetic acid-induced abdominal constriction test and on the second phase of the formalin-induced paw licking test, respectively. It was also demonstrated that MPEE had no effect on the response latency time to the heat stimulus in the thermal model of the hot-plate test. In addition, the antinociception produced by MPEE was not blocked by naloxone. Furthermore, oral administration of MPEE did not produce any effect in motor performance of the rota-rod test and in acute toxicity study no abnormal behaviors as well as mortality were observed up to a dose level of the extract of 5 g/kg. These results indicated that MPEE at all doses investigated which did not produce any sedative and toxic effects exerted pronounce antinociceptive activity that acts peripherally in experimental animals.

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