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.

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.

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.

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 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.

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 Borneol, a Bicyclic Monoterpene Alcohol, Reduces Nociceptive Behavior and Inflammatory Response in Mice

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Jackson Roberto Guedes da Silva Almeida ◽  
Grasielly Rocha Souza ◽  
Juliane Cabral Silva ◽  
Sarah Raquel Gomes de Lima Saraiva ◽  
Raimundo Gonçalves de Oliveira Júnior ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Motor Coordination ◽  
Nociceptive Behavior ◽  
Hot Plate ◽  
Rotarod Test ◽  
Hot Plate Test ◽  
Plate Test ◽  
Strength Tests ◽  
Anti Inflammatory ◽  
Motor Abnormality

Borneol, a bicyclic monoterpene, has been evaluated for antinociceptive and anti-inflammatory activities. Antinociceptive and anti-inflammatory activities were studied by measuring nociception by acetic acid, formalin, hot plate, and grip strength tests, while inflammation was prompted by carrageenan-induced peritonitis. The rotarod test was used to evaluate motor coordination. Borneol produced a significant (P<0.01) reduction of the nociceptive behavior at the early and late phases of paw licking and reduced the writhing reflex in mice (formalin and writhing tests, resp.). When the hot plate test was conducted, borneol (in higher dose) produced an inhibition (P<0.05) of the nociceptive behavior. Such results were unlikely to be provoked by motor abnormality. Additionally, borneol-treated mice reduced the carrageenan-induced leukocytes migration to the peritoneal cavity. Together, our results suggest that borneol possess significant central and peripheral antinociceptive activity; it has also anti-inflammatory activity. In addition, borneol did not impair motor coordination.

scholarly journals Analgesic Effect of Dayak Onion (Eleutherine americana (Aubl.) Merr.) on Mice (Mus musculus) by Hot Plate Test Method

2021 ◽  
Vol 4 (1) ◽  
pp. 22
Author(s):  
Muhammad Hafizh ◽  
Danti Nur Indiastuti ◽  
Indri Safitri Mukono
Keyword(s):  
Response Time ◽  
Analgesic Effect ◽  
Latency Period ◽  
Test Method ◽  
Control Group ◽  
Test Results ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test ◽  
Eleutherine Americana

Introduction: Pain is an unpleasant experience that reduces a person's quality of life. Pain related complain can be treated by administering analgesic drugs. Several studies show that the availability of analgesics is still low, especially opioid analgesics. Dayak onion (Eleutherine americana (Aubl.) Merr.) are used by the Dayaks to relieve pain. Several empirical studies have shown that Dayak onion contain compounds including quercetin as a potential analgesic. This research aimed to investigate the potential analgesic effect of Dayak onion using hot plate method.Methods: The research was conducted experimentally on 36 BALB/c male mice which randomly divided into 6 different treatment groups of Dayak onion exctract, aspirin, codein and aquadest. Each group were thermally pain-induced for latency period measurement by the hot plate test method. Obtained data were processed using Analysis of Variance (ANOVA) followed by Dunnett test.Results: There was a difference in the latency period between the baseline response time and the response time after being treated in each group. ANOVA test results showed significant results (p<0.05) so that the resulting latency period was significant. Dunnett test results showed significant results (p<0.05) in negative control group. Based on these results, Dayak onion are proven to have an analgesic effect on heat stimulation.Conclusion: Dayak onion possess significant analgesic effect on thermally pain-induced mice. Dayak onion extract 90 mg/kg mouse produced better analgesic effects than aspirin 65 mg/kg mouse.

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 Anti-inflammatory, antipyretic, analgesic, and antioxidant activities of Haloxylon salicornicum aqueous fraction

2019 ◽  
Vol 17 (1) ◽  
pp. 1034-1042
Author(s):  
Riaz Ullah ◽  
Mansour S. Alsaid ◽  
Ali S. Alqahtani ◽  
Abdelaaty A. Shahat ◽  
Almoqbil A. Naser ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Water Extract ◽  
Antioxidant Potential ◽  
High Dose ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Aqueous Fraction ◽  
Plate Test ◽  
Anti Inflammatory ◽  
Haloxylon Salicornicum

AbstractThe medicinal plant Haloxylon salicornicum is utilized for therapeutic purposes. We previously reported the antioxidant potential of hexane fraction and methanol extracts of the same species. However, since these solvents could be clinically toxic, the current findings investigated the pharmacological effects of the water fraction. The pain relieving, antioxidant, anti-inflammatory, and antipyretic potential of H. salicornicum water extract (HEW) were studied at two concentrations (250 and 500 mg/kg) in rodents. The carrageenan stimulated rat paw edema assay was exercised to assess anti inflammatory potential in rats; yeast-stimulated hyperthermia was utilized to test antipyretic activity in mice; analgesic properties were assessed based on acetic acid-induced writhing, tail flicking, and hot-plate test; and antioxidant potential was examined with the 2,2-diphenyl-1-picrylhydrazyl assay. We found that 500 mg/kg HEW inhibited edema by 44.03%. Yeast-induced hyperthermia in mice was reduced by 250 and 500 mg/kg HEW after 30, 60, and 120 min with significant level of (P < 0.001) compared to rectal temperature of yeast administered group. The high dose of HEW (500 mg/kg) improved the reaction time of mice in the hot-plate test from 6.66 ± 0.33 to 11.33 ± 0.49 s after 120 min. In the acetic acid-stimulated writhing test, 250 and 500 mg/kg HEW decreased writhing by 32.71% and 51.40%, respectively, after 20 min. HEW also showed antioxidant effects. These results demonstrate that HEW is bioactive and has therapeutic potential for treating a variety of ailments.

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