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<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 The analgesic activity of new sulfur-containing di- and tetrahydropyridine derivatives in the hot plate test

2021 ◽  
pp. 45-55
Author(s):  
E.Yu. Bibik ◽  
◽  
L.I. Kurbanov ◽  
S.A. Grygoryan ◽  
D.S. Krivokolysko ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
High Efficiency ◽  
Pain Syndrome ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Reference Drug ◽  
Plate Test ◽  
Metamizole Sodium ◽  
Sulfur Containing

Nowadays the search of new high-efficiency and safe drugs for the pharmacotherapy of diseases accompanied by pain syndrome is an active area of modern pharmacological research. 170 new derivatives of di- and tetrahydropyridines synthesized on the basis of the Chemex Research Laboratory, Vladimir Dahl Lugansk State University were exposed to the virtual bioscreening using the Swiss Target Prediction software. The paper describes screening studies in vivo of 5 samples of sulfur-containing di- and tetrahydropyridines (laboratory codes d02-138, as-262, f02-079, cv-074, cv-143) in the standard hot plate test in comparison with the reference drug — metamizole sodium. The compounds in the dose of 5 mg/kg were given intragastrically 1 hour and a half before placing the rats on the hot plate, the reference drug in the dose of 7 mg/kg also was given intragastrically 1 hour and a half before placing the rats on the hot plate. The compounds with laboratory codes as-262 (allyl 6-({2-[(4-acetylphenyl)amino]-2-oxoethyl}thio)-5-cyano-4-(2-furyl)-2-methyl-1,4-dihydropyridine-3-carboxylate) and d02-138 (ethyl 4-[({[3-cyano-5-{[(2,4-dichlorophenyl)amino]carbonyl}-4-(2-furyl)-6-methyl-1,4-dihydropyridinе-2-yl]thio}acetyl)amino]benzoate) possess the most pronounced analgesic activity in the dose of 5 mg/kg, they demonstrated 2.03 and 1.9-fold efficiency in comparison to metamizole sodium respectively. The rest three specimens demonstrated metamizole sodium-like analgesic activity.

scholarly journals Synthesis, characterization and pharmacological activity of new 2- imino –thiazolidine-4-one derivatives

2019 ◽  
Vol 10 (3) ◽  
pp. 1763-1769 ◽  
Author(s):  
Raghdah M. Alwiswasy ◽  
Raheem Jameel M ◽  
Basim Jasim Hameed
Keyword(s):  
Acetic Acid ◽  
Pharmacological Activity ◽  
Analgesic Activity ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test ◽  
Edema Model ◽  
Ft Ir ◽  
Anti Inflammatory ◽  
Analgesic Activities

A new 2-iminothiazolidin-4-ones compound and its derivatives were synthesized and characterized by FT-IR, CHN, and 1HNMR techniques. The target compounds were assessed for their anti-inflammatory and analgesic activities, and the study was performed using Swiss albino mice (25-30 g) for investigation. A hind edema model caused by , while the analgesic activity was assessed using an acetic acid-induced writhing and a hot plate test evaluated the anti-inflammatory activity.

scholarly journals Anti-nociceptive and anti-inflammatory effects of an aqueous extract of blended leaves of Ocimum gratissimum and Psidium guajava

2019 ◽  
Vol 5 (1) ◽  
Author(s):  
Akinyinka O. Alabi ◽  
Abayomi M. Ajayi ◽  
Osarume Omorogbe ◽  
Solomon Umukoro
Keyword(s):  
Acetic Acid ◽  
Aqueous Extract ◽  
Psidium Guajava ◽  
Antinociceptive Activity ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Promising Alternative ◽  
Plate Test ◽  
Ocimum Gratissimum ◽  
Anti Inflammatory

Abstract Background To investigate the antinociceptive and anti-inflammatory activities of aqueous extract of a blended mixture of dried leaves of Ocimum gratissimum and Psidium guajava, a traditional analgesic drug polyherbal (TADP) used as a remedy for pain-related conditions. Methods Antinociceptive activity of TADP (100, 200 and 400 mg/kg) was evaluated in the hot plate test and acetic acid-induced nociception in mice while the anti-inflammatory was evaluated in carrageenan-induced paw oedema in rats. Levels of nitrite, myeloperoxidase, glutathione and malondialdehyde were assayed in carrageenan-induced paw tissue. Results TADP (200 and 400 mg/kg) significantly prolong the latency time in the hot-plate test. TADP (100–400 mg/kg) produced a dose-dependent significant inhibition of the acetic-acid induced abdominal constriction. The antinociceptive activity of TADP in the presence of naloxone and atropine was not reversed whereas yohimbine and glibenclamide significantly reversed it. TADP (100, 200 and 400 mg/kg) significantly reduced the swelling in the carrageenan-induced oedema model and also produced a reduction in the nitrite and myeloperoxidase level. TADP (400 mg/kg) significantly reduced malondialdehyde concentration and increase glutathione level in the carrageenan-induced rat paw. TADP significantly decrease the number of cellular infiltrates in the histopathological assessment. Conclusion These results indicate that polyherbal product containing blended leaves of Ocimum gratissimum and Psidium guajava possess antinociceptive and anti-inflammatory properties, hence represents a promising alternative remedy in inflammation-induced pain.

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 Preparation and Analysis of New 1,3,5-Trisubstituted-2-Pyrazolines Derivative for Their Analgesic Potential

2021 ◽  
pp. 153-164
Author(s):  
Jitendra Kumar Chaudhary ◽  
Alok Pal Jain ◽  
O. P. Tiwari
Keyword(s):  
Acetic Acid ◽  
Analgesic Effect ◽  
Latency Time ◽  
Hot Plate ◽  
Phenyl Hydrazine ◽  
Hot Plate Test ◽  
Test Technique ◽  
Plate Test ◽  
Withdrawal Latency ◽  
In Series

The goal of the study was to develop, synthesise, and characterise a novel 1,3,5-trisubstituted-2-pyrazolines derivative, as well as to assess its analgesic potential. The reaction of chalcone derivatives with 4-hydrazinylbenzene sulfonamide hydrochloride and phenyl hydrazine hydrochloride yielded 1,3,5-tri-substituted-2-pyrazolines derivatives. The IR, 1HNMR, and mass spectrum analyses were used to characterise a total of sixteen substances. Analgesic activity of the proposed substances has been tested. The analgesic effect of the produced compounds was tested using two methods: the hot plate test technique and acetic acid induced writhing in mice. To compare the effectiveness, pentazocine and acetyl acetic acid were utilised as reference drugs. The hot plate test technique and acetic acid induced writhing in mice were used to assess the analgesic effect of the 16 produced chemical series A1-A8, and B1-B8. The evaluation's outcomes were viewed using Pentazocine and acetyl acetic acid as the standard drugs. In a 90-minute hot plate test, compounds A2 (10.30 s), A4 (9.45 s), A7 (11.65 s), and A8 (11.26 s) showed a delay in paw withdrawal latency time. Compounds B2 (9.10 s) and B7 (10.42 s) prolong the paw withdrawal latency time after 90 minutes in series B1-B8, reduce the pain feeling, and inhibit pain induced by heat methods. Compounds A2, A5, A6, A7, and A8 from Series A1-A8 showed 83.00, 76.01, 80.34, 86.99, 88.15 percent inhibition, substantially (p0.05 and p0.001, respectively), and decreased the number of wriths caused by 0.6 percent acetic acid at a dosage of 10 mg/kg. Acetylsalicylic acid (10 mg/kg) appears to be more successful in lowering the number of wriths, with a 99.0% reduction in the number of wriths (p0.001). B1, B3, and B4 have the least amount of active activity. These all finding suggest that these synthesized compounds have the potential as analgesic agent.

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.

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.

scholarly journals A Original Article ANALGESIC ACTIVITY OF BARK AND LEAVES OF FICUS RELIGIOSA L. FROM NEPAL

2020 ◽  
pp. 32-35
Author(s):  
DHARMA RAJ MARASINI ◽  
JITENDRA PANDEY ◽  
LAXMAN PAUDEL SHARMA ◽  
LAXMI PAUDEL ◽  
ROSHNI GYAWALI ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Analgesic Activity ◽  
Test Group ◽  
Ethanolic Extract ◽  
Stem Bark ◽  
Latency Time ◽  
Hot Plate ◽  
Ficus Religiosa ◽  
Standard Drug ◽  
Ethanolic Extracts

Objective: Because of adverse side effects, caused by NSAIDs, tolerance, and dependence induced by opiates, the use of these analgesic agents has not been successful in all cases. Therefore, alternative analgesic drugs from plant sources are the new target now days. The objective of this study was to evaluate the analgesic activity of ethanolic extracts of stem barks and leaves of Ficus religiosa. Methods: The analgesic activity of ethanolic extract of stem barks and leaves was evaluated in the Swiss albino mice model using acetic acid-induced writing response and Eddy’s hot plate method. Analgesic activity was demonstrated with the percentage inhibition of acetic acid induced writings and the percentage increased in latency time of paw licking. The potency of test extracts was compared with standard drug, Diclofenac. Results: Ethanolic extract of leaves and bark of F. religiosa showed potential analgesic activity from both methods. From Eddy’s hot plate model, it was observed that the percentage of increased latency time at 90 min by ethanolic extract of leaves and stem bark was found to be 70.81 % (8.54 min) and 70.78 % (8.53 min) respectively at a dose of 400 mg/kg. Both of these results are statistically significant (p<0.05) as compared to the test group. Furthermore, both of these extracts showed the dose-dependent and time-dependent increased in latency time and these results are compared to that of standard drug Diclofenac. Similarly, ethanolic extract of leaves and stem at 400 mg/kg significantly inhibited the number of writhings induced by acetic acid. The percentage inhibition of writhings by ethanolic extract of leaves at a dose of 400 mg/kg was 68.47 % which was similar to that of standard drug Diclofenac (68.47 %). However, ethanolic extract of bark showed relatively lower percentage inhibition (60.79 %) as compared to leaf extract and standard, but the result was significant as compared to that of the test group (p<0.05). Conclusion: Ethanolic extracts of F. religiosa stem bark and leaf possess both central and peripheral analgesic properties and these effects may be beneficial for the management of pain.

Sign in / Sign up

Export Citation Format

Share Document