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 Anti-inflammatory and Analgesic Effects in Rodent Models of Ethanol Extract of Clausena anisata Roots and their Chemical Constituents

2017 ◽  
Vol 12 (1) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Emmanuel Kofi Kumatia ◽  
Kofi Annan ◽  
Rita Akosua Dickson ◽  
Abraham Yeboah Mensah ◽  
Isaac Kingsley Amponsah ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
Crude Extract ◽  
Analgesic Effect ◽  
Chemical Constituents ◽  
Ethanol Extract ◽  
Phytochemical Analysis ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test ◽  
Anti Inflammatory

The in vivo anti-inflammatory and analgesic activities of the crude ethanol extract and chemical constituents of Clausena anisata roots were investigated. The crude extract, which was devoid of any visible acute toxicity, displayed significant anti-inflammatory effect at the dose of 1000 mg/kg (p.o.) when assessed using the carrageenan-induced oedema model. In the acetic acid-induced writhing and hot plate tests, it produced a very significant ( p < 0.001), dose-dependent analgesic effect, with maximum analgesic activity of 72.1% at 1000 mg/kg (p.o.). Phytochemical analysis of the crude extract resulted in the isolation of four coumarins (anisocoumarin B, osthol, imperatorin and xanthotoxol) and a carbazole alkaloid, heptaphylline. Among the isolated compounds, osthol and anisocoumarin B produced the highest anti-inflammatory activity at 9 mg/kg (p.o.): slightly better than the positive control, indomethacin. Except for xanthotoxol, all the isolated compounds administered at 6 mg/kg (p.o.) produced significant analgesic activity and higher than diclofenac; with heptaphylline being the most potent (48.7%). The analgesic activity of anisocoumarin B (50.4%) was the highest among the isolates tested and the standard, tramadol, in the hot plate test. The nonselective opioid receptor antagonist, naloxone, abolished the analgesic effect of the crude extract and the tested isolates (anisocoumarin B and xanthotoxol) in the hot plate test suggesting an effect via the central opioidergic system. These findings provide the scientific basis for the use of C. anisata roots in traditional medicine as anti-inflammatory and analgesic agents.

scholarly journals Kappa opioid receptor activation in the amygdala disinhibits CRF neurons to generate pain-like behaviors

2021 ◽  
Vol 185 ◽  
pp. 108456
Author(s):  
Matthew Hein ◽  
Guangchen Ji ◽  
Dalton Tidwell ◽  
Preston D'Souza ◽  
Takaki Kiritoshi ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Activation ◽  
Kappa Opioid Receptor ◽  
Kappa Opioid ◽  
Crf Neurons

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.

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 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
Sign in / Sign up

Export Citation Format

Share Document