scholarly journals Effect of adjuvant drugs on the analgesic activity of opioid morphine analgesics and compound RU-1205

2021 ◽  
Vol 7 (3) ◽  
pp. 41-47
Author(s):  
Alexander A. Spasov ◽  
Olesya Iu. Grechko ◽  
Natalya V. Eliseeva ◽  
Yuliya V. Lifanova ◽  
Angelina N. Aleksandrenkova
Keyword(s):  
Analgesic Activity ◽  
Analgesic Effect ◽  
Opioid Analgesics ◽  
Benzodiazepine Receptor ◽  
Tail Flick ◽  
Opioid Agonist ◽  
Tail Flick Test ◽  
Kappa Agonist ◽  
Kappa Opioid Agonist ◽  
Probable Interaction

Introduction: Adjuvant medications can be used to increase the analgesic effect of opioid analgesics, reduce the manifestation of side effects, and also for premedication. This paper provides information on the effect of clonidine, haloperidol, metocloparmide, diazepam, midazolam on opioid analgesics: - morphine and the selective kappa-opioid agonist compound RU-1205. Materials and methods: A probable interaction between RU-1205, morphine and adjuvant drugs in pain behaviors was carried out on the model of somatogenic pain. 95 male mice received either RU-1205 (5 mg/kg, i.p.) and morphine (1 mg/kg, i.p.) separately or in combination with haloperidol (0.45 mg/kg, i.p.); midazolam (0.3 mg/kg, i.p.); diazepam (1 mg/kg, i.p.); metoclopramide (5 mg/kg, i.p.), and clonidine (1 mg/kg, i.p.). The analgesic effect was assessed by tail flick test. Registration of the latent period of the reaction was carried out 30, 60 and 90 minutes after the adjuvant drug administration. Results: When studying the interaction with morphine, it was found that clonidine, haloperidol and metoclopramide enhanced the effects; diazepam offset them, and midazolam had no affect on the analgesic properties. In the course of the studies, RU-1205 showed an increase in analgesic activity when combined with clonidine, a slight increase with midazolam, and a decrease when co-administered with diazepam. Haloperidol had no influence on the effect of RU-1205, while metoclopramide both potentiated and reduced the analgesic effect. Discussion: Pharmacodynamic and pharmacokinetic interactions of RU-1205 with an α2AR agonist, benzodiazepine receptor agonists, D2P antagonist, and σ-receptor blocker were established. Conclusion: The presented data make it possible to more accurately formulate ideas about the localization and action mechanism of the kappa-agonist of opioid receptors, the compound RU-1205.

scholarly journals ASSESSMENT OF ANALGESIC ACTIVITY OF NELUMBO NUCIFERA FRUIT ETHANOL EXTRACT

2019 ◽  
pp. 1-5
Author(s):  
MUHAMMAD ALI RAJPUT ◽  
TABASSUM ZEHRA ◽  
FIZZAH ALI ◽  
GUNESH KUMAR
Keyword(s):  
Analgesic Activity ◽  
Analgesic Effect ◽  
Research Work ◽  
Ethanol Extract ◽  
Nelumbo Nucifera ◽  
Herbal Remedies ◽  
Tail Flick ◽  
Traditional Use ◽  
Tail Flick Test ◽  
Pathway Inhibition

Objective: Utilization of herbal remedies rich in flavonoids and vitamins have increased significantly these days to treat various disorders, thus existing research work encircled to appraise the analgesic effect of Nelumbo nucifera fruit (NNF) for evaluating its traditional use pharmacologically in disorders which are associated with pain and inflammation. Methods: Central analgesic activity in mice was assessed by tail flick test and the latency time i.e. the removal of tail from the stimulus was recorded. Similarly acetic acid induced writhing test was also conducted for the assessment of peripheral analgesic effect in mice and number of writhes was counted along with percent inhibition of writhes. Results: In tail flick test the peek anti-nociceptive effect at all doses of fruit was observed at 90 min. However, the percentage of tail elongation time was highest at a dose of 200 mg/kg i.e. 82% at 90 min. Number of writhes was highly significantly reduced at all doses of NNF but maximum effects were observed at dose 200 mg/kg as compared to control, indicating 48.41 % inhibition of writhes. Conclusion: NNF have exhibited strong analgesic effect in both animal models, which may be connected with the synergistic actions of flavonoids, saponins and tannins on arachidonic acid pathway inhibition. Hence NNF seems to have a great potential in disorders associated with pain but more experimental trials in this field are required to confirm these findings.

scholarly journals Analgesic activity of allopurinol and febuxostat in experimental animals

2018 ◽  
Vol 7 (4) ◽  
pp. 603
Author(s):  
Yajnesh P. Sahu ◽  
Sachchidanand Pandey ◽  
Sabita Mohapatra
Keyword(s):  
Acetic Acid ◽  
Analgesic Activity ◽  
Physical Dependence ◽  
Experimental Pain ◽  
Opioid Analgesics ◽  
Analgesic Nephropathy ◽  
Tail Flick ◽  
Tail Flick Test ◽  
Analgesic Effects ◽  
Peripheral Analgesia

Background: Currently, two classes of analgesics, nonsteroidal anti-inflammatory drugs (NSAIDs) and opioid analgesics are used to manage pain in different clinical situations. Chronic uses of these drugs have various adverse effects like gastric ulceration/bleeding, analgesic nephropathy and respiratory depression, physical dependence, addiction, respectively. Xanthine oxidase inhibitors, used for chronic gout, might have a role in alleviation of pain, as per literature survey. Hence, the present study was carried out to evaluate the potential analgesic activity of allopurinol and febuxostat in different experimental models.Methods: The analgesic activity of allopurinol and febuxostat was assessed by employing two different experimental pain models-tail flick latency model in rats for central analgesia and acetic acid induced writhing model in mice for peripheral analgesia and was compared with tramadol and aspirin.Results: Allopurinol and febuxostat produced significant central and peripheral analgesic effects as is evident from increase in reaction time in tail flick test and inhibition in number of writhes in acetic acid induced writhing test.Conclusions: The results of the present study demonstrate marked analgesic effect of allopurinol and febuxostat.

EFFECTIVENESS PROGNOSTICATION OF A COMBINED ANALGESIC FORMULATION DEPENDING ON QUANTITATIVE COMPOSITION OF ITS COMPONENTS

2016 ◽  
pp. 44-48
Author(s):  
N. G. Vengerovich ◽  
M. A. Yudin ◽  
A. S. Nikiforov ◽  
G. S. Sagalov ◽  
M. S. Vakhviyainen ◽  
...  
Keyword(s):  
Drug Interaction ◽  
Opioid Receptor ◽  
Analgesic Activity ◽  
Analgesic Effect ◽  
Receptor Agonist ◽  
Quantitative Composition ◽  
Tail Flick ◽  
Tail Flick Test ◽  
Opioid Receptor Agonist ◽  
Combined Administration

In experiments on rats, analgesic activity of fentanyl opioid receptor agonist and central 2-adrenomimetic dexmedetomidine as well as the character of their interaction at a combined administration were studied. Meaneffective anesthetic doses of the drugs in heat radiant tail flick test were 54.5 and 22.5 μg/kg correspondingly. Using izobolographic analysis, it was shown that for a combination with equal parts or with a greater part of fentanyl, the type of drug interaction can be characterized as potentiation. A model of prognostication of probability values of the analgesic effect development in relation to doses of combination components was elaborated and experimentally tested.

scholarly journals ASSESSMENT OF ANALGESIC ACTIVITY OF NELUMBO NUCIFERA FRUIT ETHANOL EXTRACT

2019 ◽  
pp. 1-5
Author(s):  
MUHAMMAD ALI RAJPUT ◽  
TABASSUM ZEHRA ◽  
FIZZAH ALI ◽  
GUNESH KUMAR
Keyword(s):  
Analgesic Activity ◽  
Analgesic Effect ◽  
Research Work ◽  
Ethanol Extract ◽  
Nelumbo Nucifera ◽  
Herbal Remedies ◽  
Tail Flick ◽  
Traditional Use ◽  
Tail Flick Test ◽  
Pathway Inhibition

Objective: Utilization of herbal remedies rich in flavonoids and vitamins have increased significantly these days to treat various disorders, thus existing research work encircled to appraise the analgesic effect of Nelumbo nucifera fruit (NNF) for evaluating its traditional use pharmacologically in disorders which are associated with pain and inflammation. Methods: Central analgesic activity in mice was assessed by tail flick test and the latency time i.e. the removal of tail from the stimulus was recorded. Similarly acetic acid induced writhing test was also conducted for the assessment of peripheral analgesic effect in mice and number of writhes was counted along with percent inhibition of writhes. Results: In tail flick test the peek anti-nociceptive effect at all doses of fruit was observed at 90 min. However, the percentage of tail elongation time was highest at a dose of 200 mg/kg i.e. 82% at 90 min. Number of writhes was highly significantly reduced at all doses of NNF but maximum effects were observed at dose 200 mg/kg as compared to control, indicating 48.41 % inhibition of writhes. Conclusion: NNF have exhibited strong analgesic effect in both animal models, which may be connected with the synergistic actions of flavonoids, saponins and tannins on arachidonic acid pathway inhibition. Hence NNF seems to have a great potential in disorders associated with pain but more experimental trials in this field are required to confirm these findings.

scholarly journals AN AN STUDY OF ANALGESIC ACTIVITY OF HAFFNER’S TAIL CLIP METHOD ON ALBINO WISTAR RATS OF SOME POLYHERBAL FORMULATION

2019 ◽  
pp. 142-144
Author(s):  
LOKENDRA SINGH
Keyword(s):  
Analgesic Activity ◽  
Side Effect ◽  
Analgesic Effect ◽  
Design Method ◽  
Curcuma Longa ◽  
Albino Rats ◽  
Tail Flick ◽  
Herbal Drugs ◽  
Tail Flick Test ◽  
Tail Clip

Objective: Herbal drugs are more beneficial better than aspirin because this is an herb so no side effect this drug and it is easy to collect or use to as herbal drugs. Words are inadequate to describe the motivation for my work given to my beloved guide. I would like to add special thanks to my guide Gauravbilwal, for their guidance, support, and encouragement. Purpose (Hypothesis): The main purpose of this article pays to attention for herbal drugs because they are naturally old effective drugs. As well as, Ayurveda treatment is very older effective technique. Design/Method: Haffner gave to this technique of determining analgesic are around in 1929. Procedure: This technique according to tail if clipped with any object and tightly or will be compression generation of pain in the tail as well as mice starting to bite that portion of its tail, and could evaluate and recorded the response how much it bites tail quickly or in potential. Using this simple yet important marvel, we may apply the drug to be evaluated and record the response whether it bites tail quickly or in potential. If given drugs have analgesic likely, then rat will not bite its tail so frequently. Mice that do not show any response within 15 s will reject from the experiment. Results: The found in analgesic activity of additional compounds test to significant on tail flick test than acetic acid-induced test and thus it appears that the test compounds inhibit predominantly the peripheral pain mechanism. The results of the study indicate that the extracts of polyherbal plants of analgesic activity by reducing the abdominal constriction significantly and may supposed to have a possible role in inhibition of cyclooxygenase in the prostaglandin pathways (p****<0.0001, ***0.0001, *0.05). Conclusion: The present study showed the significant analgesic effect of both aqueous and alcoholic at 400 mg/kg doses in albino rats, we reported for the 1st time analgesic effect of different plants (Curcuma longa, Colchicaceae, Colocynthis, Withania somnifera, and Achyranthes aspera) in Haffner’s tail clip models. Aspirin has each uncoated effervescent tablet content are acetylsalicylic acid I.P. 325 mg. Finally summarized in this article represent a most effective results of herbal drugs equalized allopathic drugs without any other side effect. Hence, this is very usefully combination of Ayurveda drugs.

Semi-synthesis of Novel Buprenorphine Derivatives and their Anti-nociceptive Properties and Dependency Potential

2021 ◽  
Author(s):  
Zahra Hasanpour ◽  
Peyman Salehi ◽  
Lennart Bunch ◽  
Mona Khoramjouy ◽  
Morteza Bararjanian ◽  
...  
Keyword(s):  
Opioid Receptors ◽  
Analgesic Effect ◽  
Preference Test ◽  
Biological Properties ◽  
Place Preference ◽  
Tail Flick ◽  
Tail Flick Test ◽  
Active Compounds ◽  
Methyl Group ◽  
Analgesic Activities

Abstract: Novel 1,2,3-triazole-tethered N-norbuprenorphine derivatives with an OMe or OH group at the C3 position were synthesized alongside with evaluation of their analgesic properties. The analgesic activities of the resulting library were investigated via tail flick test in mice. Our results indicated that 10b and 10e were as effective as the starting compounds 8 and 9 with ED50 equal to 16.59 and 19.44 mg/kg, respectively. To investigate the effect of a methyl group at C3 on biological properties, the most active compounds were O-demethylated and their anti-nociceptive effects were assessed. The new O-demethylated derivatives (11b and 11e) showed better analgesic properties than the parent compounds with ED50 of 14.73 and 15.80 mg/kg, respectively. Naloxone prevented the analgesic effect of the synthesized compounds, indicating that the opioid receptors are highly involved in the anti-nociceptive effects of these. The potential dependency effects of the most potent derivatives were studied by condition place preference test in mice and compared to morphine and buprenorphine. Interestingly, 10b, 10e, 11b, and 11e did not show any dependency effect, similar to buprenorphine.

kappa-Opioid agonist inhibition of osmotically induced AVP release: preferential action at hypothalamic sites

1996 ◽  
Vol 270 (2) ◽  
pp. E367-E372 ◽  
Author(s):  
N. F. Rossi ◽  
D. P. Brooks
Keyword(s):  
Potent Inhibitor ◽  
Opiate Receptors ◽  
Opioid Antagonist ◽  
Posterior Pituitary ◽  
Opioid Agonist ◽  
Kappa Opioid ◽  
Water Diuresis ◽  
Kappa Agonist ◽  
Opioid Agonists ◽  
Kappa Opioid Agonist

Although several studies indicate that kappa-opioid agonists induce a water diuresis by inhibiting vasopressin (AVP) secretion, the locus of the kappa-receptors (neurohypophysial vs. hypothalamic) responsible for this effect remains unclear. We have ascertained the effect of the selective kappa-agonist BRL-52656 (BRL) on AVP secretion by using compartmentalized rat hypothalamoneurohypophysial explants in culture. When applied to the hypothalamus, nanomolar concentrations of BRL inhibited osmotically stimulated AVP secretion. This response was blocked by the highly selective kappa-opioid antagonist nor-binaltorphimine (BNI). However, osmotically stimulated AVP release was suppressed at the neurohypophysial site only by 100 nM BRL and was not reversed by BNI but only by naloxone. This dose of BRL, administered to the posterior pituitary compartment, did not appear to act by the agonist gaining access to hypothalamic kappa-opiate receptors, because BNI added to the hypothalamus failed to prevent the inhibition of AVP secretion. The data demonstrate that BRL is a potent inhibitor of osmotically stimulated AVP secretion via activation of kappa-opiate receptors within the hypothalamus, but that higher concentrations of the drug may also stimulate non-kappa-neurohypophysial opiate receptors that suppress AVP release.

scholarly journals EVALUATION OF ANALGESIC ACTIVITY OF MURRAYA KOENIGII AND CORIANDRUM SATIVUM LEAVES EXTRACT IN ANIMAL MODEL.

2018 ◽  
Vol 11 (1) ◽  
pp. 328
Author(s):  
Kartik Salwe J ◽  
Mirunalini R ◽  
Jervin Mano ◽  
Manimekalai K
Keyword(s):  
Analgesic Activity ◽  
Analgesic Effect ◽  
Coriandrum Sativum ◽  
Control Group ◽  
Tail Flick ◽  
Murraya Koenigii ◽  
Hot Plate ◽  
Plate Method ◽  
Standard Drug ◽  
Soxhlet Apparatus

 Objective: The objective of the study was to investigate the analgesic activity of hydroalcoholic extract of Murraya koenigii and Coriandrum sativum leaves and compared it with standard drug in an animal model.Methods: Hydroalcoholic extracts of M. koenigii and C. sativum leaves were obtained using Soxhlet apparatus. The central analgesic property was screened by hot plate method in mice and tail flick method in rats. The pain reaction time (PRT) was measured at 30, 60, and 120 min. The peripheral analgesic activity was evaluated by acetic acid induced writhing in mice.Results: In hot plate method M. koenigii leaves extract at both doses and tramadol showed significant increase in PRT at 30, 60, and 120 min compared with control group. C. sativum leaves extract showed significant increase in PRT only at 60 and 120 min compared to control group. In tail flick method M. koenigii leaves extract at both doses, higher dose of C. sativum leaves extract and tramadol showed significant increase in PRT at 30, 60, and 120 min compared with control group. Higher dose of M. koenigii leaves extract (200 mg/kg) was comparable with standard drug tramadol in both the methods. M. koenigii leaves extract at both dose showed significant reduction in the number of writhing but C. sativum leaves extract failed to show any significant reduction in the number of writhing compared with control. Higher dose of M. koenigii leaves extract was comparable with standard drug tramadol.Conclusion: M. koenigii leaves extract showed both peripheral and central analgesic effect while C. sativum leaves extract showed only peripheral analgesic effect.

Anti-Inflammatory, Antipyretic and Analgesic Potential of Zilla spinosa in Animal Model

2019 ◽  
Author(s):  
Riaz Ullah ◽  
Abdelaaty A Shahat ◽  
Ali S Alqahtani ◽  
Omer Mohammed Almarfad ◽  
Mohammad Sayer M Alharbi ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
Tail Flick ◽  
Chloroform Fraction ◽  
Test Model ◽  
Hot Plate Test ◽  
Tail Flick Test ◽  
Antipyretic Activity ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Analgesic Activities

The anti-inflammatory, antipyretic and analgesic activities of two concentrations (250 and 500 mg/kg) of the chloroform and butanol fractions of Zilla spinosa were determined. The carrageenan-induced rat paw edema assay was exercised for assessing the anti-inflammatory activity in rats, yeast-induced hyperthermia was utilized to assess the antipyretic activity in mice and the analgesic activity was measured by three different methods (hot-plate test model in mice, tail flick test in mice and acetic acid-induced writhing in mice). The antioxidant activity was studied by using the DPPH assay. The chloroform fraction of the methanol extract of Z. spinosa (ZSC) demonstrated the maximum inhibition of inflammation (50% at 500 mg/kg; 44% at 250 mg/kg). The chloroform fraction showed significant antipyretic activities (p andlt; 0.001 at 500 mg/kg) after 60 and 120 min of administration. ZSC also exhibited significant analgesic activity (p andlt;0.001). The butanol fraction (ZSB) was inactive in all the biological screening assays.

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