scholarly journals Aryl Hydrocarbon Receptors in Indole Derivative Treated Mice: Neuropharmacological Perspectives

2021 ◽  
Vol 48 (1) ◽  
pp. 25-33
Author(s):  
P. Andreeva-Gateva ◽  
J. Tchekalarova ◽  
K. Kamenova ◽  
M. Strokova-Stoilova ◽  
S. Chakar ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
Indole Derivative ◽  
Molecular Mechanisms ◽  
Formalin Test ◽  
Aryl Hydrocarbon Receptors ◽  
Hot Plate ◽  
Neuroprotective Effects ◽  
Hot Plate Test ◽  
Aryl Hydrocarbon ◽  
Dose Dependent

Abstract Aim/objective. When applied in pharmacological doses, the indole derivative melatonin exhibits neuroactive and neuroprotective effects. Indoles and their metabolites, such as kynurenine, are ligands of aryl hydrocarbon receptors (AhR). This study aimed to evaluate the antiepileptic and analgesic activity of melatonin and two synthetic melatonin derivatives. The possible involvement of AhR and kynurenine in their neuropharmacological effects were also tested. Methods. The tested substances were: melatonin, two melatonin derivatives bearing aryl hydrocarbon moiety with either furyl or thienyl substitute (3e and 3f), and alpha naphthoflavone (ANF), an antagonist of AhR. After intraperitoneal injection of 30, 100, or 300 mg/kg of the tested agents for seven days, male mice ICR (25-30 g) were subjected to a corneal kindling seizure model. Two tests for analgesia, i.e., the hot plate test and the formalin test, were also applied. AhR and kynurenine concentrations were evaluated in brain homogenates. Results. Substances 3e and 3f demonstrated an antiepileptic activity comparable to that of melatonin. Some analgesic activity was also shown, albeit lower than that of melatonin in equivalent doses. For melatonin and 3f treated mice, dose-dependent increases in AhR and kynurenine levels in brain homogenates were recorded. The antagonist ANF neither blocks the antiseizure activity of the tested indoles, nor demonstrated analgesic activity. Conclusion. Melatonin and the two tested melatonin-aroylhydrazone derivatives bearing either furyl or thienyl substitute exhibit antiepileptic and analgesic activity. Our results did not support the involvement of AhR in the demonstrated neurobiological activity. Further studies are needed to elucidate their exact molecular mechanisms.

Synthesis of 8-alkoxy-1,3-dimethyl-2, 6-dioxopurin-7-yl-substituted acetohydrazides and butanehydrazides as analgesic and anti-inflammatory agents

2015 ◽  
Vol 21 (5) ◽  
pp. 273-278 ◽  
Author(s):  
Grażyna Chłoń-Rzepa ◽  
Agnieszka W. Jankowska ◽  
Małgorzata Zygmunt ◽  
Krzysztof Pociecha ◽  
Elżbieta Wyska
Keyword(s):  
Analgesic Activity ◽  
Structural Element ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Peripheral Mechanism ◽  
Anti Inflammatory ◽  
Factor Α ◽  
Necrosis Factor ◽  
Inhibit Tumor Necrosis Factor

AbstractA series of new 8-alkoxy-1,3-dimethyl-2,6-dioxopurin-7-yl-substituted acetohydrazides and butanehydrazides 6–12 was synthesized and evaluated for the analgesic activity in two in vivo models: the writhing syndrome and the hot-plate tests. Among the investigated derivatives, compounds with N′-arylidenehydrazide moiety 9–12 show analgesic activity significantly higher than that of acetylsalicylic acid, which may indicate the importance of this structural element for analgesic properties. The lack of the activity in the hot-plate test may suggest that the analgesic activity of the newly synthesized compounds is mediated by a peripheral mechanism. The selected compounds 7 and 12 inhibit tumor necrosis factor α production in a rat model of lipopolysaccharide-induced endotoxemia, similarly to theophylline, which may confirm their anti-inflammatory properties.

scholarly journals Analgesic Activity of the Kappa Opioid Receptor Agonist RU-1205 in Rats

2018 ◽  
Vol 3 (2) ◽  
pp. 13 ◽  
Author(s):  
AA Spasov ◽  
OY Grechko ◽  
DM Shtareva ◽  
AI Raschenko ◽  
Natalia Eliseeva ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Analgesic Activity ◽  
Analgesic Effect ◽  
Physical Dependence ◽  
Receptor Activation ◽  
Kappa Opioid Receptor ◽  
Kappa Opioid ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test

Introduction: Opioid analgesics are the most efficient and widely used drugs for the management of moderate to severe pain. However, side effects associated with mu receptor activation, such as respiratory depression, tolerance and physical dependence severely limit their clinical application. Currently, the kappa-opioid system is the most attractive in terms of the clinical problem of pain, because kappa-agonists do not cause euphoria and physical dependence. The purpose of this study was to evaluate the antinociceptive effect of the novel compound - RU-1205. Methods: The analgesic activity of RU-1205 was studied on nociceptive models that characterize the central and peripheral pathways of pain sensitivity (hot plate test, electrically induced vocalisation, formalin test, writhing test). Results: RU-1205 exhibited highly potent antinociceptive effects in rodent models of acute pain with ED50 values of 0.002 - 0.49 mg /kg. Pretreatment with the κ-opioid receptor antagonist norBinaltorphimine significantly attenuated the analgesic activity of investigated substance in a hot plate test. Conclusions: It was established that the compound shows a significant dose-dependent central and peripheral analgesic effect. It was assumed kappa-opioidergic mechanism of analgesic effect of RU-1205.

scholarly journals Analgesic effect of the aqueous extract of Artimisia herba alba Arial part

2010 ◽  
Vol 9 (3) ◽  
pp. 28
Author(s):  
Sh. M. Al-khazrji , and I. K. Khalil
Keyword(s):  
Acetic Acid ◽  
Aqueous Extract ◽  
Cold Water ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Writhing Test ◽  
Plate Test ◽  
Analgesic Effects ◽  
Rats And Mice ◽  
Dose Dependent

The present study was aimed to investigate the analgesic effects of the aqueous extract of Artemisia herba alba Arial part in rats and mice ( AEAHA ). The AEAHA (400- 700 mg/kg; p.o.) was evaluated for its analgesic activity by employing acetic acid-induced writhing test, hot plate test and tail immersion tests i.e. in hot and cold water. AEAHA (400- 700 mg/kg; p.o.) showed significant (P<0.01) reduction in the number of writhing induced by acetic acid,increased reaction time in hot plate test and elevated pain threshold in hot and cold water tests. AEAHA exhibited the dose-dependent analgesic effects

scholarly journals Evaluation of analgesic and anti-inflammatory activities of Warionia saharae essential oil

2021 ◽  
pp. 1-10
Author(s):  
Mimouna Yakoubi ◽  
Nasser Belboukhari ◽  
Khaled Sekkoum ◽  
Mohammed Bouchekara ◽  
Hassan Y. Aboul-Enein
Keyword(s):  
Essential Oil ◽  
Traditional Medicine ◽  
Analgesic Activity ◽  
Inflammatory Diseases ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Standard Drug ◽  
Analgesic Effects ◽  
Test Models ◽  
Anti Inflammatory

Warionia saharae Benth & Coss (W.s) (Asteraceae) is a monospecific genus endemic to Algeria and Morocco. Its leaves are used in their traditional medicine, such as gastrointestinal and inflammatory diseases; for instance, rheumatoid arthritis treatment. In this work, our team investigated the anti-inflammatory and analgesic effects of essential oil extracted from the dried upper parts of Warionia saharae based on different standard experimental test models. The analgesic activity was assessed by central and peripheral models, such as “hot plate” and “writhing” tests on Swiss albino mice. The hot plate test used latency measurements to assess acute cutaneous pain sensitivity, as a result; the latency of the hind-paw pain response was by licking and either shaking or jumping, those occurrences were recorded. Writhing test as a chemical method used to induce pain of peripheral origin in mice by injecting acetic acid intraperitoneally (IP). This results in characteristic stretching behavior of the animals (cramps and contortions). The evaluation of the analgesic activity, shows that the essential oil of this plant induces a decrease in the number of abdominal cramps in the contortion test and a maximum inhibition of pain. As for the anti-inflammatory effect, it was studied by the “paw edema” test, a phlogogenic agent (formaldehyde) was used to stimulate inflammation in the paws of mice. Anti-inflammatory properties can be observed by inhibiting this edema compared to the standard drug Diclofenac. In conclusion, Warionia saharae essential oil (75 mg/kg) showed a strong anti-inflammatory and analgesic activities which supports the conventional use of this plant in traditional medicine.

scholarly journals Evaluation of analgesic activity of turmeric (Curcuma longa Linn.) in Wister rats

2017 ◽  
Vol 6 (3) ◽  
pp. 568 ◽  
Author(s):  
Sangita Jogdand ◽  
Jagruti Bhattacharjee
Keyword(s):  
Analgesic Activity ◽  
Normal Saline ◽  
Curcuma Longa ◽  
Ethanolic Extract ◽  
Albino Rats ◽  
Time Intervals ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Analgesic Activities

Background: NSAIDs like Aspirin etc. are randomly used for mild to severe types of pain but long-term and injudicious use of NSAIDs lead to a number of side effects. The present study is designed for exploring the analgesic potential of Curcuma longa Linn (Turmeric) in albino rats, which may widen the therapeutic horizon for the said agent.Methods: Ethanolic extract of Curcuma longa in the doses 100, 200 and 400mg/kg is given orally to 6 Wister rats against a control of normal saline and a standard using Aspirin (300mg/kg) and the animals were subjected to Eddy’s hot plate test at different time intervals i.e., 30, 60, 90 and 120 minutes after administration of the drugs and the parameters were noted.Results: The analgesic activity of Curcuma longa showed significant (p<0.05) increase in mean basal reaction time in Hot plate method when compared to the control (Normal saline). As the dose of the ethanolic extract of Curcuma longa was gradually increased from 100, 200 and 400mg/kg respectively, the analgesic activity significantly increased (<0.05). Effect of curcuma longa at a dose of 400mg/kg is found to be comparable with Aspirin.Conclusions: The results of this study suggest that turmeric (Curcuma longa) has significant analgesic activities in rats. 

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.

scholarly journals Study of analgesic activity and effects of new dipharmacophores – nebracetam and cyclooxygenase-2 inhibitors derivatives on the cognitive abilities of rats

2021 ◽  
Vol 7 (4) ◽  
pp. 71-79
Author(s):  
Vitaliy S. Slyusarenko ◽  
Ivan S. Koklin ◽  
Sergiy M. Kovalenko ◽  
Vladimir P. Chuev ◽  
Alexey A. Shabalin ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Analgesic Activity ◽  
Mefenamic Acid ◽  
Cognitive Abilities ◽  
Pain Syndrome ◽  
Niflumic Acid ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Female Ratio ◽  
Male Female Ratio

Introduction: The aim of the present study was to research the analgesic activity and effect of new dipharmacophore compounds consisting of substances with proven therapeutic activity, namely nebracetam–ibuprofen (NRIP), nebracetam–dexibuprofen (NRDIP), nebracetam–niflumic acid (NRNFA), and nebracetam–mefenamic acid (NRMFA), on the cognitive abilities of rats. Materials and methods: The experimental study was performed in 110 Wistar rats (male/female ratio 50/50%), weighing 180–200 g, and 50 laboratory mice (male/female ratio 50/50%) weighing 18–22 g. The study of the analgesic activity was carried out using the acetic acid writhing test and the hot plate test. The effect on the cognitive abilities of rats was studied using the pattern recognition test in a model of neurotrauma caused by a drop-weight. Results and discussion: It has been shown that the administration of dipharmacophores nebracetam–ibuprofen (NRIP), nebracetam–dexibuprofen (NRDIP), nebracetam–niflumic acid (NRNFA) as well as nebracetam–mefenamic acid (NRMFA) in the tested dosages leads to a statistically significant (p&lt;0.05) analgesic action in acetic acid writhing tests and hot plate tests. At the same time, the analgesic activity of the compounds has been shown to conjoin with a statistically significant influence on cognitive functions in the experimental animal groups after simulating a neurotrauma. Conclusion: The dipharmacophore compounds studied in the present research, having analgesic and nootropic effects, can be used as effective and safe analgesics and can also be used for the treatment and prevention of pain syndrome, enhancing the cognitive abilities of healthy people in complicated professional conditions.

scholarly journals Synthesis and Analgesic Activity of η6-(Anisole)- Triscarbonyl-Chromium(0)

1999 ◽  
Vol 6 (1) ◽  
pp. 25-29
Author(s):  
Márcio Luís Andrade e Silva ◽  
Alberto Federman Neto ◽  
Joseph Miller
Keyword(s):  
Analgesic Activity ◽  
Wistar Rats ◽  
Pain Threshold ◽  
The Body ◽  
Test Method ◽  
Control Group ◽  
Synthetic Method ◽  
Hot Plate ◽  
Hot Plate Test ◽  
General Method

The general method for synthesis the η6-(arene)-triscarbonyl-chromium(0) complexes was modified and applied for preparation of η6-(anisole)-triscarbonyl-chromium(0) and the study of its analgesic activity was undertaken. A significant analgesic activity was observed after intraperitoneal injection, in Wistar rats. Two doses (30 and 50 mg/Kg of the body weight) of η6-(anisole)- triscarbonyl-chromium(0) were injected and the analgesic activity was evaluated by the Hot Plate Test method. They showed a significant analgesic effect in comparison with the control group and the group treated with dipyrone standard, but not so high when compared with the group treated with morphine standard. Overall, it was observed that the η6-(anisole)- triscarbonyl-chromium(0) was easily obtained by the modified synthetic method and was effective in increasing the pain threshold.

scholarly journals Analgesic effect of intrathecally administered orexin-A in the rat formalin test and in the rat hot plate test

2002 ◽  
Vol 137 (2) ◽  
pp. 170-176 ◽  
Author(s):  
Tatsuo Yamamoto ◽  
Natsuko Nozaki-Taguchi ◽  
Tanemichi Chiba
Keyword(s):  
Analgesic Effect ◽  
Formalin Test ◽  
Hot Plate ◽  
Orexin A ◽  
Hot Plate Test ◽  
Plate Test

scholarly journals Ethnopharmacological Evaluation ofBreuEssential Oils fromProtiumSpecies Administered by Inhalation

2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Eduardo Rodrigues da Silva ◽  
Danilo Ribeiro de Oliveira ◽  
Patrícia Dias Fernandes ◽  
Humberto Ribeiro Bizzo ◽  
Suzana Guimarães Leitão
Keyword(s):  
Essential Oils ◽  
Formalin Test ◽  
Significant Inhibition ◽  
Chemical Compositions ◽  
Static Headspace ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Test Formulation ◽  
Similar Chemical ◽  
Sedative Effects

Background.Breuis an aromatic oleoresin which has been used by Amazonian traditional communities as a remedy for headaches and migraines by burning and inhaling the smoke produced during its combustion. This study evaluated the antinociceptive and sedative activities of formulations containingbreuessential oils administered by inhalation.Methods. Five different formulations (A–E) containingbreuessential oils were evaluated for their sedative and antinociceptive activities in mice. They were delivered for 20 minutes using an inhalation chamber coupled with a nebulizer and the air inside was collected by static headspace and analyzed by GC-FID.Results. All nebulized formulations had similar chemical compositions and major compounds as the original essential oils. None of them resulted in significant increase in response time during the hot plate test. In the formalin test, Formulation E showed a significant inhibition of licking responses in the early (46.8%) and late (60.2%) phases. Formulation B was effective (36.9%) in the first phase and Formulation D (37.9%) in the second. None of the formulations presented sedative effects.Conclusion.Breuessential oils, when inhaled, may present antinociceptive and anti-inflammatory properties without sedation. Additionally, nebulization proved to be an efficient method for administration of formulations containing these essential oils.

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